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
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
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
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
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
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
In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepare...In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepared by oil-in-oil solvent evaporation method. Matrix tablets were prepared by wet and melt granulation techniques. Diclofenac sodium(DFS) and diltiazem hydrochloride(DLTZ) were used as model drugs. Mastic produced discrete and spherical microspheres with DLTZ and microcapsules with DFS. Particle size and drug loading of microparticles was in the range of 22–62 μm and 50–87%, respectively. Increase in mastic:drug ratio increased microparticle size, improved drug loading and decreased the drug release rate. Microparticles with gum: drug ratio of 2:1 could sustain DLTZ release up to 12 h and released 57% DFS in 12 h. Mastic produced tablets with acceptable pharmacotechnical properties. A 30% w/w of mastic in tablet could sustain DLTZ release for 5 h from wet granulation,and DFS release for 8 h and 11 h from wet and melt granulation, respectively. Results revealed that a natural gum mastic can be used successfully to formulate matrix tablets and microparticles for sustained drug release.展开更多
目的观察阿利沙坦酯联合硝苯地平缓释片对中重度原发性高血压伴心绞痛疗效和安全性。方法选取2021年1月至2022年1月佛山市中医院禅城高新区医院老年医学科收治的符合纳入标准的120例中重度原发性高血压伴心绞痛患者,根据随机数表法分为...目的观察阿利沙坦酯联合硝苯地平缓释片对中重度原发性高血压伴心绞痛疗效和安全性。方法选取2021年1月至2022年1月佛山市中医院禅城高新区医院老年医学科收治的符合纳入标准的120例中重度原发性高血压伴心绞痛患者,根据随机数表法分为研究组和对照组,每组各60例。对照组使用硝苯地平缓释片Ⅰ治疗,研究组在对照组基础上联合阿利沙坦酯片治疗,疗程为12周。治疗前后测量诊室血压并进行动态血压监测,评估降压效果,计算血压达标率。记录治疗期间两组心绞痛发作持续时间、发作频率、硝酸甘油用量,评估心绞痛改善情况。测量治疗前后患者生命体征,并行血尿常规、血糖、胆固醇、三酰甘油、尿素氮、肌酐、尿酸、血电解质、转氨酶、血清肌酐等实验室检查,记录治疗期间不良反应发生情况。结果治疗后,两组诊室收缩压(SBP)和舒张压(DBP)均较治疗前降低,且研究组低于对照组(P<0.05)。治疗后,两组24 h SBP、24 h DBP、白昼SBP(dSBP)、白昼DBP(dDBP)、夜间SBP(nSBP)和夜间DBP(nDBP)均降低,且研究组低于对照组(P<0.05)。研究组降压总有效率高于对照组(P<0.05)。两组与同组治疗2周后和治疗4周后比较,治疗8周后和治疗12周后两组血压达标率均增加(P<0.05)。治疗后,两组心绞痛发作持续时间、发作频率、硝酸甘油用量均较治疗前减少,且研究组低于对照组(P<0.05)。研究组心绞痛改善总有效率高于对照组(P<0.05)。两组不良反应总发生率比较,差异无统计学意义(P>0.05)。结论阿利沙坦酯联合硝苯地平缓释片治疗中重度原发性高血压伴心绞痛疗效显著,有效降压并维持血压稳定的同时,还可改善心绞痛症状,且安全性较高,具有临床应用价值。展开更多
Blue emitting perovskite ink obtained from cesium lead halide quantum dots bearing chlorine(CsPbClxBr3-x,0<x<3)suffers from the low photoluminescence quantum yield and poor stability.Cesium lead bromine(CsPbBr3)...Blue emitting perovskite ink obtained from cesium lead halide quantum dots bearing chlorine(CsPbClxBr3-x,0<x<3)suffers from the low photoluminescence quantum yield and poor stability.Cesium lead bromine(CsPbBr3)quantum dots free of chlori ne have more stable crystalstructure and fewer crystal defects.Precise control of crystal sizes and surface passivation comporients of CsPbBr3 quantum dots is crucial for the best use of quantum confinement effect and blueshift of emission wavelength to blue region.Here,by polymerizing acrylamide under UV-light irradiation to form polymer gel networks in dimethyl sulfoxide(DMSO)with CsPbBr3 precursors and passivating agents trapped,wesuccessfully prepared novel sustained release tablets with different shapes and sizes.Thanks to the limitation of the polymer networks onsolve nt releasi ng,the resulting CsPbBr3 qua ntum dots have the average size of 1.1±0.2 nm.On the basis of the excelle nt quantum confin eme nteffect and optimized surface passivation,the obtained PQD ink can emit high quality blue light for more than 6 weeks.This work elucidates anew and convenient technique to prepare blue emission perovskite quantum dots ink with high stability and photoluminescence qua ntumyield and provides a great potential technology for the preparation of perovskite optoelectronic devices.展开更多
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?.
