【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。更多还原

【Abstract】 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.更多还原