自研琥珀酸去甲文拉法辛缓释片与参比制剂体外溶出度一致性评价

目的：评价2种规格的自研琥珀酸去甲文拉法辛缓释片与参比制剂Pristiq^®体外溶出行为的一致性。方法：采用高效液相色谱法，色谱柱为Kromasil 100-5C₈（250 mm×4.6 mm，5 μm），流动相为0.1 mol·L^-1磷酸二氢铵溶液（pH 4.4）-乙腈（80：20），检测波长为226 nm，柱温为30℃，根据仿制药一致性评价要求，并参考Pristiq^®在FDA溶出数据库中的条件（0.9%氯化钠溶液，篮法和转速100 r·min^-1）分别考察自研制剂与参比制剂在5种不同介质（水、0.9%氯化钠溶液、pH 1.0盐酸溶液、pH 4.5磷酸盐缓冲液及pH 6.8磷酸盐缓冲液）中的体外释放行为及其相似性，并采用乙醇倾泻和转速强力变化进一步考察两者缓释片的相似性。结果：自研制剂与参比制剂在5种不同介质中溶出曲线均相似；在强力变化的不同转速下溶出曲线相似；在乙醇倾泻实验中溶出曲线相似（f₂因子均>50%）。结论：2种规格的自研制剂与参比参比制剂体外溶出行为具有一致性。

Objective: To evaluate the consistency of the in vitro release behavior between self-prepared desvenlafaxine succinate extended-release tablets and original preparation.Methods: The dissolution was analyzed by the HPLC method.Kromasil 100-5C₈(250 mm×4.6 mm,5 μm)column was used with the mobile phase of a mixture of acetonitrile and 0.1 mol·L^-1 potassium dihydrogen phosphate solution(pH4.4).The flow rate was 1.0 mL·min^-1;the detection wavelength was 226 nm and the column temperature was 30℃.According to the requirement of drug consistency evaluation and the dissolution test conditions of the reference preparation(Pristiq)from FDA,the release behaviors of self-prepared desvenlafaxine succinate extended-release tablets and reference preparation in water,0.9% sodium chloride solution,pH 1.0 solution,pH 4.5 phosphate buffer and pH 6.8 phosphate buffer was investigated,respectively;the behavior under different speeds of revolution and the behavior under alcohol-induced dose dumping were analyzed.Results: The release curves of self-prepared desvenlafaxine succinate extended-release tablets were similar to those of the reference preparation under not only 5 different dissolution mediums but also different rotation speeds;furthermore,self-prepared preparation under alcohol-induced dose dumping showed the same release behavior to the original preparation(f₂ factor>50%).Conclusion: The self-prepared preparation of two strength and the reference preparation showed consistency in vitro release behavior.