We previously determined 'Tableting properties' by using a multi-functional single-punch tablet press(GTP-1). We proposed plotting 'Compactability' on the x-axis against'Manufacturability' on t...We previously determined 'Tableting properties' by using a multi-functional single-punch tablet press(GTP-1). We proposed plotting 'Compactability' on the x-axis against'Manufacturability' on the y-axis to allow visual evaluation of 'Tableting properties'. Various types of tableting failure occur in commercial drug production and are influenced by the amount of lubricant used and the shape of the punch. We used the GTP-1 to measure'Tableting properties' with different amounts of lubricant and compared the results with those of tableting on a commercial rotary tableting machine. Tablets compressed with a small amount of lubricant showed bad 'Manufacturability', leading to sticking of powder on punches.We also tested various punch shapes. The GTP-1 correctly predicted the actual tableting results for all punch shapes. With punches that were more likely to cause tableting failure, our system predicted the effects of lubricant quantity in the tablet formulation and the occurrence of sticking in the rotary tableting machine.展开更多
We previously determined "Tableting properties" by using a multi-functional single-punch tablet press(GTP-1). We plotted "Compactability" on the x-axis against "Manufacturability"on the y...We previously determined "Tableting properties" by using a multi-functional single-punch tablet press(GTP-1). We plotted "Compactability" on the x-axis against "Manufacturability"on the y-axis to allow visual evaluation of "Tableting properties". Here, we examined whether this evaluation method can be used in the formulation design of tablets prepared by wet granulation. We used the GTP-1 to measure "Tableting properties" with different amounts of binder, disintegrant, and lubricant, and compared the results with those of tableting on a commercial rotary tableting machine. Tableting failures(capping and binding in particular) occurred when samples that had been evaluated as having poor "Compactability" or"Manufacturability" on the GTP-1 were compressed on the rotary tableting machine. Thus,our evaluation method predicted tableting failure at the commercial scale. The method will prove useful for scaling up production.展开更多
The ability to predict tableting properties of a powder mixture from individual components is of both fundamental and practical importance to the efficient formulation development of tablet products. A common tabletin...The ability to predict tableting properties of a powder mixture from individual components is of both fundamental and practical importance to the efficient formulation development of tablet products. A common tableting classification system(TCS) of binary powder mixtures facilitates the systematic development of new knowledge in this direction. Based on the dependence of tablet tensile strength on weight fraction in a binary mixture,three main types of tableting behavior are identified. Each type is further divided to arrive at a total of 15 sub-classes. The proposed classification system lays a framework for a better understanding of powder interactions during compaction. Potential applications and limitations of this classification system are discussed.展开更多
A combination of melt-granulated dispersion and surface adsorption techniques was used to enhance the dissolution and tableting properties of cefuroxime axetil(CA).Gelucire 50/13 was used as the melt-dispersion carrie...A combination of melt-granulated dispersion and surface adsorption techniques was used to enhance the dissolution and tableting properties of cefuroxime axetil(CA).Gelucire 50/13 was used as the melt-dispersion carrier and Sylysia 350 was used to adsorb the melt dispersion.Solubility studies showed an 8-fold increase in solubility at a ratio of 1:1.5 for CA:Gelucire 50/13.The minimum quantity of Sylysia 350 required to achieve the desired flowability and compressibility was 0.5 parts of Sylysia 350 per unit of Gelucire 50/13.Phase solubility studies showed negative ΔG_(tr)^(0) values for Gelucire 50/13 at various concentrations(2-10%,vv/v),indicating the spontaneous nature of solubilization.FT-IR and DSC spectra exhibited drug-excipient compatibility.Molecular modeling by a computational method employing energy minimization revealed entrapment of CA in Gelucire 50/13.The total potential energy of CA(70.562 keal/mol)was reduced to 33.578 keal/mol after solid dispersion with Gelucire 50/13.P-XRD studies indicated that the presence of Sylysia 350 is less likely to promote the reversion of the amorphous CA to a crystalline state.In vitro dissolution studies demonstrated an improved dissolution rate,and drug release at 15 min(Q_(15min))exhibited a 15-fold improvement.The rapidly dissolving CA tablets showed improved dissolution with improved tableting properties.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
Inspired by brick-and-mortar architectures and suture interfaces,we propose a design of bioinspired nacre-like materials with interlocking sutures to improve the toughness of brittle materials.Laser-engraved glass int...Inspired by brick-and-mortar architectures and suture interfaces,we propose a design of bioinspired nacre-like materials with interlocking sutures to improve the toughness of brittle materials.Laser-engraved glass interlockers are laminated with soft interlayers in a staggered arrangement,and the fundamental mechanical properties of the structure are investigated through experiments and numerical modeling.It is found that the tensile performance,such as the strength and toughness,is strongly affected by the interlocking angle and suture line spacing.The geometric interlocking originated from suture interfaces as well as tablet sliding arising from the staggered arrangement of interlockers cooperatively contribute to enhancing the strength and toughness of this bioinspired design.Additionally,the finite element modeling shows the interfacial failure and plastic deformation,revealing the interplay of the geometric interlocking mechanism and the sliding mechanism.This novel bioinspired design paves a new path for fabrication of structural materials combining high stiffness,high strength,and enhanced toughness.展开更多
