Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 （5 μm, 4....Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 （5 μm, 4.6 mm ×150 mm） column and a mobile phase of methanol： 0.01 mol·L^-1ammonium acetate （60：40, V/V） were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization （AP-ESI） mode and ion mass spectrum （m/z） of 314.9 [M＋H]^＋ for nifedipine, and 320.8 [M＋H]^＋ for lorazepam （Internal Standard, IS）. Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 （ r = 0.9997）, and the limit of quantitation （LOQ） was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test （T） or reference （R） were as the followings, t1/2 （6.73 ± 2.00） h and （7.04 ± 2.18） h, Tmax （4.28 ± 0.70） h and （4.48 ± 0.70） h, Cmax（39.66 ± 10.58） ng·mL^-1 and （40.19 ± 10.97） ng·mL^-1, AUC0-36 （391.63 ± 108.55） ng·mL^-1·h and （387.57 ± 121.51） ng·mL^-1·h, and AUC0-∞ （408.28 ± 121.16） ng·mL^-1·h and （406.15 ± 133.13） ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets （test） was （103.02 ± 13.93） %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.展开更多
A qualitative and quantitative test method of fingerprint of Wuji gastric floating sustained-release tablets was established. High performance liquid chromatography （HPLC） was adopted, using Agilent ZORBAX SB-C18 co...A qualitative and quantitative test method of fingerprint of Wuji gastric floating sustained-release tablets was established. High performance liquid chromatography （HPLC） was adopted, using Agilent ZORBAX SB-C18 column （250 mm×4.6 mm, 5 μm） as the chromatographic column, and acetonitrile-0.05 mol/L potassium dihydrogen phosphate solution as the mobile phase in a gradient elution with the flow rate of 1.0 mL/min. Sample solution （10 μL） was injected and was tested at the wavelength of 225 nm for 75 min at the column temperature of 30 ℃, Fingerprint similarity software （2004A version） was used to conduct data analysis. A total of 11 batches of Wuji gastric floating sustained-release tablets were tested and analyzed with HPLC fingerprint. Seventeen common peaks were found and the similarity of the 11 batches of agents was greater than 0.9, indicating that the production process of the agent is stable and feasible. The method is operable and could effectively control the quality of Wuji gastric floating sustained-release tablets.展开更多
The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms.Here,the 3D structures of doxazosin mesylate sustained-release...The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms.Here,the 3D structures of doxazosin mesylate sustained-release tablets were parallelly assessed by micro-computed tomography(micro-CT).There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution,but the generic preparation released slightly faster in media with ethanol during an alcohol-induced dose-dumping test.With their 3D structures obtained via micro-CT determination,the unique release behaviors of both RLD and the generic were investigated to reveal the effects of internal fine structure on the release kinetics.The structural parameters for both preparations were similar in conventional dissolution test,while the dissolutions in ethanol media showed some distinctions between RLD and generic preparations due to their static and dynamic structures.Furthermore,the findings revealed that the presence of ethanol accelerated dissolution and induced changes in internal structure of both RLD and generic preparations.Moreover,structure parameters like volume and area of outer contour,remaining solid volume and cavity volumewere not equivalent between the two formulations in 40%ethanol.In conclusion,the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control.展开更多
The contents of indapamide and related impurities in generic indapamide sustained-release tablets were simultaneously detected by a single-run high performance liquid chromatography equipped with photodiode array dete...The contents of indapamide and related impurities in generic indapamide sustained-release tablets were simultaneously detected by a single-run high performance liquid chromatography equipped with photodiode array detector(HPLC-PDA)method for the quality control in this paper.The results showed the method had a good selectivity and was validated through linearity,limits of detection and quantification,recovery,and precision.The linear ranges of indapamide,2-methyl-1-nitroso-2,3-dihydro-1H-indole(impurity A,ImA),4-chloro-N-(2-methyl-1H-indol-1-yl)-3-sulphamoyl-benzamide(impurity B,ImB)and 4-chloro-3-sulfamoylbenzoic acid(impurity 1,Im1)were 0.028-1.80μg/mL(R=0.99995),0.060-1.20μg/mL(R=0.9996),0.0324-1.20μg/mL(R=0.99985)and 0.060-1.20μg/mL(R=0.9997)with detection limits of 0.0093,0.012,0.012 and 0.006μg/mL,respectively.ImA and Im1 were not detectable in the generic drug.The content of indapamide was 96.7%of the labeled amount with a relative standard deviation(RSD)of 1.30%,and the percentage of ImB relative to the labeled amounts of indapamide was 0.106%with an RSD of 1.82%.The content of other unspecified impurities all met the reference quality standards.The results provided references for the quality control and the quality standard study of generic indapamide sustained-release tablets.展开更多
The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assay...The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.展开更多
Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divi...Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divided into 4 groups, 39 patients in group A （directed TCM permeation）, 26 patients in group B （oxycodone sustained-release tablets）, 32 patients in group C （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets）, and 29 patients group D （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets ＋ nimesulide sustained release tablets）, according to KPS scores. Results： Transdermal preparations of traditional Chinese medicine can significantly alleviate cancer pain. For the treatment of moderate to severe cancer pain, the Chinese medicine transdermal preparation can reduce the dosage of oxycodone sustained-release tablets. At the same time, the patient＇s KPS and NRS scores were significantly reduced. Moreover, the transdermal preparation of traditional Chinese medicine has a better therapeutic effect on visceral pain. Conclusion： The traditional Chinese medicine tra_nsdermal preparation combined with western medicine for the treatment of cancer pain may be a new method for the treatment of cancer pain.展开更多
Objective: To explore the therapeutic effect of nifedipine sustained-release tablets combined with enalapril in the treatment of elderly patients whose age above 60 years old with coronary heart disease and hypertensi...Objective: To explore the therapeutic effect of nifedipine sustained-release tablets combined with enalapril in the treatment of elderly patients whose age above 60 years old with coronary heart disease and hypertension. Methods: 260 elderly patients whose age above 60 years old with coronary heart disease and hypertension were selected and analyzed. The research time span was from August 2019 to April 2020. The patients were randomly divided into control group and observation group with 130 cases in each group. There was no significant difference in general data after statistical analysis. The treatment intervention program formulated by the control group was nifedipine sustained-release tablets, while the treatment intervention program formulated by the observation group was combined with enalapril on the basis of control group. The clinical value of nifedipine sustained-release tablets combined with enalapril was compared in the evaluation of condition control and safety of the two treatment regimens. Results: after the intervention of the two treatment schemes, the total effective rate of disease control treatment evaluation of elderly patients with coronary heart disease and hypertension was higher than that of the control group, and there were significant differences between groups, and statistical significance was indicated after analysis and calculation, (P < 0.05). There were no serious adverse reactions in the two groups during the treatment, there was no significant difference in the data between the groups, and there was no statistical significance after calculation and analysis, (P > 0.05). Conclusion: nifedipine sustained-release tablets combined with enalapril in the treatment of elderly patients with coronary heart disease and hypertension can achieve better clinical efficacy than use nifedipine sustained-release tablets alone, and will not increase the probability of adverse reactions, can improve the quality of life of patients, has the value of popularization and application.展开更多
