Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of t...Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of the size of melatonin, type and amount of HPMC, drug loading, type and amount of additives, and compressing pressure were investigated. Plasma concentration of melatonin in dogs after intravenous injection of two doses and oral administration of sustained release tablets and unmodified release capsules was detected by HPLC using fluorescence detector. Results The drug release from sustained release tablets was influenced by the size of melatonin, type and amount of HPMC, drug loading, and type and amount of additives. Melatonin was found to fit two compartment model after intravenous injection, AUC was proportional to doses, and t(1/2β) of two doses has no significant difference. Relative bioavailability of melatonin sustained release tablet to normal capsule was 83.8%, and absolute bioavailability was 3.75% for sustained release tablet and 4.49% for capsule. Conclusion The melatonin sustained release tablet was well formulated. The absolute bioavilability for oral administration of either sustained release tablet or unmodified release capsule of melatonin was less than 5%. The bioavailability of melatonin sustained release tablet was lower than that of unmodified release capsule, but MRT of sustained release tablet was significantly longer than that of capsule.展开更多
To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given...To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.展开更多
Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 ...Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 patients with arrhythmia who were treated in our hospital from September 2019 to September 2020.According to different treatment methods,they were divided into observation group(Wenxin Granule+metoprolol succinate treatment)and control group(metoprolol succinate treatment),25 cases in each group.The curative effects of the two groups were compared.Results:After treatment,there was no significant difference in rnn50,RMSSD,sdnni and SDANN between the two groups(P>0.05).Compared with the control group,the SDNN in the observation group was higher than that in the control group(P<0.05);Before treatment,there was no significant difference in the above indexes between the two groups(P>0.05);The effective rates of the observation group and the control group were 92.00%and 68.00%respectively,and the curative effect of the observation group was higher than that of the control group(P<0.05);There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).Conclusion:In the treatment of patients with coronary heart disease and arrhythmia,Wenxin Granule Combined with metoprolol succinate sustained-release tablets has significant effect,which can effectively improve the dynamic electrocardiogram indexes of patients,improve the clinical efficacy,and has high safety.展开更多
The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performe...The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.展开更多
Nimodipine(NMDP)sustained release formulations were designed with hydroxypropylmethylcellulose(HPMC)as swellable polymer and with solid dispersion of the drug in polyvinyl pyrrolidone(K30).a water-soluble system.and c...Nimodipine(NMDP)sustained release formulations were designed with hydroxypropylmethylcellulose(HPMC)as swellable polymer and with solid dispersion of the drug in polyvinyl pyrrolidone(K30).a water-soluble system.and compressed into tablets by direct compression.Drug release kinetics from tablets withdifferent compositions was investigated in vitro.Results showed that dissolution process of NMDP from poroushydrophilic matrix conformed to zero-order release kinetics.The addition of microcrystalline cellulose to the porousswellable release system increased the NMDP release rate constant.The presence of hydroxyethylcellulose(HEC)inthe system,which had a lower viscosity,increased the drug release rate constant.When tablets were prepared withHPMC 40 mesh granulation,the release rate of the drug was sustained.These show that the dosage form may beformulated as a drug-polymer system with constant release at a desired rate.The release properties of the sustainedrelease tablets made by pure drug instead of drug solid dispersion were also investigated.In the present study,theoptimal formulations that constantly released the drug during 12 h were selected for in vivo analysis.展开更多
Objective: to explore the treatment and nursing of moxibustion in alleviating knee osteoarthritis (KOA) pain. Methods: a total of 92 patients with Arthralgia syndrome were selected from January 2019 to February 2021 a...Objective: to explore the treatment and nursing of moxibustion in alleviating knee osteoarthritis (KOA) pain. Methods: a total of 92 patients with Arthralgia syndrome were selected from January 2019 to February 2021 and randomly divided into two groups. The control group was treated with diclofenac sodium sustained release tablets, and the study group was treated with moxibustion. The therapeutic effects and TCM syndrome scores of the two groups were compared. Results: the total effective rate of study group was higher than that of control group (P < 0.05). After treatment, the score level of the study group was significantly lower than that of the control group (P < 0.05). Conclusion: the combined use of Moxa box moxibustion on the basis of diclofenac sodium sustained release tablets for KOA patients can significantly improve the curative effect, relieve the clinical symptoms of KOA patients and reduce the symptom score level.展开更多
Adopting prospective, multi-center, random, single-blind and equal rank-control methods,226 patients with rlieumatoid arthritis (RA) were divided into two groups. The 114 patients ot the test groupwere treated with or...Adopting prospective, multi-center, random, single-blind and equal rank-control methods,226 patients with rlieumatoid arthritis (RA) were divided into two groups. The 114 patients ot the test groupwere treated with oral sustained release tablets of Tripterygium Wiltordii (TW-SR) , 2 tablets twice a day for4 weeks, 112 patients of the control group received tablets of Tripterygium Wiltordii(TW) orally 2 tablets 3times per day for 4 weeks. Testing results showed thetotal effective rates of the two groups were 92 . 11%and 90. 65 % , respectively (P >0. 05) . The adverse reaction rate of TW-SR was 20 . 18% , which was low-er than that of TW group of 70. 54% (P < 0. 01 ) . Results of pre-clinical pharmacologic experimental studydemonstrated that TW-SR has obvious anti-inflammatory , analgesic and immunosuppressive actions the sameas TW, while the toxicity of TW-SR was less than that of TW significantly.展开更多
文摘Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of the size of melatonin, type and amount of HPMC, drug loading, type and amount of additives, and compressing pressure were investigated. Plasma concentration of melatonin in dogs after intravenous injection of two doses and oral administration of sustained release tablets and unmodified release capsules was detected by HPLC using fluorescence detector. Results The drug release from sustained release tablets was influenced by the size of melatonin, type and amount of HPMC, drug loading, and type and amount of additives. Melatonin was found to fit two compartment model after intravenous injection, AUC was proportional to doses, and t(1/2β) of two doses has no significant difference. Relative bioavailability of melatonin sustained release tablet to normal capsule was 83.8%, and absolute bioavailability was 3.75% for sustained release tablet and 4.49% for capsule. Conclusion The melatonin sustained release tablet was well formulated. The absolute bioavilability for oral administration of either sustained release tablet or unmodified release capsule of melatonin was less than 5%. The bioavailability of melatonin sustained release tablet was lower than that of unmodified release capsule, but MRT of sustained release tablet was significantly longer than that of capsule.