This article presents a case study of a 20-year-old male patient diagnosed with dilated cardiomyopathy(DCM)(NYHA IV).This condition was diagnosed as"heart failure disease"(water overflowing due to yang defic...This article presents a case study of a 20-year-old male patient diagnosed with dilated cardiomyopathy(DCM)(NYHA IV).This condition was diagnosed as"heart failure disease"(water overflowing due to yang deficiency,intermingled phlegm and stasis)in traditional Chinese medicine(TCM).The treatment approach employed a combination of TCM and Western medicine.Western medicine involved the administration of sacubitril valsartan sodium tablets to inhibit ventricular remodeling,in conjunction with diuretics and cardiotonic agents.Initially,TCM utilized a static infusion of Shenfu injection,which was subsequently supplemented with Qiliqiangxin capsules to invigorate qi,warm yang,activate blood circulation,and promote diuresis.After a follow-up period of 3 years,the patient's ejection fraction(EF)improved from 23%to 51%,and the left ventricular end diastolic diameter(LVed)decreased from 68 to 52 mm,accompanied by a significant alleviation of symptoms.These findings indicate that the combined treatment of TCM and Western medicine can synergistically enhance cardiac function and impede the progression of the disease,thereby offering valuable insights for the optimal management of DCM.展开更多
OBJECTIVE:To examine Hedan tablet(HDT,荷丹片)'s potential mechanisms in hyperlipidemic rats induced by a high-fat diet(HFD),as well as its regulatory effects and primary active constituents.METHODS:By using ultra-...OBJECTIVE:To examine Hedan tablet(HDT,荷丹片)'s potential mechanisms in hyperlipidemic rats induced by a high-fat diet(HFD),as well as its regulatory effects and primary active constituents.METHODS:By using ultra-performance liquid chromatography(UPLC)-quadrupole-time-of-flight(QTOF)-tandem mass spectrometry(MS/MS),the components of HDT that can enter the circulatory system were found,aiming to investigate its active constituents with pharmacological effects.Based on network pharmacology approaches,the relevant HDT targets in the therapy of hyperlipidemia were anticipated.The possible mechanism of HDT for hyperlipidemia treatment was verified by in-vivo experiments,and the main active components of HDT for hyperlipidemia treatment were analyzed via in-vitro experiments.RESULTS:UPLC-QTOF-MS/MS identified 30 components of HDT entering the circulatory system,primarily consisting of flavonoids,diterpenoids and alkaloids.The results of a network pharmacology study revealed that 30 active components mostly target 74 genes associated with hyperlipidemia.The primary active ingredients may include quercetin,kaempferol,and epicatechin,and the main gene targets may be tumor necrosis factor(TNF),interleukin-6(IL-6),interleukin 1 beta(IL-1β),etc.The results of animal experiments demonstrated that HDT can significantly regulate the blood lipid level in rats with HFD,improve the degree of inflammatory infiltration in rat liver cells,lower TNF-α,Creactive protein(CRP),IL-6,matrix metalloproteinase 9(MMP9) and malondialdehyde(MDA) levels while raising total superoxide dismutase(T-SOD) level.Meanwhile,HDT can considerably lower the expression of sterol regulatory element-binding transcription factor 2(SREBF2),3-hydroxy-3-methylglutaryl-CoA reductase(HMGCR),and MMP9 while significantly increasing the expression of peroxisome proliferator-activated receptor alpha(PPAR-α) and PPAR-γ.In vitro study confirmed that quercetin and kaempferol could reduce the levels of IL-6,IL1B,MMP9 and HMGCR in the high-fat model of hepatoma G2 cells.CONCLUSIONS:The mechanism by which HDT treats hyperlipidemia involves modification of the lipid metabolism targets such as downregulating SREBF2,HMGCR and MMP9,and upregulating PPAR-α and PPAR-γ,as well as anti-inflammatory and antioxidant actions.This study provides a pharmacological and biological rationale for the use of HDT in clinical hyperlipidemia management.展开更多
Objective:To evaluate the clinical effect of combined therapy with Diosmin Tablets and Mayinglong Musk Hemorrhoids Ointment for patients with acute hemorrhoids.Methods:A total of 50 patients with acute hemorrhoids who...Objective:To evaluate the clinical effect of combined therapy with Diosmin Tablets and Mayinglong Musk Hemorrhoids Ointment for patients with acute hemorrhoids.Methods:A total of 50 patients with acute hemorrhoids who visited the hospital from January 2023 to January 2025 were selected as samples and randomly divided into two groups.Group A was treated with Diosmin Tablets combined with Mayinglong Musk Hemorrhoids Ointment,while Group B was treated with Mayinglong Musk Hemorrhoids Ointment only.The efficacy,wound recovery time,perianal pain score,hemorrhoid symptom score,and stress indicators were compared between the two groups.Results:The efficacy of Group A was higher than that of Group B(P<0.05).The postoperative perianal edema time and wound healing time in Group A were shorter than those in Group B,and the Visual Analog Scale(VAS)score was lower than that in Group B(P<0.05).The hemorrhoid symptom score in Group A was lower than that in Group B(P<0.05).The stress level in Group A was lower than that in Group B(P<0.05).Conclusion:The combination therapy of Diosmin Tablets and Mayinglong Musk Hemorrhoids Ointment for postoperative treatment of acute hemorrhoids can effectively relieve perianal pain,shorten the duration of hemorrhoids,and is highly feasible.展开更多
Objective:To analyze the efficacy of Bifidobacterium triple viable bacteria tablets on neonatal necrotizing enterocolitis(NEC)and its impact on serum factors of the patients.Methods:From January 2021 to May 2025,88 ne...Objective:To analyze the efficacy of Bifidobacterium triple viable bacteria tablets on neonatal necrotizing enterocolitis(NEC)and its impact on serum factors of the patients.Methods:From January 2021 to May 2025,88 neonates with NEC admitted to our hospital were selected as study subjects.During the study,these 88 patients were evenly divided into two groups,namely the observation group and the control group,with 44 patients in each group based on the random number table method.In terms of treatment,the control group was treated with meropenem,while the observation group received additional treatment with Bifidobacterium triple viable bacteria powder based on the treatment plan of the control group.The clinical efficacy and differences in serum inflammatory factor levels between the two groups were compared.Results:The efficacy of the observation group(90.91%)was better than that of the control group(72.73%)(P<0.05).After treatment,the levels of C-reactive protein(CRP)and procalcitonin(PCT)in both groups decreased compared to those before treatment,and the values of the above indicators in the observation group were lower than those in the control group(P<0.05).Conclusion:Based on conventional treatment for NEC neonates,the use of Bifidobacterium triple viable bacteria tablets has significant efficacy and can effectively reduce serum inflammatory factor levels.展开更多
