盐酸苯丙醇胺的HPMC K100M卡波普971P缓释骨架片的研制

盐酸苯丙醇胺的HPMC K100M卡波普971P缓释骨架片的研制

吕丹, 裴元英^*

上海医科大学药剂教研室, 上海 200032

收稿日期:2000-07-18 修回日期:2000-10-19 出版日期:2000-12-15 发布日期:2000-12-15
通讯作者: 裴元英*

Study of Sustained Release Phenylpropanolamine Hydrochloride Hydrophilic Matrix Tablets Containing Hydroxypropylmethylcellulose K100M and Carbopol 971P

Lu Dan, Pei Yuanying^*

Department of Pharmaceutics, School of Pharmacy, Shanghai Medical University, Shanghai, 200032

Received:2000-07-18 Revised:2000-10-19 Online:2000-12-15 Published:2000-12-15
Contact: Pei Yuanying*

摘要/Abstract

摘要： 选用HPMC K100M和卡波普971P为骨架材料,粉末直接压片法制备骨架片,考察释放度,反相高效液相色谱法检测盐酸苯丙醇胺(PPA-HCl)的浓度。释药曲线均符合Higuchi方程(R>0.98,P<0.01)。运用正交设计法, 以美国市场的PPA-HCl缓释片AcutrimR为对照, 相似因子f2值为指标, 筛选获得了最优处方。其工艺重现性合格。研制片在0.1 mol·L^-1 HCl, H2O (pH 6.5), 磷酸盐缓冲液(PBS) pH 5.0, 6.8和7.4的介质中, 以及在0.1 mol·L^-1 HCl中释放2 h, 转移至PBS6.8中释放10 h, 相对于对照品的f2值为63～74, 表明在各介质中两制剂的释药曲线相似。释药影响因素的考察结果表明: 在本实验考察的范围内, 骨架片在水中的释药速率与HPMC K100M和卡波普971P的用量呈负相关。HPMC K100M和卡波普971P的比例(保持聚合物总用量相同), 硬脂酸镁用量和骨架片硬度对释药速率无显著性影响。

关键词: 羟丙基甲基纤维素HPMC, K100M, 卡波普, 971P, 盐酸苯丙醇胺, 亲水凝胶缓释骨架片, 相似因子法

Abstract: In this study sustained release Phenylpropanolamine Hydrochloride (PPA(HCl) hydrophilic matrix tablets containing HPMC K100M and Carbopol 971P were prepared by direct compression method, and the release tests were performed. In all cases the plot of cumulative drug release percentage against t1/2 produced a straight line (r>0.98, P<0.01). The composition of polymers was selected employing orthogonal design. The chosen formulation showed consistent performance. The release profiles of the test and reference preparation were similar in 0.1 mol·L^-1 HCl, distilled water, phosphate buffer pH 5.0, 6.8, 7.4 and in 0.1 mol·L^-1 HCl for 2 h followed by release in phosphate buffer pH 6.8 for 10 h, for in these cases, the values of "similarity factor, f2" varied within the range of 63~74. The rate of PPA(HCl released in 0.1 mol·L^-1 HCl was significantly higher than in other four media (P<0.05). It was found that in the ranges examined, the rate of PPA(HCl released in distilled water decreased with the content of HPMC K100M or Carbopol 971P increased (P<0.05), but variations of the polymers ratio (using the same total content of polymers), the content of magnesium stearate or hardness of matrices appeared to insignificantly affect release rates (P>0.05).

Key words: Hydroxypropylmethylcellulose HPMC, K100M, Hydroxypropylmethylcellulose HPMC, K100M, Carbopol 971P, Carbopol 971P, Phenylpropanolamine Hydrochloride, Phenylpropanolamine Hydrochloride, Hydrophilic sustained release matrix tablets, Hydrophilic sustained release matrix tablets, Similarity factor, Similarity factor

Supporting: ^*To whom correspondence should be addressed. Tel: 021-64041900-2186. E-mail: yypei@shmu.edu.cn

吕丹, 裴元英^*. 盐酸苯丙醇胺的HPMC K100M卡波普971P缓释骨架片的研制[J]. .

Lu Dan, Pei Yuanying^*. Study of Sustained Release Phenylpropanolamine Hydrochloride Hydrophilic Matrix Tablets Containing Hydroxypropylmethylcellulose K100M and Carbopol 971P[J]. .