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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Acutrim(r)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。
HPMC K100M and Carbopol 971P were selected as the matrix materials and the powder tablets were directly compressed to prepare the matrix tablets. The release degree and the concentration of PPA (HCl) were determined by reversed-phase high performance liquid chromatography According to the Higuchi equation (R> 0.98, P <0.01), orthogonal design method was used to obtain the optimal prescription by using PPA (Acutrim (HCl) in the American market as a control and similarity factor f2 as an index. The process was reproducible and qualified.Produced in 0.1 mol (L-1 HCl, H2O (pH 6.5), phosphate buffer (PBS) pH 5.0, 6.8 and 7.4 medium, and in 0.1 mol Release 2 h, transferred to PBS6.8 release 10 h, f2 value relative to the control of 63 to 74, indicating that the release profiles of the two agents in each medium similar to the release of the factors affecting the study results showed that: in The rate of release of matrix tablets in water was negatively correlated with the dosage of HPMC K100M and carbopol 971P in the range investigated in this experiment.The ratio of HPMC K100M to carbopol 971P (keeping the same total amount of polymer), stearic acid Magnesium content and hardness of matrix tablets had no significant effect on drug release rate.