OBJECTIVE:To investigate the impact of Shenhua tablet(肾华片,SHT)on renal macrophage polarization and renal injury in mice with diabetic kidney disease(DKD)and to explore the potential mechanism involving the hypoxia-...OBJECTIVE:To investigate the impact of Shenhua tablet(肾华片,SHT)on renal macrophage polarization and renal injury in mice with diabetic kidney disease(DKD)and to explore the potential mechanism involving the hypoxia-inducible factor-1α(HIF-1α)and pyruvate kinase M2(PKM2)signaling pathway,along with the glycolysis metabolism pathway.METHODS:The animals were divided into the following groups:Model,Control,dapagliflozin,SHT low-dose,SHT medium-dose,and SHT high-dose.We assessed 24-hour urine protein(24 h-UTP)levels,urinary albuminto-creatinine ratio,and regularly monitored fasting blood glucose during the treatment period.After treatment,we examined renal tissue structure,renal function(urea nitrogen,uric acid,creatinine,cystatin C,β2-microglobulin),and glycolysis in renal macrophages.Additionally,we observed macrophage polarization in renal tissue and measured inflammatory factors(tumor necrosis factor-α,interleukin-1β,interleukin-6,interleukin-10,monocyte chemoattractant protein-1)to assess the immunoinflammatory status of the renal tissue.Finally,we investigated the expression of the HIF-1α/PKM2 signaling pathway in macrophages to explore its role in the glycolysis process.RESULTS:SHT shows a beneficial effect in treating DKD by reducing 24 h-UTP,regulating blood glucose levels,improving renal tissue structure,protecting renal function,inhibiting macrophage glycolysis,reducing macrophage transformation to the M1 state,and suppressing the expression of the HIF-1α/PKM2 signaling pathway.CONCLUSION:SHT may exert renoprotective effects by inhibiting macrophage glycolysis via the HIF-1α/PKM2 signaling pathway.This inhibition decreases macrophage M1 polarization and reduces immunoinflammatory injury in the renal tissue of DKD mice.展开更多
[Objectives]To explore the clinical efficacy of Qinjin Tablet in treating unstable angina with phlegm-stasis syndrome and preliminarily explore its intervention mechanism.[Methods]Sixty unstable angina patients with p...[Objectives]To explore the clinical efficacy of Qinjin Tablet in treating unstable angina with phlegm-stasis syndrome and preliminarily explore its intervention mechanism.[Methods]Sixty unstable angina patients with phlegm-stasis syndrome were randomly divided into a treatment group and a control group(30 each).The control group received standardized Western medicine treatment,while the treatment group also took Qinjin Tablet.After a 4-week treatment,comparisons were made on improvement of angina symptoms,TCM syndrome scores,blood stasis scores,reduction/cessation of short-acting anti-angina drugs,Seattle Angina Questionnaire(SAQ)scores,blood lipid levels,and matrix metalloproteinase-9(MMP-9)concentrations between the two groups.[Results]No statistical differences existed in baseline data like age,gender,and disease duration between the two groups(P>0.05).The treatment group showed significantly better efficacy than the control group in improving angina symptoms,TCM syndrome scores,blood stasis scores,and reduction or discontinuation of short-acting anti-anginal drugs(P<0.05).The SAQ score increase was more significant in the treatment group(P<0.05).The control group significantly reduced low-density lipoprotein cholesterol(LDL-C)(P<0.05),while the treatment group markedly increased high-density lipoprotein cholesterol(HDL-C)(P<0.05).Post-treatment,the treatment group had a marked reduction in serum MMP-9(P<0.05),with no significant change in the control group.[Conclusions]Qinjin Tablet can significantly alleviate clinical symptoms and improve quality of life in UA patients by modulating the HDL-C/MMP-9 signaling pathway.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
Objective:To analyze the therapeutic efficacy of Shexiang Baoxin Pill combined with Rosuvastatin Calcium Tablets(ROS)in patients with angina pectoris due to coronary atherosclerotic heart disease(CHD-AP).Methods:Eight...Objective:To analyze the therapeutic efficacy of Shexiang Baoxin Pill combined with Rosuvastatin Calcium Tablets(ROS)in patients with angina pectoris due to coronary atherosclerotic heart disease(CHD-AP).Methods:Eighty CHD-AP patients admitted for treatment from January 2023 to December 2024 were selected and evenly divided using a random number table.The combined group(40 cases)received treatment with Shexiang Baoxin Pill combined with ROS,while the reference group(40 cases)received ROS monotherapy.The overall response rate,frequency and duration of AP attacks,blood lipid levels,and cardiac function indicators were compared between the two groups.Results:The combined group exhibited a higher overall response rate than the reference group.After treatment,the frequency and duration of AP attacks were lower in the combined group than in the reference group.Additionally,blood lipid levels and cardiac function indicators were superior in the combined group(p<0.05).Conclusion:The combination of Shexiang Baoxin Pill and ROS demonstrates favorable therapeutic effects in CHD-AP patients,effectively preventing AP attacks,regulating blood lipid levels,protecting cardiac function,and reducing disease risk.展开更多
