普鲁斯的明缓释片体外释放与体内吸收的相关性研究  

Correlation Between in vitro Release and in vivo Absorption of Sustained-releasing Tablets of Neostigmine Bromide

作　　者：罗文[1] 谭群友[2] 熊华蓉[1] 赵春景[3] 张景勍[1] 

机构地区：[1]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,重庆400016 [2]第三军医大学大坪医院野战外科研究所胸外科,重庆400042 [3]重庆医科大学附属第二医院药剂科,重庆400010

出　　处：《四川大学学报（医学版）》2013年第1期80-83,共4页Journal of Sichuan University(Medical Sciences)

基　　金：教育部博士点基金资助项目(No.20095503120008);重庆市教育委员会资助项目(首批高等学校优秀人才资助;No.KJ090308)资助

摘　　要：目的评价普鲁斯的明缓释片体外释放和体内吸收之间的相关性。方法以水为溶出介质,测定普鲁斯的明缓释片的体外释放度,采用高效液相色谱法测定兔单剂量口服普鲁斯的明缓释片或普通片后的血药浓度,分别以Loo-Riegelman法计算体内吸收分数Fa和反卷积分法计算输入函数R。结果以体外累计释放度Y与Fa和R建立的回归方程分别为:Fa=0.9298Y+4.6074,r=0.9961;R=2.0163Y-11.242,r=0.9270。结论普鲁斯的明缓释片体外释放与体内吸收之间相关性良好。Objective To determine the correlation between in vitro release and in vivo absorption of sustained-releasing tablets of neostigmine bromide. Methods Water was used as dissolution medium to measured in vitro release of neostigmine bromide. After a single oral administration of 100 mg neostigmine bromide to rabbits, the plasma concentrations of neostigmine bromide in the rabbits were determined by HPLC. The compartment model and deconvolution method were employed to explain the in vitro-in vivo correlation. Results Using Y as cumulative in vitro release and Fa as percentage of absorption, the regression equation was established： Fa = 0. 9298Y＋4. 6074,r=0. 9961. The input function of R=2. 0163Y-11. 242,r=0. 9270. Conclusion The correlation between in vitro release and in vivo absorption of neostigmine bromide is good.

关 键 词：普鲁斯的明 缓释片 体内外相关性 

分 类 号：R943[医药卫生—药剂学]