The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitr...The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitro drug release rate of MHSRT and the commercial tablets Fortamet? made in the United States of America in water was fitted with zero order kinetic equation, and Ritger-Peppas kinetic equation in 0.1 M HCl and pH 6.8-phosphate buffer, respectively. The similarity factor f2 values of MHSRT in three different dissolution medium were 82, 80 and 74, respectively in comparison with imported Fortamet?, which were all greater than 50. The results of storage-stability showed that MHSRT were stable for at least 6 months under stress condition (40℃ ± 2℃, RH 75% ± 5%). Therefore, in this study, MHSRT were successfully prepared using optimized formulation technologies that meet mass produce. The in vitro release behavior of MHSRT was almost similar to that of imported Fortamet?.展开更多
Objective:To observe the clinical efficacy of Baitou Weng Decoction combined with mesalazine sustained-release tablets in the treatment of ulcerative colitis with febrile heat and its effect on immune function and ser...Objective:To observe the clinical efficacy of Baitou Weng Decoction combined with mesalazine sustained-release tablets in the treatment of ulcerative colitis with febrile heat and its effect on immune function and serum inflammatory factors.Methods: A total of 84 patients with ulcerative colitis were randomly divided into control group and treatment group, with 42 cases in each group. The control group was given mesalazine sustained-release tablets orally, while the treatment group was given Baitou Weng Decoction and mesalazine sustained-release tablets orally. The treatment period was 30 days and the patients were followed up for 3 months. After treatment, the clinical efficacy, quality of life, immune function and serum inflammatory factors of the two groups were observed.Results: The effective rate of treatment group (90.47%) was higher than that of control group (73.81%) (P<0.05);compared with before treatment, the scores of inflammatory bowel disease quality of life questionnaire scale in both groups were significantly improved (P<0.05), and the difference between the two groups was significant (P<0.05);after treatment, the plasma CD4+/CD8+ ratio and NK+ levels in both groups were significantly higher than those before treatment (P<0.05), and the treatment group was changed. The serum levels of tumor necrosis factor-α, interleukin-17 and interleukin-23 were significantly decreased in both groups after treatment (P<0.05), and the improvement was more significant in the treatment group (P<0.05). No significant adverse reactions were observed in the treatment group.Conclusions: Modified Baitou Weng Decoction combined with mesalazine in the treatment of heat-toxic and incandescent ulcerative colitis can significantly improve the clinical efficacy, improve the quality of life of patients, effectively regulate the expression level of serum inflammatory factors in ulcerative colitis patients, promote the recovery of patients' immune function, and have high drug safety.展开更多
In the present study,cefditoren sodium(CT-Na),the sodium salt form of cefditoren(CT),was selected as the model compound,and cholestyramine resin was employed as the drug carrier to formulate CT-Na-resin complexes.The ...In the present study,cefditoren sodium(CT-Na),the sodium salt form of cefditoren(CT),was selected as the model compound,and cholestyramine resin was employed as the drug carrier to formulate CT-Na-resin complexes.The interaction mechanism between CT-Na and cholestyramine resin was elucidated using scanning electron microscopy(SEM),fourier-transform infrared spectroscopy(FTIR),and differential scanning calorimetry(DSC).Bioadhesive,sustained-release microcapsules were subsequently developed via an emulsification—solvent evaporation technique.Comprehensive characterization of the formulation was conducted,with key quality indices systematically evaluated.Notably,the formulation exhibited minimal leakage(0.07%)after 7 d of storage and retained 94.59%of its drug content over a 6-month period.Pharmacokinetic studies comparing the CT-Na active pharmaceutical ingredient(APl)solution and the self-developed dry suspension revealed a marked extension in drug release for the latter.The dry suspension displayed a delayed T_(max)(3 h vs.2 h),an extended half-life(t_(1/2))(12.44 h vs.4 h),and a moderately reduced peak concentration(C_(max))(3.99μg/mL vs.4.82μg/mL),while achieving a significantly higher overall drug exposure(AUC_(0-24h):50.868μg·h/mL vs.30.281μg·h/mL).These findings indicated that relative to the API solution,the optimized dry suspension provided sustained drug release with improved bioavailability.展开更多
Objective:To investigate the effects of switching to either Prandilin 25R monotherapy or Prandilin 25R combined with ganagliflozin proline tablets after short-term intensive continuous subcutaneous insulin infusion du...Objective:To investigate the effects of switching to either Prandilin 25R monotherapy or Prandilin 25R combined with ganagliflozin proline tablets after short-term intensive continuous subcutaneous insulin infusion during hospitalization in elderly patients with type 2 diabetes mellitus on glycemic control,glycometabolic indicators,and cardiovascular risk factors,and to evaluate the safety of the two regimens.Methods:A total of 78 elderly patients with type 2 diabetes mellitus admitted to our hospital from January 2025 to September 2025 were selected and randomly divided into a control group and an observation group,with 39 cases in each group.The control group received monotherapy with insulin lispro protamine recombinant injection(Prandilin 25R)after intensive continuous subcutaneous insulin infusion,while the observation group received Prandilin 25R combined with ganagliflozin proline tablets.Continuous glucose monitoring(CGM)was performed for 14 days during the intensive continuous subcutaneous insulin infusion therapy phase in the hospital,followed by routine fingertip blood glucose monitoring after 14 days.Glycemic control indicators,glycometabolic indicators,and the incidence of adverse reactions were compared between the two groups.Results:After treatment,the mean amplitude of glycemic excursions and the 24-hour blood glucose standard deviation were significantly lower in the observation group than in the control group,while the time spent within the target blood glucose range was significantly higher(p<0.05).The levels of glycated hemoglobin,fasting blood glucose,and 2-hour postprandial blood glucose were better in the observation group than in the control group;moreover,the body mass index,systolic blood pressure,and blood lipid levels improved more significantly in the observation group than in the control group(p<0.05).There was no statistically significant difference in the incidence of hypoglycemia between the two groups.Conclusion:Combination therapy with ganagliflozin proline tablets after short-term intensive continuous subcutaneous insulin infusion therapy can effectively improve glycemic variability in elderly patients with type 2 diabetes mellitus,with good safety.This suggests that ganagliflozin proline tablets have a hypoglycemic advantage in the combination regimen and possess high clinical promotional value.展开更多