Lappaconitine is a water-insoluble drug, which was used as model drug in this study. Currently, two osmotically controlled delivery systems that are widely used for water-insoluble drug are monolithic osmotic tablet ...Lappaconitine is a water-insoluble drug, which was used as model drug in this study. Currently, two osmotically controlled delivery systems that are widely used for water-insoluble drug are monolithic osmotic tablet （MOT） and push-pull osmotic pump （PPOP）. In the present study, lappaconitine solid dispersion monolithic osmotic tablet （lappaconitine-SD-MOT） and lappaconitine-PPOP were developed. The prepared lappaconitine-PPOP was able to delivery drug at the rate of approximate zero-order （r = 0.9931）, and the cumulative release was above 95.0%. The lappaconitine-SD-MOT showed a comparatively poor linearity when the data were plotted according to the zero-order equation （r = 0.9798）, and the cumulative release was 84.69%. Lappaconitine-PPOP exhibited better controlled drug release （higher regression value） compared with lappaconitine-SD-MOT. The similarity index （f2） between lappaconitine-PPOP and lappaconitine-SD-MOT was 49.1 （〈50）. A clear difference of drug release characteristics between the lappaconitine-SD-MOT and lappaconitine-PPOP was revealed. It indicated that the drug release performance of lappaconitine-PPOP could gain favorable zero-order kinetics and higher cumulative release compared with lappaconitine-SD-MOT. Therefore, these results suggested that PPOP was still a very effective device for the delivery of poorly water-soluble drug with zero-order pattern.展开更多
Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was perform...Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was performed on a Kromasil C_(18) column with TEA-adjusted0.02 mol·L^(-1) H_3PO_4 (pH 6.78)-acetonitrile-methanol (40 : 9 : 7) as mobile phase at aflow-rate of 1.0 mL·min^(-1), with detection at 254 ran. Considering interaction between acidic andalkaline compounds, three standard markers were added respectively and the volume of samplesolution was doubled in recovery experiments. Results Three regression equations revealed excellentlinear relationship between the peak areas and concentrations and the correlation coefficients allsurpassed 0.999 8. The average recovery was 96.1% (RSD = 2.1%) baicalin, 98.5% (RSD = 2.4%) forberberine, and 101.5% (RSD =1.3%) for rhein. Conclusion The method developed can be used to controlthe quality of Sanhuang tablets comprehensively.展开更多
The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersi...The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersion, suspending agents, osmotic agents and other conventional excipients were used as tablet core composition and cellulose acetate （CA） with plasticizer as release controlling membrane. Different formulation variables, the amounts of PEO （polyethylene oxide）, NaC1, plasticizer, and coating weight gain were optimized to gain the optimum formulation. The mechanism of drug release from monolithic osmotic tablet was also discussed. The optimal monolithic osmotic pump tablet could deliver quercetin at the rate of approximate zero-order up to 12 h, and the cumulative release was 90.74%. The developed monolithic osmotic system for quercetin loaded by solid dispersion was found to be a promising approach for controlled release of poorly-water soluble drug candidates.展开更多
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
The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma con...The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma concentration-time curves could be fitted to two-compartment open model, with 12.0 min of t1/2( , 143.4 min of t1/2( and 7.92 mg(min/L of AUC. The same eight dogs received 5 mg dose of the sublingual naloxone tablet after an interval of a week. The main pharmacokinetic parameters were: t1/2ka = 11.0 min, t1/2( = 15.4 min, t1/2( = 164.1 min, Tmax = 27.7 min, Cmax = 34.2 ng / ml, and AUC = 6.79 mg(min / L, respectively. The plasma concentration-time curves were fitted to the first order absorption two-compartment open model also. The mean absolute bioavailability of the sublingual naloxone tablet was 86.8 ( 10.9%. No statistically significant differences were found with t1/2(, t1/2(, ( and ( between the two routes of administration. These results indicated that the course of disposition for naloxone in dogs was similar for the two routes of administration, and the absolute bioavailability of the sublingual naloxone tablet was high. Thus satisfactory clinical effects could be expected.展开更多
The objectives of this present investigation were to develop and formulate nimesulide bilayer tablets by using different polymer combinations and fillers, to optimize the formulations for different drug release variab...The objectives of this present investigation were to develop and formulate nimesulide bilayer tablets by using different polymer combinations and fillers, to optimize the formulations for different drug release variables by orthogonal design and central composite design-surface methodology and to evaluate drug release pattern of the optimized product. The bilayer tablet containing a fast release layer（FRL） and a sustained release layer（SRL） provided an initial burst release of nimesulide, followed by the sustained release for a period of time. The optimal formulation obtained was as follows：（I） the formulation of FRL： nimesulide, 50 mg; lactose, 92 mg; starch, 22 mg; CCMC-Na, 14 mg; PVP K30, 1 mg; micronized silica gel, 1 mg; magnesium stearate, 0.9 mg; and iron oxide red, 0.1 mg; and（II） the formulation of SRL： nimesulide, 150 mg; HPMC K100LV, 26 mg; HPMC K4M, 33 mg; lactose, 54 mg; PVP K30, 1 mg; micronized silica gel, 1 mg; and magnesium stearate, 0.9 mg. According to the optimal formulation, the biphasic type of release was identified. The in vitro drug dissolution from the bilayer tablets was sustained for about 16 h after releasing 15% of drug in the first 10 min. The developed nimesulide bilayer tablets with improved efficacy can perform therapeutically better than the conventional tablets.展开更多
文摘We previously determined 'Tableting properties' by using a multi-functional single-punch tablet press(GTP-1). We proposed plotting 'Compactability' on the x-axis against'Manufacturability' on the y-axis to allow visual evaluation of 'Tableting properties'. Various types of tableting failure occur in commercial drug production and are influenced by the amount of lubricant used and the shape of the punch. We used the GTP-1 to measure'Tableting properties' with different amounts of lubricant and compared the results with those of tableting on a commercial rotary tableting machine. Tablets compressed with a small amount of lubricant showed bad 'Manufacturability', leading to sticking of powder on punches.We also tested various punch shapes. The GTP-1 correctly predicted the actual tableting results for all punch shapes. With punches that were more likely to cause tableting failure, our system predicted the effects of lubricant quantity in the tablet formulation and the occurrence of sticking in the rotary tableting machine.
