盐酸二甲双胍缓释片释放度及体内体外相关性研究

Study on Correlation Between in Vitro Release and in Vivo Absorption of Metformin Hydrochloride Sustained-Release Tablets

目的测定受试制剂盐酸二甲双胍缓释片的体外释放度,并进行体内体外相关性研究。方法采用转篮法测定释放度,紫外分光光度法测定含量,测定波长233 nm,计算受试制剂与原研产品释放曲线的相似因子f2,进行释放度的比较;单剂量口服受试制剂后测定血药浓度,将体外释放度数据与用Wagner-Nelson方法计算的药物体内吸收百分数进行线性回归后,进行体内体外相关性研究。结果受试制剂与原研产品体外释药曲线相似,受试制剂的体内体外相关性良好。结论受试制剂体外释放度合格,与原研产品有相似的体外释放特性,且可以通过体外释放曲线预测体内情况。

OBJECTIVE To study the correlation between the in vitro release and in vivo absorption of mefformin hydrochloride sustained-release tablets. METHODS The rotatory-basket method was used to determine the release rate, and UV spectrophotometer at 233 nm was used to assay the concentration. Similarity factor was calculated to compare the release rates of the test product and the original product. A single dose of metformin hydrochloride sustained-release tablets was given to 20 healthy volunteers, and the met- formin hydroch]oride concentrations in plasma at different time were determined. RESULTS The test product and the original product showed similar in vitro release characteristics, and the test product demonstrated good in vitro-in vivo correlation. CONCLUSION The in vitro release characteristic of the test product is qualified, and similar to that of the original product. The in vitro release curve of the test product can be used to evaluate its in vivo absorption.