Spinal cord injury is accompanied by a substantial loss of neurons.Cell replacement therapy improves motor and sensory dysfunction by replacing dead neurons,and endogenous neurogenesis is an important cell replacement...Spinal cord injury is accompanied by a substantial loss of neurons.Cell replacement therapy improves motor and sensory dysfunction by replacing dead neurons,and endogenous neurogenesis is an important cell replacement source.Stimulating endogenous neurogenesis is therefore a viable approach for treating spinal cord injury.Given that basic fibroblast growth factor is a potent inducer of neurogenesis,we developed a sustained-release system of basic fibroblast growth factor-chitosan to enhance tissue repair in spinal cord injury.In the present study,we isolated neural stem cells from the spinal cords of neonatal rats and used single-cell RNA sequencing to trace the complete process of neurogenesis under ex vivo culture conditions.Under the influence of basic fibroblast growth factor-chitosan,neural stem cells were able to transition from a quiescent state to an activated state and subsequently differentiate into neuronal precursor cells and immature neurons.Additionally,basic fibroblast growth factor-chitosan significantly enhanced neural stem cell proliferation in vitro and promoted neuronal generation.Subsequent in vivo experiments confirmed the therapeutic efficacy of basic fibroblast growth factor-chitosan in spinal cord injury,demonstrating enhanced neurogenesis and tissue repair.展开更多
Background:Modified Qiangli Dingxuan Tablets(ZYSJ)is an optimized formulation derived from the classic Chinese patent medicine Qiangli Dingxuan Tablet.It targets the pathological features associated with metabolic hyp...Background:Modified Qiangli Dingxuan Tablets(ZYSJ)is an optimized formulation derived from the classic Chinese patent medicine Qiangli Dingxuan Tablet.It targets the pathological features associated with metabolic hypertension(MH)and metabolic disorders,although its antihypertensive mechanism remains unclear.Methods:A rat model of metabolic hypertension was established using a high-sugar,high-fat diet combined with progressively increasing concentrations of ethanol.Blood pressure,serum lipids,inflammatory cytokines,and endothelial function markers were assessed.Serum pharmacochemistry combined with network pharmacology was employed to predict key targets and pathways,followed by in vivo validation using qRT-PCR,Western blotting,immunofluorescence,and immunohistochemistry.Results:ZYSJ significantly reduced blood pressure and serum lipid levels in model rats.Thirty absorbed bioactive components were identified.Mechanistic studies revealed that ZYSJ downregulated the TLR4/MyD88/NF-κB signaling pathway at both the mRNA and protein levels,upregulated endothelial nitric oxide synthase(eNOS)expression,and decreased the levels of inflammatory cytokines(TNF-α,IL-1β,IL-6),thereby improving vascular endothelial function.Conclusion:ZYSJ effectively lowers blood pressure and serum lipids in rats with metabolic hypertension.Its mechanism of action is closely associated with regulation of the TLR4/MyD88/NF-κB signaling pathway,improvement of vascular endothelial function,and alleviation of inflammation.展开更多
The objective of this study is to design sustained-release tablets using matrix technology, which can well control the release of highly water-soluble drugs with good system robustness and simple preparation process. ...The objective of this study is to design sustained-release tablets using matrix technology, which can well control the release of highly water-soluble drugs with good system robustness and simple preparation process. Taking venlafaxine hydrochloride(VH) as a drug model, the feasibility of using chitosan(CS), carbomer(CBM) combination system to achieve this goal was studied. Formulation and process variables influencing drug release from CS–CBM matrix tablets were investigated. It was found that CS–CBM combination system weakened the potential influence of CS, CBM material properties and gastric emptying time on drug release profile. Demonstrated by direct observation, differential scanning calorimetry(DSC) and Fourier transform infrared spectroscopy(FTIR), in situ self-assembled polyelectrolyte complex(PEC) film was formed on the tablet surface during gastrointestinal tract transition, which contributed to the tunable and robust control of drug release. The sustained drug release behavior was further demonstrated in vivo in Beagle dogs, with level A in vitro and in vivo correlation(IVIVC) established successfully. In conclusion, CS–CBM matrix tablets are promising system to tune and control the release of highly water-soluble drugs with good system robustness.展开更多
The objective of this study was to prepare azithromycin(AZI)sustained-release products in order to allow for a high dose to be administered,reduce gastrointestinal side-effects and increase the compliance of patients....The objective of this study was to prepare azithromycin(AZI)sustained-release products in order to allow for a high dose to be administered,reduce gastrointestinal side-effects and increase the compliance of patients.AZI sustained-release tablets with different release performance(F-I:T_(100%)=3 h and F-II:T_(100%)=8 h in pH 6.0 phosphate buffer)were successfully prepared by wet granulation.The in vitro release rate and drug release mechanism were studied.The release rate of F-Iwas affected by dissolutionmedia with different pH,but not for F-II.HixsoneCrowellmodel was the best regression fitting model for F-I and F-II.Additionally,F-I and F-II both belonged to non-Fick diffusion.Oral pharmacokinetics of the two tablets and one AZI dispersible tablet as reference were studied in six healthy beagle dogs after oral administration.Compared with the reference,the C_(max)of F-I and F-II were decreased,and the T_(max)were prolonged,in that case which meet the requirement of sustained-release tablets.The relative bioavailability of F-I and F-II were 79.12%and 64.09%.T-test ofAUC_(0-144),and AUC_(0-∞)for F-I and F-II indicated there was no significant difference between F-I and F-II.These mean that the extended release rate did not induce different pharmacokinetics in vivo.展开更多
This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagl...This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagle dog plasma. Pharmacokinetic findings were compared among three preparation(lovastatin sustained-release tablet,T p; sustained-release capsule,T J and conventional capsule). Our results showed that the pharmacokinetic parameters in 6 dogs after single-dose oral administration of three perparations were calculated. T max, C max and MRT revealed significant difference (P<0.05). Relative bioavailability was 111.5±16.9 % (T P) and 110.4%±9.6 % (T J). The pharmacokinetic parameters in the 6 dogs after multiple-dose oral administration of three perparations, T max, C max MRT and DF had significant difference (P<0.05); C av , C min and AUC 0-24 h displayed no significant difference (P>0.05). It is concluded that the lovastatin sustained-release tablet and sustained-release capsule are able to maintain a sustained-release for 24 h.展开更多
Different dosage forms can significantly impact pharmacokinetics in vivo,leading to varied effects and potential adverse reactions.This study aimed to evaluate the efficacy,safety,and cost-effectiveness of isosorbide ...Different dosage forms can significantly impact pharmacokinetics in vivo,leading to varied effects and potential adverse reactions.This study aimed to evaluate the efficacy,safety,and cost-effectiveness of isosorbide mononitrate sustained-release capsules(IMSRC)combined with conventional treatments,compared to isosorbide mononitrate tablets(IMT)combined with conventional treatments,for managing angina pectoris in patients with coronary heart diseases.A network meta-analysis(NMA)was conducted to assess the efficacy and safety of IMSRC and IMT.Relevant literature was sourced from databases,including PubMed,Embase,Cochrane Library,ScienceDirect,Web of Science,CNKI,Wanfang,and VIP,covering publications up to July 2023.The cost-effectiveness analysis(CEA)was performed from the perspective of China’s healthcare system,utilizing inputs derived from the NMA.The analysis included 15 studies.The NMA results revealed no significant difference in efficacy and safety between IMSRC plus conventional treatments and IMT plus conventional treatments.However,both combinations were more effective than conventional treatments without isosorbide mononitrate.No differences in safety were observed among the three groups.The surface under the cumulative ranking(SUCRA)of the NMA indicated that IMT had a slight edge over IMSRC in the total effective rate of angina pectoris,whereas IMSRC showed higher probabilities for markedly effective rate and ECG effective rate compared to IMT.The incidence of adverse events was ranked as IMT>conventional preparation>IMSRC.The CEA results highlighted that the incremental cost-effectiveness ratios(ICERs)for the markedly effective and total effective rates of angina pectoris were-133.41 and-260.20,respectively.The ICERs for ECG effective rates were-83.34 and-234.24,respectively.In conclusion,while IMSRC combined with conventional treatments and IMT combined with conventional treatments were similar in efficacy and safety,IMSRC proved to be more economical.展开更多