文摘We previously determined "Tableting properties" by using a multi-functional single-punch tablet press(GTP-1). We plotted "Compactability" on the x-axis against "Manufacturability"on the y-axis to allow visual evaluation of "Tableting properties". Here, we examined whether this evaluation method can be used in the formulation design of tablets prepared by wet granulation. We used the GTP-1 to measure "Tableting properties" with different amounts of binder, disintegrant, and lubricant, and compared the results with those of tableting on a commercial rotary tableting machine. Tableting failures(capping and binding in particular) occurred when samples that had been evaluated as having poor "Compactability" or"Manufacturability" on the GTP-1 were compressed on the rotary tableting machine. Thus,our evaluation method predicted tableting failure at the commercial scale. The method will prove useful for scaling up production.
文摘The ability to predict tableting properties of a powder mixture from individual components is of both fundamental and practical importance to the efficient formulation development of tablet products. A common tableting classification system(TCS) of binary powder mixtures facilitates the systematic development of new knowledge in this direction. Based on the dependence of tablet tensile strength on weight fraction in a binary mixture,three main types of tableting behavior are identified. Each type is further divided to arrive at a total of 15 sub-classes. The proposed classification system lays a framework for a better understanding of powder interactions during compaction. Potential applications and limitations of this classification system are discussed.
文摘A combination of melt-granulated dispersion and surface adsorption techniques was used to enhance the dissolution and tableting properties of cefuroxime axetil(CA).Gelucire 50/13 was used as the melt-dispersion carrier and Sylysia 350 was used to adsorb the melt dispersion.Solubility studies showed an 8-fold increase in solubility at a ratio of 1:1.5 for CA:Gelucire 50/13.The minimum quantity of Sylysia 350 required to achieve the desired flowability and compressibility was 0.5 parts of Sylysia 350 per unit of Gelucire 50/13.Phase solubility studies showed negative ΔG_(tr)^(0) values for Gelucire 50/13 at various concentrations(2-10%,vv/v),indicating the spontaneous nature of solubilization.FT-IR and DSC spectra exhibited drug-excipient compatibility.Molecular modeling by a computational method employing energy minimization revealed entrapment of CA in Gelucire 50/13.The total potential energy of CA(70.562 keal/mol)was reduced to 33.578 keal/mol after solid dispersion with Gelucire 50/13.P-XRD studies indicated that the presence of Sylysia 350 is less likely to promote the reversion of the amorphous CA to a crystalline state.In vitro dissolution studies demonstrated an improved dissolution rate,and drug release at 15 min(Q_(15min))exhibited a 15-fold improvement.The rapidly dissolving CA tablets showed improved dissolution with improved tableting properties.
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Project supported by the National Natural Science Foundation of China(Nos.12202257,12072184,12002197)。
文摘Inspired by brick-and-mortar architectures and suture interfaces,we propose a design of bioinspired nacre-like materials with interlocking sutures to improve the toughness of brittle materials.Laser-engraved glass interlockers are laminated with soft interlayers in a staggered arrangement,and the fundamental mechanical properties of the structure are investigated through experiments and numerical modeling.It is found that the tensile performance,such as the strength and toughness,is strongly affected by the interlocking angle and suture line spacing.The geometric interlocking originated from suture interfaces as well as tablet sliding arising from the staggered arrangement of interlockers cooperatively contribute to enhancing the strength and toughness of this bioinspired design.Additionally,the finite element modeling shows the interfacial failure and plastic deformation,revealing the interplay of the geometric interlocking mechanism and the sliding mechanism.This novel bioinspired design paves a new path for fabrication of structural materials combining high stiffness,high strength,and enhanced toughness.
文摘This article presents a case study of a 20-year-old male patient diagnosed with dilated cardiomyopathy(DCM)(NYHA IV).This condition was diagnosed as"heart failure disease"(water overflowing due to yang deficiency,intermingled phlegm and stasis)in traditional Chinese medicine(TCM).The treatment approach employed a combination of TCM and Western medicine.Western medicine involved the administration of sacubitril valsartan sodium tablets to inhibit ventricular remodeling,in conjunction with diuretics and cardiotonic agents.Initially,TCM utilized a static infusion of Shenfu injection,which was subsequently supplemented with Qiliqiangxin capsules to invigorate qi,warm yang,activate blood circulation,and promote diuresis.After a follow-up period of 3 years,the patient's ejection fraction(EF)improved from 23%to 51%,and the left ventricular end diastolic diameter(LVed)decreased from 68 to 52 mm,accompanied by a significant alleviation of symptoms.These findings indicate that the combined treatment of TCM and Western medicine can synergistically enhance cardiac function and impede the progression of the disease,thereby offering valuable insights for the optimal management of DCM.
