盐酸丁螺环酮胃漂浮缓释胶囊的制备及处方优化  

Preparation and Formulation Optimization of Buspirone Hydrochloride Gastric-Floating Sustained-Release Capsules

作　　者：金桂兰[1,2] 李雪怡 王柯玉 林宁 邢翔飞 龚大春[2] JIN Guilan;LI Xueyi;WANG Keyu;LIN Ning;XING Xiangfei;GONG Dachun(The People's Hospital of China Three Gorges University,Yichang First People's Hospital,Yichang,Hubei,China 443000;Institute of Pharmaceutic Preparation,China Three Gorges University,Yichang,Hubei,China 443000;College of Pharmacy,Hubei University of Chinese Medicine,Wuhan,Hubei,China 430065)

机构地区：[1]三峡大学人民医院·宜昌市第一人民医院,湖北宜昌443000 [2]三峡大学药物制剂研究所,湖北宜昌443000 [3]湖北中医药大学药学院,湖北武汉430065

出　　处：《中国药业》2019年第16期9-12,共4页China Pharmaceuticals

摘　　要：目的制备盐酸丁螺环酮胃漂浮胶囊,并采用星点设计-响应面(CCD-RSM)法优化处方。方法以羟丙甲基纤维素(HPMC)K15M、HPMCK100M、聚乙烯吡咯烷酮(PVP)K30和十六醇的用量为考察因素,以累积释放度(Q)与制剂漂浮性能为评价指标,采用CCD-RSM法优化处方,并进行验证。结果最优处方为HPMCK15M35mg,HPMCK100M100mg,PVPK3011mg,十六醇14mg。按优化的处方制得盐酸丁螺环酮胃漂浮缓释胶囊起漂时间<1min,续漂时间>8h,Q8h>75%;Q2h,Q4h,Q8h的实测值分别为(28.8±0.7)%,(54.8±0.5)%,(79.7±1.1)%,与预测值的偏差分别为1.0%,3.6%,2.6%。结论经CCD-RSM法优化的处方制得的盐酸丁螺环酮胃漂浮缓释胶囊,漂浮性能良好,且能持续缓慢释药。Objective To prepare Buspirone Hydrochloride Gastric-Floating Sustained-Release Capsules and optimize this formulation by the central composite design-response surface methodology( CCD-RSM). Methods Taking the amount of hydroxypropyl methyl cellulose( HPMC) K15 M,HPMC K100 M,polyvinylpyrrolidone( PVP) K30 and cetyl alcohol as the factors,and taking the in vitro cumulative release rate( Q) and the floating performance of the preparation as indexes,the formulation was optimized by CCD-RSM,and then it was validated. Results The optimized formulation was as follows: 35 mg HPMC K15 M,100 mg HPMC K100 M,11 mg PVP K30 and 14 mg cetyl alcohol. The indexes of Buspirone Hydrochloride Gastric-Floating Sustained-Release Capsules prepared according to the optimized formulation were as follows: the initial floating time was shorter than 1 min,the duration of floating was longer than 8 h,and the Q8h was over 75%. The measured values of Q2h,Q4h,Q8hfrom the prepared sustained-release capsules were( 28. 8 ± 0. 7) %,( 54. 8 ± 0. 5) % and( 79. 7 ± 1. 1) %,and the related errors of them to predictive value were 1. 0%,3. 6% and 2. 6%. Conclusion The Buspirone Hydrochloride Gastric-Floating Sustained Release Capsules prepared by optimized formulation with CCD-RSM has good sustained-release and floating performance.

关 键 词：盐酸丁螺环酮 胃漂浮缓释胶囊 星点设计-响应面法 累积释放度 漂浮性能 处方优化 

分 类 号：R917[医药卫生—药物分析学] TQ460.6[医药卫生—药学]