BACKGROUND Rheumatic immune diseases are a group of chronic inflammatory diseases charac-terized by joint and systemic multi-organ involvement,including rheumatoid arthritis,systemic lupus erythematosus,and Sjogren’s...BACKGROUND Rheumatic immune diseases are a group of chronic inflammatory diseases charac-terized by joint and systemic multi-organ involvement,including rheumatoid arthritis,systemic lupus erythematosus,and Sjogren’s syndrome,among others.The pathogenesis of these diseases is related to the abnormal activation and regulatory imbalance of the immune system.The prevalence and morbidity of rheumatic immune diseases are high,imposing a significant burden on patients'quality of life and socio-economic costs.Currently,the treatment of rheumatic immune diseases mainly relies on Western medicine,such as non-steroidal anti-inflammatory drugs,glucocorticoids,disease-modifying antirheumatic drugs,and biologics.However,the therapeutic effects of Western medicine are not ideal,some patients poorly respond or are resistant to Western medicine,and long-term use often causes various adverse reactions.AIM To systematically evaluate the efficacy and safety of Tripterygium wilfordii gly-cosides tablets combined with Western medicine in the treatment of patients with rheumatic immune diseases.METHODS This study conducted a meta-analysis to systematically evaluate the efficacy and safety of Tripterygium wilfordii glycosides tablets combined with Western medicine for patients with rheumatic immune diseases.Chinese and English databases were searched for randomized controlled trials(RCTs)on the treatment of rheumatic immune diseases with Tripterygium wilfordii glycosides tablets combined with Western medicine.The quality of the included studies was assessed using the Cochrane risk of bias assessment tool.Meta-analysis was performed using RevMan 5.4 software.RESULTS The meta-analysis included 11 RCTs involving 1026 patients with rheumatic immune diseases.The combined treatment significantly reduced the risk of disease recurrence(relative risk=1.07,95%confidence interval:1.01-1.15,P<0.05)and showed no significant heterogeneity(I2=0%,P=0.53),indicating that Tripterygium wilfordii glycosides tablets combined with Western medicine is an effective method to reduce the possibility of postoperative recurrence in patients with rheumatic immune diseases.However,due to the limited number and quality of the studies included,these results should be interpreted with caution.CONCLUSION Tripterygium wilfordii glycosides tablets combined with Western medicine is an effective and safe treatment option for patients with rheumatic immune diseases and can be considered a clinical choice.However,more high-quality research is needed to validate this conclusion and provide more solid evidence for clinical practice.展开更多
Oseltamivir phosphate(OP),renowned as one of the most effective drugs for influenza treatment,encounters several challenges,including poor stability,difficulty in swallowing,and a bitter taste,thereby limiting its com...Oseltamivir phosphate(OP),renowned as one of the most effective drugs for influenza treatment,encounters several challenges,including poor stability,difficulty in swallowing,and a bitter taste,thereby limiting its compliance,particularly among children.Consequently,this study aimed to devise a novel sustained-release suspension of OP employing an ion exchange resin as a carrier to address these challenges.The OP-drug resin complex(OP-DRC)was synthesized utilizing ion exchange technology,while OP-coated microcapsules(OP-CM)were fabricated via the emulsion-evaporation method.The optimization of the formulation process for the OP sustained-release suspension was achieved through a combination of single-factor experimentation and orthogonal experimental design.Furthermore,the drug release kinetics and pharmacokinetic properties of the sustained-release suspension were thoroughly evaluated both in vitro and in vivo.Scanning electron microscopy(SEM),X-ray diffraction(XRD),and attenuated total reflectance Fourier-transform infrared spectroscopy(ATR-FTIR)analyses confirmed the formation of drug-resin complexes via ionic bonding.The in vitro cumulative release rates were found to be 16%(1 h),53%(6 h),and 84%(24 h),respectively.Notably,the self-made sustained-release suspension exhibited an extended half-life(21.518 h),delayed time to peak concentration(T_(max))(6 h),and reduced maximum plasma concentration(C_(max))(0.397μg/mL)in comparison to commercial granules(half-life=8.466 h;T_(max)=2 h;C_(max)=0.631μg/mL).Additionally,the area under the curve(AUC)indicated that the bioavailability of the self-made OP suspension surpassed that of the commercial OP granules by 101%.These findings underscored the successful development of an oral OP sustained-release suspension characterized by stability,tastelessness,ease of swallowing,convenient administration,and sustained-release properties,thereby potentially enhancing drug compliance among children.展开更多
Objective:To evaluate the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease,in order to provide a more scientific basis for the application of the drug in Parkinson’s disease.Methods:...Objective:To evaluate the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease,in order to provide a more scientific basis for the application of the drug in Parkinson’s disease.Methods:This study is a single-arm,prospective,observational study.The trial collected patients with primary Parkinson’s disease who met the inclusion and exclusion criteria after being assessed by the investigator to evaluate the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease patients through UPDRSIII and UPDRSII scales,and evaluated the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease patients.Results:A total of 3560 patients were included in this study.44.1%of patients had early Parkinson’s disease,52.4%had intermediate Parkinson’s disease,and 3.5%had advanced Parkinson’s disease.The UPDRSIII(exercise capacity)score was 26.76 at baseline,25.47 at 1 month,24.18 at 2 months,and 23.39 at 3 months after treatment,and scores significantly improved over time(P<0.001).The UPDRSII(ability to perform daily living)score was an average of 23.60 at baseline,22.49 at 1 month,21.53 at 2 months,and 21.09 at 3 months after treatment,with statistically significant differences in scores between months(P<0.001).A total of 18 adverse events/reactions occurred in this study,and adverse symptoms eventually disappeared or resolved,without termination due to adverse events/reactions or patient discharge.Conclusion:Rasagiline tablets have significant efficacy in improving daily exercise capacity and living ability in patients with Parkinson’s disease,and have a certain safety,which supports the effectiveness of rasagiline as a treatment for Parkinson’s disease and provides new evidence for its clinical application.展开更多
文摘Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 （5 μm, 4.6 mm ×150 mm） column and a mobile phase of methanol： 0.01 mol·L^-1ammonium acetate （60：40, V/V） were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization （AP-ESI） mode and ion mass spectrum （m/z） of 314.9 [M＋H]^＋ for nifedipine, and 320.8 [M＋H]^＋ for lorazepam （Internal Standard, IS）. Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 （ r = 0.9997）, and the limit of quantitation （LOQ） was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test （T） or reference （R） were as the followings, t1/2 （6.73 ± 2.00） h and （7.04 ± 2.18） h, Tmax （4.28 ± 0.70） h and （4.48 ± 0.70） h, Cmax（39.66 ± 10.58） ng·mL^-1 and （40.19 ± 10.97） ng·mL^-1, AUC0-36 （391.63 ± 108.55） ng·mL^-1·h and （387.57 ± 121.51） ng·mL^-1·h, and AUC0-∞ （408.28 ± 121.16） ng·mL^-1·h and （406.15 ± 133.13） ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets （test） was （103.02 ± 13.93） %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.
