阿维菌素缓释注射液体外释放度的研究

Study of avermectin sustained-release injections in vitro

目的:设计两种兽用阿维菌素 ( AVM)缓释注射液的处方工艺 ,通过体外释放度试验筛选得到释放时间较长、释放较稳定的一种制剂。 方法:将两种 AVM缓释注射液分别放入透析袋中 ,置于释放介质中 ,同时用它们各自的空白辅料作为对照。以其累积释药量进行不同模型拟合 ,观察相关系数 ,选择最佳拟合方程并提取药动学参数 t50 及 td。根据每日释放 AVM的速率和平均释放量及其 t50 和 td,对它们进行评价。结果 :AVM-硬脂酸铝蓖麻油油胶注射液 ( AVM- COOGI)的最佳拟合方程为 Higuchi方程 ,由此计算得其 t50 =15 .1d,td=2 2 .0 d;AVM-硬脂酸铝豆油油胶注射液 ( AVM- SOOGI)的最佳拟合方程为一级释放 ,由此计算得其 t50 为 9.6 6 d,td为 13.9d。 AVM-COOGI的 t50 与 AVM- SOOGI的 t50 间差异有统计学意义。 结论 :体外试验结果表明 AVM-

Objective: To study two AVM sustained release injections which were made by ourself in vitro,so as to get a better formulation. Methods: Under the sink condition, these two formulations were set into each dialyser, then sinked them into the suitable liquid at 38℃ in a water bath to release, at the same time using their drug free oil gel as their control in the same condition. According to their daily dose rate of AVM and their average daily drug release amount, we can estimate which AVM oil gel injection is better. According to the accumulative drug release amount, we obtain the release profile of each AVM oil gel injections and to pretest their long acting effect. Results: According to each formulation accumulative drug release amount, using quasilinearization test of goodness of fit, we can obtain that the best pseudo equation for AVM aluminum stearate castor oil oil gel injection(AVM COOGI) was Higuchi equation,the best pseudo equation for AVM aluminum stearate soybean oil oil gel injection(AVM SOOGI) was first order release equation. The t 50 for AVM aluminum stearate castor oil oil gel injection (t 50 =15.1 d) was significantly longer than AVM aluminum stearate soybean oil oil gel injection (t 50 =9.66 d). Conclusion: With the statistics analysis ,the results shows that the AVM aluminum stearate castor oil oil gel injection is the optimum prescription.