顺铂植入剂植入给药的体内外相关性  

Correlation between in vivo absorption and in vitro release of cisplatin implants

作　　者：王世亮[1,2] 刘华顶[3] 叶红杨[2] 许媛媛[4] 丁满志[2] 储成顶[2,4] 宣凤琴[1,2] 付艳华[1,2] 钟静[1,2] 

机构地区：[1]安徽职业技术学院,合肥230051 [2]合肥工业大学控释药物研究室,合肥230009 [3]安徽阜阳肿瘤医院,阜阳236018 [4]安徽医科大学理化中心,合肥230032

出　　处：《中国新药杂志》2010年第20期1915-1920,共6页Chinese Journal of New Drugs

基　　金：安徽省十一五科技攻关重点项目(06013062A);安徽高校省级自然科学研究重点项目(KJ2007135AZC)

摘　　要：目的:探索顺铂植入剂的体内外相关性指标。方法:体内试验采用肿瘤局部植入给药,原子吸收光谱法测定血药浓度,建立药动学模型并计算体内吸收率;体外采用改良的大杯法测定体外释放度,取样时间点为预选的关联时间点;体内外相关按中华人民共和国药典规定的"点对点"方法进行。结果:体内药动学模型为一室缓释模型,体外释放为一级方程,体内外相关试验的对应时间点数n=10,统计自由度ν=9,体内外相关系数r=0.884 2,大于临界相关系数0.847 0(P=0.001)。结论:提示本试验的体内吸收和体外释放过程具有较好的相关性。Objective： To investigate the correlation between in vivo absorption and in vitro release of cisplatin implants.Methods： In the in vivo test,cisplatin implant was topically administered into the tumor,and the drug level in blood was determined by atomic absorption spectrophotometer.Then the pharmacokinetics model was built and in vivo absorption rate was computed.In the in vitro test,the releasing rate was assayed by shake flask method,and the sampling times were preselected time-points.The correlation between the in vivo and in vitro tests was analyzed by linear correlation according to Chinese Pharmacopoeia.Results： The in vivo pharmacokinetics fitted to one compartment controlled-release model.The in vitro release fitted one-order equation.The corresponding times in the in vivo and in vitro correlation tests were 10;the degree of freedom（ν） was 9;the coefficient correlation was 0.8842 that exceeded critical coefficient correlation（0.8470,P=0.001）.Conclusion： There is a preferable correlation between in vivo absorption and in vitro release.

关 键 词：顺铂 植入剂 体内吸收 体外释放 体内外相关 

分 类 号：R979.1[医药卫生—药品]