基金The National Natural Science Foundation of China(Grant No.81460609)
文摘A qualitative and quantitative test method of fingerprint of Wuji gastric floating sustained-release tablets was established. High performance liquid chromatography （HPLC） was adopted, using Agilent ZORBAX SB-C18 column （250 mm×4.6 mm, 5 μm） as the chromatographic column, and acetonitrile-0.05 mol/L potassium dihydrogen phosphate solution as the mobile phase in a gradient elution with the flow rate of 1.0 mL/min. Sample solution （10 μL） was injected and was tested at the wavelength of 225 nm for 75 min at the column temperature of 30 ℃, Fingerprint similarity software （2004A version） was used to conduct data analysis. A total of 11 batches of Wuji gastric floating sustained-release tablets were tested and analyzed with HPLC fingerprint. Seventeen common peaks were found and the similarity of the 11 batches of agents was greater than 0.9, indicating that the production process of the agent is stable and feasible. The method is operable and could effectively control the quality of Wuji gastric floating sustained-release tablets.
基金This work was supported by the Key Programfor International Science and Technology Cooperation Projects of China(2020YFE0201700)State Drug Administration key laboratory project(2024HYZX04).
文摘The structures of solid dosage forms determine their release behaviors and are critical attributes for the design and evaluation of the solid dosage forms.Here,the 3D structures of doxazosin mesylate sustained-release tablets were parallelly assessed by micro-computed tomography(micro-CT).There were no significant differences observed in the release profiles between the RLD and the generic formulation in the conventional dissolution,but the generic preparation released slightly faster in media with ethanol during an alcohol-induced dose-dumping test.With their 3D structures obtained via micro-CT determination,the unique release behaviors of both RLD and the generic were investigated to reveal the effects of internal fine structure on the release kinetics.The structural parameters for both preparations were similar in conventional dissolution test,while the dissolutions in ethanol media showed some distinctions between RLD and generic preparations due to their static and dynamic structures.Furthermore,the findings revealed that the presence of ethanol accelerated dissolution and induced changes in internal structure of both RLD and generic preparations.Moreover,structure parameters like volume and area of outer contour,remaining solid volume and cavity volumewere not equivalent between the two formulations in 40%ethanol.In conclusion,the structure data obtained from this study provided valuable insights into the diverse release behaviors observed in various modified-release formulations in drug development and quality control.
基金the Natural Science Foundation of Anhui Province,China(11040606M41)the Natural Science Project in Colleges and Universities of Anhui Province,China(kj2016A683)the Natural Science Project of Huangshan University,China(hxkt20190042,xdhz202007)。
文摘The contents of indapamide and related impurities in generic indapamide sustained-release tablets were simultaneously detected by a single-run high performance liquid chromatography equipped with photodiode array detector(HPLC-PDA)method for the quality control in this paper.The results showed the method had a good selectivity and was validated through linearity,limits of detection and quantification,recovery,and precision.The linear ranges of indapamide,2-methyl-1-nitroso-2,3-dihydro-1H-indole(impurity A,ImA),4-chloro-N-(2-methyl-1H-indol-1-yl)-3-sulphamoyl-benzamide(impurity B,ImB)and 4-chloro-3-sulfamoylbenzoic acid(impurity 1,Im1)were 0.028-1.80μg/mL(R=0.99995),0.060-1.20μg/mL(R=0.9996),0.0324-1.20μg/mL(R=0.99985)and 0.060-1.20μg/mL(R=0.9997)with detection limits of 0.0093,0.012,0.012 and 0.006μg/mL,respectively.ImA and Im1 were not detectable in the generic drug.The content of indapamide was 96.7%of the labeled amount with a relative standard deviation(RSD)of 1.30%,and the percentage of ImB relative to the labeled amounts of indapamide was 0.106%with an RSD of 1.82%.The content of other unspecified impurities all met the reference quality standards.The results provided references for the quality control and the quality standard study of generic indapamide sustained-release tablets.
文摘The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.
文摘Objective： To study the effect of the transdermal preparation of traditional Chinese medicine in treating cancer pain. Methods： From October 2016 to January 2018, 126 patients with cancer pain were enrolled and divided into 4 groups, 39 patients in group A （directed TCM permeation）, 26 patients in group B （oxycodone sustained-release tablets）, 32 patients in group C （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets）, and 29 patients group D （Chinese medicine directed drug penetration ＋ oxycodone sustained-release tablets ＋ nimesulide sustained release tablets）, according to KPS scores. Results： Transdermal preparations of traditional Chinese medicine can significantly alleviate cancer pain. For the treatment of moderate to severe cancer pain, the Chinese medicine transdermal preparation can reduce the dosage of oxycodone sustained-release tablets. At the same time, the patient＇s KPS and NRS scores were significantly reduced. Moreover, the transdermal preparation of traditional Chinese medicine has a better therapeutic effect on visceral pain. Conclusion： The traditional Chinese medicine tra_nsdermal preparation combined with western medicine for the treatment of cancer pain may be a new method for the treatment of cancer pain.
文摘Objective: To explore the therapeutic effect of nifedipine sustained-release tablets combined with enalapril in the treatment of elderly patients whose age above 60 years old with coronary heart disease and hypertension. Methods: 260 elderly patients whose age above 60 years old with coronary heart disease and hypertension were selected and analyzed. The research time span was from August 2019 to April 2020. The patients were randomly divided into control group and observation group with 130 cases in each group. There was no significant difference in general data after statistical analysis. The treatment intervention program formulated by the control group was nifedipine sustained-release tablets, while the treatment intervention program formulated by the observation group was combined with enalapril on the basis of control group. The clinical value of nifedipine sustained-release tablets combined with enalapril was compared in the evaluation of condition control and safety of the two treatment regimens. Results: after the intervention of the two treatment schemes, the total effective rate of disease control treatment evaluation of elderly patients with coronary heart disease and hypertension was higher than that of the control group, and there were significant differences between groups, and statistical significance was indicated after analysis and calculation, (P < 0.05). There were no serious adverse reactions in the two groups during the treatment, there was no significant difference in the data between the groups, and there was no statistical significance after calculation and analysis, (P > 0.05). Conclusion: nifedipine sustained-release tablets combined with enalapril in the treatment of elderly patients with coronary heart disease and hypertension can achieve better clinical efficacy than use nifedipine sustained-release tablets alone, and will not increase the probability of adverse reactions, can improve the quality of life of patients, has the value of popularization and application.