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.
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In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepared by oil-in-oil solvent evaporation method. Matrix tablets were prepared by wet and melt granulation techniques. Diclofenac sodium(DFS) and diltiazem hydrochloride(DLTZ) were used as model drugs. Mastic produced discrete and spherical microspheres with DLTZ and microcapsules with DFS. Particle size and drug loading of microparticles was in the range of 22–62 μm and 50–87%, respectively. Increase in mastic:drug ratio increased microparticle size, improved drug loading and decreased the drug release rate. Microparticles with gum: drug ratio of 2:1 could sustain DLTZ release up to 12 h and released 57% DFS in 12 h. Mastic produced tablets with acceptable pharmacotechnical properties. A 30% w/w of mastic in tablet could sustain DLTZ release for 5 h from wet granulation,and DFS release for 8 h and 11 h from wet and melt granulation, respectively. Results revealed that a natural gum mastic can be used successfully to formulate matrix tablets and microparticles for sustained drug release.
文摘目的观察阿利沙坦酯联合硝苯地平缓释片对中重度原发性高血压伴心绞痛疗效和安全性。方法选取2021年1月至2022年1月佛山市中医院禅城高新区医院老年医学科收治的符合纳入标准的120例中重度原发性高血压伴心绞痛患者,根据随机数表法分为研究组和对照组,每组各60例。对照组使用硝苯地平缓释片Ⅰ治疗,研究组在对照组基础上联合阿利沙坦酯片治疗,疗程为12周。治疗前后测量诊室血压并进行动态血压监测,评估降压效果,计算血压达标率。记录治疗期间两组心绞痛发作持续时间、发作频率、硝酸甘油用量,评估心绞痛改善情况。测量治疗前后患者生命体征,并行血尿常规、血糖、胆固醇、三酰甘油、尿素氮、肌酐、尿酸、血电解质、转氨酶、血清肌酐等实验室检查,记录治疗期间不良反应发生情况。结果治疗后,两组诊室收缩压(SBP)和舒张压(DBP)均较治疗前降低,且研究组低于对照组(P<0.05)。治疗后,两组24 h SBP、24 h DBP、白昼SBP(dSBP)、白昼DBP(dDBP)、夜间SBP(nSBP)和夜间DBP(nDBP)均降低,且研究组低于对照组(P<0.05)。研究组降压总有效率高于对照组(P<0.05)。两组与同组治疗2周后和治疗4周后比较,治疗8周后和治疗12周后两组血压达标率均增加(P<0.05)。治疗后,两组心绞痛发作持续时间、发作频率、硝酸甘油用量均较治疗前减少,且研究组低于对照组(P<0.05)。研究组心绞痛改善总有效率高于对照组(P<0.05)。两组不良反应总发生率比较,差异无统计学意义(P>0.05)。结论阿利沙坦酯联合硝苯地平缓释片治疗中重度原发性高血压伴心绞痛疗效显著,有效降压并维持血压稳定的同时,还可改善心绞痛症状,且安全性较高,具有临床应用价值。
基金The work is supported by the National Natural Science Foundation of China(No.21761132007)the National Key R&D Program of China(No.2016YFE0114900).
文摘Blue emitting perovskite ink obtained from cesium lead halide quantum dots bearing chlorine(CsPbClxBr3-x,0<x<3)suffers from the low photoluminescence quantum yield and poor stability.Cesium lead bromine(CsPbBr3)quantum dots free of chlori ne have more stable crystalstructure and fewer crystal defects.Precise control of crystal sizes and surface passivation comporients of CsPbBr3 quantum dots is crucial for the best use of quantum confinement effect and blueshift of emission wavelength to blue region.Here,by polymerizing acrylamide under UV-light irradiation to form polymer gel networks in dimethyl sulfoxide(DMSO)with CsPbBr3 precursors and passivating agents trapped,wesuccessfully prepared novel sustained release tablets with different shapes and sizes.Thanks to the limitation of the polymer networks onsolve nt releasi ng,the resulting CsPbBr3 qua ntum dots have the average size of 1.1±0.2 nm.On the basis of the excelle nt quantum confin eme nteffect and optimized surface passivation,the obtained PQD ink can emit high quality blue light for more than 6 weeks.This work elucidates anew and convenient technique to prepare blue emission perovskite quantum dots ink with high stability and photoluminescence qua ntumyield and provides a great potential technology for the preparation of perovskite optoelectronic devices.