文摘To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.
文摘Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 patients with arrhythmia who were treated in our hospital from September 2019 to September 2020.According to different treatment methods,they were divided into observation group(Wenxin Granule+metoprolol succinate treatment)and control group(metoprolol succinate treatment),25 cases in each group.The curative effects of the two groups were compared.Results:After treatment,there was no significant difference in rnn50,RMSSD,sdnni and SDANN between the two groups(P>0.05).Compared with the control group,the SDNN in the observation group was higher than that in the control group(P<0.05);Before treatment,there was no significant difference in the above indexes between the two groups(P>0.05);The effective rates of the observation group and the control group were 92.00%and 68.00%respectively,and the curative effect of the observation group was higher than that of the control group(P<0.05);There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).Conclusion:In the treatment of patients with coronary heart disease and arrhythmia,Wenxin Granule Combined with metoprolol succinate sustained-release tablets has significant effect,which can effectively improve the dynamic electrocardiogram indexes of patients,improve the clinical efficacy,and has high safety.
文摘The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.
文摘Nimodipine(NMDP)sustained release formulations were designed with hydroxypropylmethylcellulose(HPMC)as swellable polymer and with solid dispersion of the drug in polyvinyl pyrrolidone(K30).a water-soluble system.and compressed into tablets by direct compression.Drug release kinetics from tablets withdifferent compositions was investigated in vitro.Results showed that dissolution process of NMDP from poroushydrophilic matrix conformed to zero-order release kinetics.The addition of microcrystalline cellulose to the porousswellable release system increased the NMDP release rate constant.The presence of hydroxyethylcellulose(HEC)inthe system,which had a lower viscosity,increased the drug release rate constant.When tablets were prepared withHPMC 40 mesh granulation,the release rate of the drug was sustained.These show that the dosage form may beformulated as a drug-polymer system with constant release at a desired rate.The release properties of the sustainedrelease tablets made by pure drug instead of drug solid dispersion were also investigated.In the present study,theoptimal formulations that constantly released the drug during 12 h were selected for in vivo analysis.
文摘Objective: to explore the treatment and nursing of moxibustion in alleviating knee osteoarthritis (KOA) pain. Methods: a total of 92 patients with Arthralgia syndrome were selected from January 2019 to February 2021 and randomly divided into two groups. The control group was treated with diclofenac sodium sustained release tablets, and the study group was treated with moxibustion. The therapeutic effects and TCM syndrome scores of the two groups were compared. Results: the total effective rate of study group was higher than that of control group (P < 0.05). After treatment, the score level of the study group was significantly lower than that of the control group (P < 0.05). Conclusion: the combined use of Moxa box moxibustion on the basis of diclofenac sodium sustained release tablets for KOA patients can significantly improve the curative effect, relieve the clinical symptoms of KOA patients and reduce the symptom score level.
文摘Adopting prospective, multi-center, random, single-blind and equal rank-control methods,226 patients with rlieumatoid arthritis (RA) were divided into two groups. The 114 patients ot the test groupwere treated with oral sustained release tablets of Tripterygium Wiltordii (TW-SR) , 2 tablets twice a day for4 weeks, 112 patients of the control group received tablets of Tripterygium Wiltordii(TW) orally 2 tablets 3times per day for 4 weeks. Testing results showed thetotal effective rates of the two groups were 92 . 11%and 90. 65 % , respectively (P >0. 05) . The adverse reaction rate of TW-SR was 20 . 18% , which was low-er than that of TW group of 70. 54% (P < 0. 01 ) . Results of pre-clinical pharmacologic experimental studydemonstrated that TW-SR has obvious anti-inflammatory , analgesic and immunosuppressive actions the sameas TW, while the toxicity of TW-SR was less than that of TW significantly.