文摘The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitro drug release rate of MHSRT and the commercial tablets Fortamet? made in the United States of America in water was fitted with zero order kinetic equation, and Ritger-Peppas kinetic equation in 0.1 M HCl and pH 6.8-phosphate buffer, respectively. The similarity factor f2 values of MHSRT in three different dissolution medium were 82, 80 and 74, respectively in comparison with imported Fortamet?, which were all greater than 50. The results of storage-stability showed that MHSRT were stable for at least 6 months under stress condition (40℃ ± 2℃, RH 75% ± 5%). Therefore, in this study, MHSRT were successfully prepared using optimized formulation technologies that meet mass produce. The in vitro release behavior of MHSRT was almost similar to that of imported Fortamet?.
基金This study was supported by the Liaoning Natural Science Foundation Guiding Plan Project(Grant 20170540609).
文摘Objective:To observe the clinical efficacy of Baitou Weng Decoction combined with mesalazine sustained-release tablets in the treatment of ulcerative colitis with febrile heat and its effect on immune function and serum inflammatory factors.Methods: A total of 84 patients with ulcerative colitis were randomly divided into control group and treatment group, with 42 cases in each group. The control group was given mesalazine sustained-release tablets orally, while the treatment group was given Baitou Weng Decoction and mesalazine sustained-release tablets orally. The treatment period was 30 days and the patients were followed up for 3 months. After treatment, the clinical efficacy, quality of life, immune function and serum inflammatory factors of the two groups were observed.Results: The effective rate of treatment group (90.47%) was higher than that of control group (73.81%) (P<0.05);compared with before treatment, the scores of inflammatory bowel disease quality of life questionnaire scale in both groups were significantly improved (P<0.05), and the difference between the two groups was significant (P<0.05);after treatment, the plasma CD4+/CD8+ ratio and NK+ levels in both groups were significantly higher than those before treatment (P<0.05), and the treatment group was changed. The serum levels of tumor necrosis factor-α, interleukin-17 and interleukin-23 were significantly decreased in both groups after treatment (P<0.05), and the improvement was more significant in the treatment group (P<0.05). No significant adverse reactions were observed in the treatment group.Conclusions: Modified Baitou Weng Decoction combined with mesalazine in the treatment of heat-toxic and incandescent ulcerative colitis can significantly improve the clinical efficacy, improve the quality of life of patients, effectively regulate the expression level of serum inflammatory factors in ulcerative colitis patients, promote the recovery of patients' immune function, and have high drug safety.
基金The 2023 Nantong Jianghai Talents Project2023 Nantong Social Livelihood Science and Technology Plan+2 种基金2022 New Drugs and Platform Enhancement Project of the Yangtze Delta Drug Advanced Research InstituteWuyi University Scientific Research Project (Grant No.2023AL001)the Innovation and Entrepreneurship Project for Returned Overseas Students in Jiangmen。
文摘In the present study,cefditoren sodium(CT-Na),the sodium salt form of cefditoren(CT),was selected as the model compound,and cholestyramine resin was employed as the drug carrier to formulate CT-Na-resin complexes.The interaction mechanism between CT-Na and cholestyramine resin was elucidated using scanning electron microscopy(SEM),fourier-transform infrared spectroscopy(FTIR),and differential scanning calorimetry(DSC).Bioadhesive,sustained-release microcapsules were subsequently developed via an emulsification—solvent evaporation technique.Comprehensive characterization of the formulation was conducted,with key quality indices systematically evaluated.Notably,the formulation exhibited minimal leakage(0.07%)after 7 d of storage and retained 94.59%of its drug content over a 6-month period.Pharmacokinetic studies comparing the CT-Na active pharmaceutical ingredient(APl)solution and the self-developed dry suspension revealed a marked extension in drug release for the latter.The dry suspension displayed a delayed T_(max)(3 h vs.2 h),an extended half-life(t_(1/2))(12.44 h vs.4 h),and a moderately reduced peak concentration(C_(max))(3.99μg/mL vs.4.82μg/mL),while achieving a significantly higher overall drug exposure(AUC_(0-24h):50.868μg·h/mL vs.30.281μg·h/mL).These findings indicated that relative to the API solution,the optimized dry suspension provided sustained drug release with improved bioavailability.
文摘Objective:To investigate the effects of switching to either Prandilin 25R monotherapy or Prandilin 25R combined with ganagliflozin proline tablets after short-term intensive continuous subcutaneous insulin infusion during hospitalization in elderly patients with type 2 diabetes mellitus on glycemic control,glycometabolic indicators,and cardiovascular risk factors,and to evaluate the safety of the two regimens.Methods:A total of 78 elderly patients with type 2 diabetes mellitus admitted to our hospital from January 2025 to September 2025 were selected and randomly divided into a control group and an observation group,with 39 cases in each group.The control group received monotherapy with insulin lispro protamine recombinant injection(Prandilin 25R)after intensive continuous subcutaneous insulin infusion,while the observation group received Prandilin 25R combined with ganagliflozin proline tablets.Continuous glucose monitoring(CGM)was performed for 14 days during the intensive continuous subcutaneous insulin infusion therapy phase in the hospital,followed by routine fingertip blood glucose monitoring after 14 days.Glycemic control indicators,glycometabolic indicators,and the incidence of adverse reactions were compared between the two groups.Results:After treatment,the mean amplitude of glycemic excursions and the 24-hour blood glucose standard deviation were significantly lower in the observation group than in the control group,while the time spent within the target blood glucose range was significantly higher(p<0.05).The levels of glycated hemoglobin,fasting blood glucose,and 2-hour postprandial blood glucose were better in the observation group than in the control group;moreover,the body mass index,systolic blood pressure,and blood lipid levels improved more significantly in the observation group than in the control group(p<0.05).There was no statistically significant difference in the incidence of hypoglycemia between the two groups.Conclusion:Combination therapy with ganagliflozin proline tablets after short-term intensive continuous subcutaneous insulin infusion therapy can effectively improve glycemic variability in elderly patients with type 2 diabetes mellitus,with good safety.This suggests that ganagliflozin proline tablets have a hypoglycemic advantage in the combination regimen and possess high clinical promotional value.
基金supported by the National Natural Science Foundation of China,Nos.82271403(to XL),82272171(to ZY),31730030(to XL),81941011(to XL),31971279(to ZY)the Natural Science Foundation of Beijing,No.7222004(to HD).
