溴新斯的明缓释片的研制及体内外相关性评价.docVIP

溴吡斯的明12h缓释片的体内外释放行为相关性研究 熊华蓉1，谭群友2，赵德璋1，王睿2，张景勍1 （400016重庆重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室1； 400042重庆第三军医大学大坪医院野战外科研究所2）Loo-Riegelman法研究其体内外相关性。 方法 按《中国药典》2010版二部附录XD释放度测定第二法，以磷酸缓冲液为释放介质，采用紫外分光光度法测定溴吡斯的明的累积释放百分率。采用HPLC-紫外色谱法测定不同时间点的体内血药浓度。 结果 Loo-Riegelman法计算溴吡斯的明缓释片体内外的相关性，其体内累积吸收百分率与体外累积释放百分数X建立的线性回归方程为: fa = 0.4851 fr +3.8377 ,r = 0.9865, 大于临界值r6 ,0. 01(P＜0.01)。结论 溴吡斯的明缓释片释放行为的体内外相关性显著，通过体外释放行为可预测其体内释放动力学。 [关键词] 溴吡斯的明；；valuation of the in vivo-in vitro relationship of pyridostigmine bromide sustained release tablets Xiong Hua-rong1, Tan Qun-you2, Zhao De-zhang1, Wang Rui, Zhang Jing-qing1(1 Medicine Engineering Research Center, Key Laboratory of Biochemical＆Molecular Pharmacology, Chongqing Medical UniversityChongqing 400016；2 Department of Thoracic Surgery, Institute of Surgery Research，Daping Hospital , Third Military Medical University, Chongqing, 400042, China) [Abstract] Objective To determine the in-vitro release of Pyridostigmine Bromide sustained-release tablets and its pharmaceutical characteristics and to evaluate the in vitro-in vivo correlation using Loo-Riegelman method. Methods Using the phosphate buffer as dissolution medium to determine the accumulated release in vitro and the drug concentration in serum by HPLC. Results Loo-Riegelman method was adopt to evaluate the in vitro-in vivo correlation. The linear regressive equation was established between the absorption percentage in vivo and accumulate release percentage in vitro of sodium valproate sustained-release tablets as fa = 0.485 1 fr +3.8377, r = 0.986 5, which is bigger than the critical value r6 ,0. 01(P＜0.01) . Conclusion The results suggest that there is a significant correlation between the absorption percentage in vivo and accumulate release in vitro of the Pyridostigmine Bromide sustained-release tablets. [Key words] pyridostigmine bromide；pharmacokinetics；in vitro-in vivo correslation yridostigmine bromide），溴化1-甲基-3-羟基吡啶翁二甲氨基甲酸酯，为拟胆碱药、抗胆碱酯酶药1.2 方法 1.2.1 溴吡斯的明的含量测定 精密称取适量的对照品用蒸馏水