基金the National Natural Science Foundation of China:Effects of Hawthorn Leaves Flavonoids on Atherosclerosis Unstable Plaques based on the Mechanism of Liver-gut axis Liver X Receptor (LXR-a)-mediated Iron and Lipid Metabolism Disorders (No.82260794)the Natural Science Foundation of Jiangxi Province:based on Secreted Phospholipase A2 TypeⅡA (sPLA2-ⅡA) Regulating Lipid Mediated Foam Cell Formation to Explore the Effect and Molecular Mechanism of Hawthorn Leaf Flavonoids on Antiatherosclerosis (No.20212BAB206013)+1 种基金the Key R&D Program of Jiangxi Province:Research on the Quality Enhancement and Industrialization Technology Improvement of the Lipid-Lowering Traditional Chinese Medicine"Hedan Tablet"(No.20201BBG71005)Science and Technology Project of Jiangxi Provincial Department of Education:based on the"Phlegm-Stasis"Theory to Explore the Effects and Molecular Mechanisms of Hawthorn Leaves Flavonoids on Improving Iron and Lipid Metabolism Disorders in Atherosclerosis (No.GJJ2203502)。
文摘OBJECTIVE:To examine Hedan tablet(HDT,荷丹片)'s potential mechanisms in hyperlipidemic rats induced by a high-fat diet(HFD),as well as its regulatory effects and primary active constituents.METHODS:By using ultra-performance liquid chromatography(UPLC)-quadrupole-time-of-flight(QTOF)-tandem mass spectrometry(MS/MS),the components of HDT that can enter the circulatory system were found,aiming to investigate its active constituents with pharmacological effects.Based on network pharmacology approaches,the relevant HDT targets in the therapy of hyperlipidemia were anticipated.The possible mechanism of HDT for hyperlipidemia treatment was verified by in-vivo experiments,and the main active components of HDT for hyperlipidemia treatment were analyzed via in-vitro experiments.RESULTS:UPLC-QTOF-MS/MS identified 30 components of HDT entering the circulatory system,primarily consisting of flavonoids,diterpenoids and alkaloids.The results of a network pharmacology study revealed that 30 active components mostly target 74 genes associated with hyperlipidemia.The primary active ingredients may include quercetin,kaempferol,and epicatechin,and the main gene targets may be tumor necrosis factor(TNF),interleukin-6(IL-6),interleukin 1 beta(IL-1β),etc.The results of animal experiments demonstrated that HDT can significantly regulate the blood lipid level in rats with HFD,improve the degree of inflammatory infiltration in rat liver cells,lower TNF-α,Creactive protein(CRP),IL-6,matrix metalloproteinase 9(MMP9) and malondialdehyde(MDA) levels while raising total superoxide dismutase(T-SOD) level.Meanwhile,HDT can considerably lower the expression of sterol regulatory element-binding transcription factor 2(SREBF2),3-hydroxy-3-methylglutaryl-CoA reductase(HMGCR),and MMP9 while significantly increasing the expression of peroxisome proliferator-activated receptor alpha(PPAR-α) and PPAR-γ.In vitro study confirmed that quercetin and kaempferol could reduce the levels of IL-6,IL1B,MMP9 and HMGCR in the high-fat model of hepatoma G2 cells.CONCLUSIONS:The mechanism by which HDT treats hyperlipidemia involves modification of the lipid metabolism targets such as downregulating SREBF2,HMGCR and MMP9,and upregulating PPAR-α and PPAR-γ,as well as anti-inflammatory and antioxidant actions.This study provides a pharmacological and biological rationale for the use of HDT in clinical hyperlipidemia management.
文摘Objective:To evaluate the clinical effect of combined therapy with Diosmin Tablets and Mayinglong Musk Hemorrhoids Ointment for patients with acute hemorrhoids.Methods:A total of 50 patients with acute hemorrhoids who visited the hospital from January 2023 to January 2025 were selected as samples and randomly divided into two groups.Group A was treated with Diosmin Tablets combined with Mayinglong Musk Hemorrhoids Ointment,while Group B was treated with Mayinglong Musk Hemorrhoids Ointment only.The efficacy,wound recovery time,perianal pain score,hemorrhoid symptom score,and stress indicators were compared between the two groups.Results:The efficacy of Group A was higher than that of Group B(P<0.05).The postoperative perianal edema time and wound healing time in Group A were shorter than those in Group B,and the Visual Analog Scale(VAS)score was lower than that in Group B(P<0.05).The hemorrhoid symptom score in Group A was lower than that in Group B(P<0.05).The stress level in Group A was lower than that in Group B(P<0.05).Conclusion:The combination therapy of Diosmin Tablets and Mayinglong Musk Hemorrhoids Ointment for postoperative treatment of acute hemorrhoids can effectively relieve perianal pain,shorten the duration of hemorrhoids,and is highly feasible.
基金Project Name:Correlation Analysis between Intestinal Flora and Differential Proteins in Intestinal Tissue of Neonatal Necrotizing Enterocolitis(Project No.:FYX202336)。
文摘Objective:To analyze the efficacy of Bifidobacterium triple viable bacteria tablets on neonatal necrotizing enterocolitis(NEC)and its impact on serum factors of the patients.Methods:From January 2021 to May 2025,88 neonates with NEC admitted to our hospital were selected as study subjects.During the study,these 88 patients were evenly divided into two groups,namely the observation group and the control group,with 44 patients in each group based on the random number table method.In terms of treatment,the control group was treated with meropenem,while the observation group received additional treatment with Bifidobacterium triple viable bacteria powder based on the treatment plan of the control group.The clinical efficacy and differences in serum inflammatory factor levels between the two groups were compared.Results:The efficacy of the observation group(90.91%)was better than that of the control group(72.73%)(P<0.05).After treatment,the levels of C-reactive protein(CRP)and procalcitonin(PCT)in both groups decreased compared to those before treatment,and the values of the above indicators in the observation group were lower than those in the control group(P<0.05).Conclusion:Based on conventional treatment for NEC neonates,the use of Bifidobacterium triple viable bacteria tablets has significant efficacy and can effectively reduce serum inflammatory factor levels.