文摘Spinal cord injury is accompanied by a substantial loss of neurons.Cell replacement therapy improves motor and sensory dysfunction by replacing dead neurons,and endogenous neurogenesis is an important cell replacement source.Stimulating endogenous neurogenesis is therefore a viable approach for treating spinal cord injury.Given that basic fibroblast growth factor is a potent inducer of neurogenesis,we developed a sustained-release system of basic fibroblast growth factor-chitosan to enhance tissue repair in spinal cord injury.In the present study,we isolated neural stem cells from the spinal cords of neonatal rats and used single-cell RNA sequencing to trace the complete process of neurogenesis under ex vivo culture conditions.Under the influence of basic fibroblast growth factor-chitosan,neural stem cells were able to transition from a quiescent state to an activated state and subsequently differentiate into neuronal precursor cells and immature neurons.Additionally,basic fibroblast growth factor-chitosan significantly enhanced neural stem cell proliferation in vitro and promoted neuronal generation.Subsequent in vivo experiments confirmed the therapeutic efficacy of basic fibroblast growth factor-chitosan in spinal cord injury,demonstrating enhanced neurogenesis and tissue repair.
基金supported by Natural science foundation of Zhejiang province(No.ZCLMS25H2801 to Ying-Jie Dong)Zhejiang Provincial"Vanguard"and"Leading Goose"R&D Tackling Program(No.2025C02183 to Su-Hong Chen)+1 种基金National Natural Science Foundation of China(No.82274134 to Su-Hong Chen and No.82404900 to Ying-Jie Dong)the Key Laboratory of Zhejiang Province(No.2012E10002 to Gui-Yuan Lv).
文摘Background:Modified Qiangli Dingxuan Tablets(ZYSJ)is an optimized formulation derived from the classic Chinese patent medicine Qiangli Dingxuan Tablet.It targets the pathological features associated with metabolic hypertension(MH)and metabolic disorders,although its antihypertensive mechanism remains unclear.Methods:A rat model of metabolic hypertension was established using a high-sugar,high-fat diet combined with progressively increasing concentrations of ethanol.Blood pressure,serum lipids,inflammatory cytokines,and endothelial function markers were assessed.Serum pharmacochemistry combined with network pharmacology was employed to predict key targets and pathways,followed by in vivo validation using qRT-PCR,Western blotting,immunofluorescence,and immunohistochemistry.Results:ZYSJ significantly reduced blood pressure and serum lipid levels in model rats.Thirty absorbed bioactive components were identified.Mechanistic studies revealed that ZYSJ downregulated the TLR4/MyD88/NF-κB signaling pathway at both the mRNA and protein levels,upregulated endothelial nitric oxide synthase(eNOS)expression,and decreased the levels of inflammatory cytokines(TNF-α,IL-1β,IL-6),thereby improving vascular endothelial function.Conclusion:ZYSJ effectively lowers blood pressure and serum lipids in rats with metabolic hypertension.Its mechanism of action is closely associated with regulation of the TLR4/MyD88/NF-κB signaling pathway,improvement of vascular endothelial function,and alleviation of inflammation.
基金supported by the Distinguished Professor Project of Liaoning Province(2015)
文摘The objective of this study is to design sustained-release tablets using matrix technology, which can well control the release of highly water-soluble drugs with good system robustness and simple preparation process. Taking venlafaxine hydrochloride(VH) as a drug model, the feasibility of using chitosan(CS), carbomer(CBM) combination system to achieve this goal was studied. Formulation and process variables influencing drug release from CS–CBM matrix tablets were investigated. It was found that CS–CBM combination system weakened the potential influence of CS, CBM material properties and gastric emptying time on drug release profile. Demonstrated by direct observation, differential scanning calorimetry(DSC) and Fourier transform infrared spectroscopy(FTIR), in situ self-assembled polyelectrolyte complex(PEC) film was formed on the tablet surface during gastrointestinal tract transition, which contributed to the tunable and robust control of drug release. The sustained drug release behavior was further demonstrated in vivo in Beagle dogs, with level A in vitro and in vivo correlation(IVIVC) established successfully. In conclusion, CS–CBM matrix tablets are promising system to tune and control the release of highly water-soluble drugs with good system robustness.
文摘The objective of this study was to prepare azithromycin(AZI)sustained-release products in order to allow for a high dose to be administered,reduce gastrointestinal side-effects and increase the compliance of patients.AZI sustained-release tablets with different release performance(F-I:T_(100%)=3 h and F-II:T_(100%)=8 h in pH 6.0 phosphate buffer)were successfully prepared by wet granulation.The in vitro release rate and drug release mechanism were studied.The release rate of F-Iwas affected by dissolutionmedia with different pH,but not for F-II.HixsoneCrowellmodel was the best regression fitting model for F-I and F-II.Additionally,F-I and F-II both belonged to non-Fick diffusion.Oral pharmacokinetics of the two tablets and one AZI dispersible tablet as reference were studied in six healthy beagle dogs after oral administration.Compared with the reference,the C_(max)of F-I and F-II were decreased,and the T_(max)were prolonged,in that case which meet the requirement of sustained-release tablets.The relative bioavailability of F-I and F-II were 79.12%and 64.09%.T-test ofAUC_(0-144),and AUC_(0-∞)for F-I and F-II indicated there was no significant difference between F-I and F-II.These mean that the extended release rate did not induce different pharmacokinetics in vivo.
文摘This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagle dog plasma. Pharmacokinetic findings were compared among three preparation(lovastatin sustained-release tablet,T p; sustained-release capsule,T J and conventional capsule). Our results showed that the pharmacokinetic parameters in 6 dogs after single-dose oral administration of three perparations were calculated. T max, C max and MRT revealed significant difference (P<0.05). Relative bioavailability was 111.5±16.9 % (T P) and 110.4%±9.6 % (T J). The pharmacokinetic parameters in the 6 dogs after multiple-dose oral administration of three perparations, T max, C max MRT and DF had significant difference (P<0.05); C av , C min and AUC 0-24 h displayed no significant difference (P>0.05). It is concluded that the lovastatin sustained-release tablet and sustained-release capsule are able to maintain a sustained-release for 24 h.
基金The 2022 Ministry of Education General Project for Humanities and Social Sciences Research(Grant No.22YJAZH147)the General Subject of Guangzhou Philosophy and Social Science Development“14th Five-Year Plan”in 2023(Grant No.2023GZYB68)+2 种基金China University Industry-Academia-Research Innovation Fund-Huatong Guokang Medical Research Special Project(Grant No.2023HT017)2024 Guangdong Province General Project for the Planning of Philosophy and Social Sciences(Grant No.GD24CGL29)the Innovation Team Project of Colleges and Universities in Guangdong Province(Grant No.2022WCXTD011).
