阿昔莫司缓释片的体外释放度与犬体内吸收相关性  

Study of acipimox sustained-release tablets on correlation of in vitro release and in vivo absorption in dogs

作　　者：杨星钢[1] 张国华[2] 李伟[1] 潘卫三[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]沈阳药科大学成人教育学院,辽宁沈阳110016

出　　处：《中国新药与临床杂志》2005年第7期508-511,共4页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的:研究阿昔莫司缓释片的体外释放度与其在家犬体内吸收的相关性。方法:以水为溶出介质,测定阿昔莫司缓释片的体外释放度。采用高效液相色谱法测定家犬单剂量口服阿昔莫司胶囊和缓释片后的血药浓度,用非隔室模型对阿昔莫司的体内过程进行拟合,以反卷积分法求算积分方程中的输入函数。以输入函数与同时间点体外累积释放度回归求得相关系数并与相关系数临界值进行比较。结果:以累积释放度Y与输入函数R建立的回归方程为:Y=18.118R+35.717(r=0.9309),相关系数临界值r4,0.05=0.811,r>r4,0.05,表明回归方程显著。结论:自制阿昔莫司缓释片体内外相关性良好。AIM:To study the in vitro-in vivo correlation of acipimox sustained- release tablet. METHODS: The release rate of acipimox from sustained-release ta blets was studied by using distilled water as dissolution medium to determine the plasma conce ntration through HPLC after oral administration of acipimox ca psules and sustained-release tablets to dogs with a single dose. The in vivo co urse of the drug characterized with using non-compartment and the input functi ons outcoming through deconvolution method. The correlation coefficients o f the calibration graph by plotting the release rate to the input functions were calculated and then compared to the critical correlation coefficients. RESULTS: The regressive equation obtained by plotting the release rate(Y) to the inpu t function(R) was: Y=18.118 R+35.717 (r=(0.930 9),) critical cor relat ion coefficie nt r_(4,0.05)=(0.811,) r>r_(4,0.05), indicated a significant lever of regression. CONCLUSION: The in vitro-in vivo correlation of self-made acipimox sustained-relea se tablet shows fine choracter.

关 键 词：阿昔莫司 片剂 迟效制剂 体内外相关性 反卷积分法 

分 类 号：R943.4[医药卫生—药剂学]