基金National Natural Science Foundation of China:Basic Research on the Mechanism of Organ Immune Damage and the Diagnosis and Treatment of Integrated Traditional Chinese and Western Medicine(No.32141005)。
文摘OBJECTIVE:To investigate the impact of Shenhua tablet(肾华片,SHT)on renal macrophage polarization and renal injury in mice with diabetic kidney disease(DKD)and to explore the potential mechanism involving the hypoxia-inducible factor-1α(HIF-1α)and pyruvate kinase M2(PKM2)signaling pathway,along with the glycolysis metabolism pathway.METHODS:The animals were divided into the following groups:Model,Control,dapagliflozin,SHT low-dose,SHT medium-dose,and SHT high-dose.We assessed 24-hour urine protein(24 h-UTP)levels,urinary albuminto-creatinine ratio,and regularly monitored fasting blood glucose during the treatment period.After treatment,we examined renal tissue structure,renal function(urea nitrogen,uric acid,creatinine,cystatin C,β2-microglobulin),and glycolysis in renal macrophages.Additionally,we observed macrophage polarization in renal tissue and measured inflammatory factors(tumor necrosis factor-α,interleukin-1β,interleukin-6,interleukin-10,monocyte chemoattractant protein-1)to assess the immunoinflammatory status of the renal tissue.Finally,we investigated the expression of the HIF-1α/PKM2 signaling pathway in macrophages to explore its role in the glycolysis process.RESULTS:SHT shows a beneficial effect in treating DKD by reducing 24 h-UTP,regulating blood glucose levels,improving renal tissue structure,protecting renal function,inhibiting macrophage glycolysis,reducing macrophage transformation to the M1 state,and suppressing the expression of the HIF-1α/PKM2 signaling pathway.CONCLUSION:SHT may exert renoprotective effects by inhibiting macrophage glycolysis via the HIF-1α/PKM2 signaling pathway.This inhibition decreases macrophage M1 polarization and reduces immunoinflammatory injury in the renal tissue of DKD mice.
基金Supported by Jiangsu Provincial Traditional Chinese Medicine Leading Talent Training Project[Su TCM Science-Education(2023)17]National Administration of Traditional Chinese Medicine Fifth Batch of National Excellent Clinical Talent Training Project[TCM Personnel-Education(2022)1].
文摘[Objectives]To explore the clinical efficacy of Qinjin Tablet in treating unstable angina with phlegm-stasis syndrome and preliminarily explore its intervention mechanism.[Methods]Sixty unstable angina patients with phlegm-stasis syndrome were randomly divided into a treatment group and a control group(30 each).The control group received standardized Western medicine treatment,while the treatment group also took Qinjin Tablet.After a 4-week treatment,comparisons were made on improvement of angina symptoms,TCM syndrome scores,blood stasis scores,reduction/cessation of short-acting anti-angina drugs,Seattle Angina Questionnaire(SAQ)scores,blood lipid levels,and matrix metalloproteinase-9(MMP-9)concentrations between the two groups.[Results]No statistical differences existed in baseline data like age,gender,and disease duration between the two groups(P>0.05).The treatment group showed significantly better efficacy than the control group in improving angina symptoms,TCM syndrome scores,blood stasis scores,and reduction or discontinuation of short-acting anti-anginal drugs(P<0.05).The SAQ score increase was more significant in the treatment group(P<0.05).The control group significantly reduced low-density lipoprotein cholesterol(LDL-C)(P<0.05),while the treatment group markedly increased high-density lipoprotein cholesterol(HDL-C)(P<0.05).Post-treatment,the treatment group had a marked reduction in serum MMP-9(P<0.05),with no significant change in the control group.[Conclusions]Qinjin Tablet can significantly alleviate clinical symptoms and improve quality of life in UA patients by modulating the HDL-C/MMP-9 signaling pathway.
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.
文摘Objective:To analyze the therapeutic efficacy of Shexiang Baoxin Pill combined with Rosuvastatin Calcium Tablets(ROS)in patients with angina pectoris due to coronary atherosclerotic heart disease(CHD-AP).Methods:Eighty CHD-AP patients admitted for treatment from January 2023 to December 2024 were selected and evenly divided using a random number table.The combined group(40 cases)received treatment with Shexiang Baoxin Pill combined with ROS,while the reference group(40 cases)received ROS monotherapy.The overall response rate,frequency and duration of AP attacks,blood lipid levels,and cardiac function indicators were compared between the two groups.Results:The combined group exhibited a higher overall response rate than the reference group.After treatment,the frequency and duration of AP attacks were lower in the combined group than in the reference group.Additionally,blood lipid levels and cardiac function indicators were superior in the combined group(p<0.05).Conclusion:The combination of Shexiang Baoxin Pill and ROS demonstrates favorable therapeutic effects in CHD-AP patients,effectively preventing AP attacks,regulating blood lipid levels,protecting cardiac function,and reducing disease risk.