文摘Different dosage forms can significantly impact pharmacokinetics in vivo,leading to varied effects and potential adverse reactions.This study aimed to evaluate the efficacy,safety,and cost-effectiveness of isosorbide mononitrate sustained-release capsules(IMSRC)combined with conventional treatments,compared to isosorbide mononitrate tablets(IMT)combined with conventional treatments,for managing angina pectoris in patients with coronary heart diseases.A network meta-analysis(NMA)was conducted to assess the efficacy and safety of IMSRC and IMT.Relevant literature was sourced from databases,including PubMed,Embase,Cochrane Library,ScienceDirect,Web of Science,CNKI,Wanfang,and VIP,covering publications up to July 2023.The cost-effectiveness analysis(CEA)was performed from the perspective of China’s healthcare system,utilizing inputs derived from the NMA.The analysis included 15 studies.The NMA results revealed no significant difference in efficacy and safety between IMSRC plus conventional treatments and IMT plus conventional treatments.However,both combinations were more effective than conventional treatments without isosorbide mononitrate.No differences in safety were observed among the three groups.The surface under the cumulative ranking(SUCRA)of the NMA indicated that IMT had a slight edge over IMSRC in the total effective rate of angina pectoris,whereas IMSRC showed higher probabilities for markedly effective rate and ECG effective rate compared to IMT.The incidence of adverse events was ranked as IMT>conventional preparation>IMSRC.The CEA results highlighted that the incremental cost-effectiveness ratios(ICERs)for the markedly effective and total effective rates of angina pectoris were-133.41 and-260.20,respectively.The ICERs for ECG effective rates were-83.34 and-234.24,respectively.In conclusion,while IMSRC combined with conventional treatments and IMT combined with conventional treatments were similar in efficacy and safety,IMSRC proved to be more economical.
文摘BACKGROUND Rheumatic immune diseases are a group of chronic inflammatory diseases charac-terized by joint and systemic multi-organ involvement,including rheumatoid arthritis,systemic lupus erythematosus,and Sjogren’s syndrome,among others.The pathogenesis of these diseases is related to the abnormal activation and regulatory imbalance of the immune system.The prevalence and morbidity of rheumatic immune diseases are high,imposing a significant burden on patients'quality of life and socio-economic costs.Currently,the treatment of rheumatic immune diseases mainly relies on Western medicine,such as non-steroidal anti-inflammatory drugs,glucocorticoids,disease-modifying antirheumatic drugs,and biologics.However,the therapeutic effects of Western medicine are not ideal,some patients poorly respond or are resistant to Western medicine,and long-term use often causes various adverse reactions.AIM To systematically evaluate the efficacy and safety of Tripterygium wilfordii gly-cosides tablets combined with Western medicine in the treatment of patients with rheumatic immune diseases.METHODS This study conducted a meta-analysis to systematically evaluate the efficacy and safety of Tripterygium wilfordii glycosides tablets combined with Western medicine for patients with rheumatic immune diseases.Chinese and English databases were searched for randomized controlled trials(RCTs)on the treatment of rheumatic immune diseases with Tripterygium wilfordii glycosides tablets combined with Western medicine.The quality of the included studies was assessed using the Cochrane risk of bias assessment tool.Meta-analysis was performed using RevMan 5.4 software.RESULTS The meta-analysis included 11 RCTs involving 1026 patients with rheumatic immune diseases.The combined treatment significantly reduced the risk of disease recurrence(relative risk=1.07,95%confidence interval:1.01-1.15,P<0.05)and showed no significant heterogeneity(I2=0%,P=0.53),indicating that Tripterygium wilfordii glycosides tablets combined with Western medicine is an effective method to reduce the possibility of postoperative recurrence in patients with rheumatic immune diseases.However,due to the limited number and quality of the studies included,these results should be interpreted with caution.CONCLUSION Tripterygium wilfordii glycosides tablets combined with Western medicine is an effective and safe treatment option for patients with rheumatic immune diseases and can be considered a clinical choice.However,more high-quality research is needed to validate this conclusion and provide more solid evidence for clinical practice.
基金2023 Nantong Jianghai Talents Project2023 Nantong Social Livelihood Science and Technology Plan+4 种基金2021 Jurong Social Development Science&Technology Program(Grant No.ZA42109)2022 New Drugs and Platform Enhancement Project of the Yangtze Delta Drug Advanced Research InstituteChina Postdoctoral Science Foundation(Grant No.2020M681532)Jiangsu Planned Projects for Postdoctoral Research Funds(Grant No.2020Z209)Natural Science Research Projects of Universities in Jiangsu Province(Grant No.20KJD350001)。
文摘Oseltamivir phosphate(OP),renowned as one of the most effective drugs for influenza treatment,encounters several challenges,including poor stability,difficulty in swallowing,and a bitter taste,thereby limiting its compliance,particularly among children.Consequently,this study aimed to devise a novel sustained-release suspension of OP employing an ion exchange resin as a carrier to address these challenges.The OP-drug resin complex(OP-DRC)was synthesized utilizing ion exchange technology,while OP-coated microcapsules(OP-CM)were fabricated via the emulsion-evaporation method.The optimization of the formulation process for the OP sustained-release suspension was achieved through a combination of single-factor experimentation and orthogonal experimental design.Furthermore,the drug release kinetics and pharmacokinetic properties of the sustained-release suspension were thoroughly evaluated both in vitro and in vivo.Scanning electron microscopy(SEM),X-ray diffraction(XRD),and attenuated total reflectance Fourier-transform infrared spectroscopy(ATR-FTIR)analyses confirmed the formation of drug-resin complexes via ionic bonding.The in vitro cumulative release rates were found to be 16%(1 h),53%(6 h),and 84%(24 h),respectively.Notably,the self-made sustained-release suspension exhibited an extended half-life(21.518 h),delayed time to peak concentration(T_(max))(6 h),and reduced maximum plasma concentration(C_(max))(0.397μg/mL)in comparison to commercial granules(half-life=8.466 h;T_(max)=2 h;C_(max)=0.631μg/mL).Additionally,the area under the curve(AUC)indicated that the bioavailability of the self-made OP suspension surpassed that of the commercial OP granules by 101%.These findings underscored the successful development of an oral OP sustained-release suspension characterized by stability,tastelessness,ease of swallowing,convenient administration,and sustained-release properties,thereby potentially enhancing drug compliance among children.
文摘Objective:To evaluate the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease,in order to provide a more scientific basis for the application of the drug in Parkinson’s disease.Methods:This study is a single-arm,prospective,observational study.The trial collected patients with primary Parkinson’s disease who met the inclusion and exclusion criteria after being assessed by the investigator to evaluate the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease patients through UPDRSIII and UPDRSII scales,and evaluated the efficacy and safety of rasagiline tablets in the treatment of Parkinson’s disease patients.Results:A total of 3560 patients were included in this study.44.1%of patients had early Parkinson’s disease,52.4%had intermediate Parkinson’s disease,and 3.5%had advanced Parkinson’s disease.The UPDRSIII(exercise capacity)score was 26.76 at baseline,25.47 at 1 month,24.18 at 2 months,and 23.39 at 3 months after treatment,and scores significantly improved over time(P<0.001).The UPDRSII(ability to perform daily living)score was an average of 23.60 at baseline,22.49 at 1 month,21.53 at 2 months,and 21.09 at 3 months after treatment,with statistically significant differences in scores between months(P<0.001).A total of 18 adverse events/reactions occurred in this study,and adverse symptoms eventually disappeared or resolved,without termination due to adverse events/reactions or patient discharge.Conclusion:Rasagiline tablets have significant efficacy in improving daily exercise capacity and living ability in patients with Parkinson’s disease,and have a certain safety,which supports the effectiveness of rasagiline as a treatment for Parkinson’s disease and provides new evidence for its clinical application.