基金Science and Technology Department of Henan Pro vince Fund Project(Grant No.144300510019)
文摘Lappaconitine is a water-insoluble drug, which was used as model drug in this study. Currently, two osmotically controlled delivery systems that are widely used for water-insoluble drug are monolithic osmotic tablet （MOT） and push-pull osmotic pump （PPOP）. In the present study, lappaconitine solid dispersion monolithic osmotic tablet （lappaconitine-SD-MOT） and lappaconitine-PPOP were developed. The prepared lappaconitine-PPOP was able to delivery drug at the rate of approximate zero-order （r = 0.9931）, and the cumulative release was above 95.0%. The lappaconitine-SD-MOT showed a comparatively poor linearity when the data were plotted according to the zero-order equation （r = 0.9798）, and the cumulative release was 84.69%. Lappaconitine-PPOP exhibited better controlled drug release （higher regression value） compared with lappaconitine-SD-MOT. The similarity index （f2） between lappaconitine-PPOP and lappaconitine-SD-MOT was 49.1 （〈50）. A clear difference of drug release characteristics between the lappaconitine-SD-MOT and lappaconitine-PPOP was revealed. It indicated that the drug release performance of lappaconitine-PPOP could gain favorable zero-order kinetics and higher cumulative release compared with lappaconitine-SD-MOT. Therefore, these results suggested that PPOP was still a very effective device for the delivery of poorly water-soluble drug with zero-order pattern.
基金Innovation Fund of Chinese Academy of Sciences(KGCX2 SW 213 05)
文摘Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was performed on a Kromasil C_(18) column with TEA-adjusted0.02 mol·L^(-1) H_3PO_4 (pH 6.78)-acetonitrile-methanol (40 : 9 : 7) as mobile phase at aflow-rate of 1.0 mL·min^(-1), with detection at 254 ran. Considering interaction between acidic andalkaline compounds, three standard markers were added respectively and the volume of samplesolution was doubled in recovery experiments. Results Three regression equations revealed excellentlinear relationship between the peak areas and concentrations and the correlation coefficients allsurpassed 0.999 8. The average recovery was 96.1% (RSD = 2.1%) baicalin, 98.5% (RSD = 2.4%) forberberine, and 101.5% (RSD =1.3%) for rhein. Conclusion The method developed can be used to controlthe quality of Sanhuang tablets comprehensively.
基金National Science & Technology Pillar Program during the 12~(th) Five-year Plan Period(Grant No.2012BAI29B08)
文摘The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersion, suspending agents, osmotic agents and other conventional excipients were used as tablet core composition and cellulose acetate （CA） with plasticizer as release controlling membrane. Different formulation variables, the amounts of PEO （polyethylene oxide）, NaC1, plasticizer, and coating weight gain were optimized to gain the optimum formulation. The mechanism of drug release from monolithic osmotic tablet was also discussed. The optimal monolithic osmotic pump tablet could deliver quercetin at the rate of approximate zero-order up to 12 h, and the cumulative release was 90.74%. The developed monolithic osmotic system for quercetin loaded by solid dispersion was found to be a promising approach for controlled release of poorly-water soluble drug candidates.
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.
文摘The pharmacokinetics and absolute bioavailability of the sublingual naloxone tablet were studied with HPLC-electrochemical detection. Eight male dogs received single 5 mg dose of naloxone intravenously, the plasma concentration-time curves could be fitted to two-compartment open model, with 12.0 min of t1/2( , 143.4 min of t1/2( and 7.92 mg(min/L of AUC. The same eight dogs received 5 mg dose of the sublingual naloxone tablet after an interval of a week. The main pharmacokinetic parameters were: t1/2ka = 11.0 min, t1/2( = 15.4 min, t1/2( = 164.1 min, Tmax = 27.7 min, Cmax = 34.2 ng / ml, and AUC = 6.79 mg(min / L, respectively. The plasma concentration-time curves were fitted to the first order absorption two-compartment open model also. The mean absolute bioavailability of the sublingual naloxone tablet was 86.8 ( 10.9%. No statistically significant differences were found with t1/2(, t1/2(, ( and ( between the two routes of administration. These results indicated that the course of disposition for naloxone in dogs was similar for the two routes of administration, and the absolute bioavailability of the sublingual naloxone tablet was high. Thus satisfactory clinical effects could be expected.
基金Important National Science & Technology Specific Projects of China(Grant No.2012ZX09301003-001-009)
文摘The objectives of this present investigation were to develop and formulate nimesulide bilayer tablets by using different polymer combinations and fillers, to optimize the formulations for different drug release variables by orthogonal design and central composite design-surface methodology and to evaluate drug release pattern of the optimized product. The bilayer tablet containing a fast release layer（FRL） and a sustained release layer（SRL） provided an initial burst release of nimesulide, followed by the sustained release for a period of time. The optimal formulation obtained was as follows：（I） the formulation of FRL： nimesulide, 50 mg; lactose, 92 mg; starch, 22 mg; CCMC-Na, 14 mg; PVP K30, 1 mg; micronized silica gel, 1 mg; magnesium stearate, 0.9 mg; and iron oxide red, 0.1 mg; and（II） the formulation of SRL： nimesulide, 150 mg; HPMC K100LV, 26 mg; HPMC K4M, 33 mg; lactose, 54 mg; PVP K30, 1 mg; micronized silica gel, 1 mg; and magnesium stearate, 0.9 mg. According to the optimal formulation, the biphasic type of release was identified. The in vitro drug dissolution from the bilayer tablets was sustained for about 16 h after releasing 15% of drug in the first 10 min. The developed nimesulide bilayer tablets with improved efficacy can perform therapeutically better than the conventional tablets.
