美乐托宁缓释片在不同介质中的释放试验

Study on the release of melatonin sustained release tablets in different mediums

目的:制备美乐托宁缓释片,以国外上市制剂美乐托宁缓释片为参比制剂,考察自研制剂和参比制剂在不同pH释放介质中体外释放行为的相似性及体外释药机制。方法:采用释放度测定法转篮法的装置进行体外释放实验,用HPLC法测定释放度,采用f2相似因子对2种制剂释放曲线的相似度进行评价,并进行释放行为模型的拟合。结果:在不同pH的释放介质中,自制制剂释放度曲线与参比制剂比较,f2相似因子均大于50;美乐托宁缓释片在4种释放介质中体外释药拟合模型更接近一级方程、Higuchi方程和Peppas方程。结论:参比制剂与自制制剂在不同pH释放介质中的体外释放一致,释放机制为扩散释药。

OBJECTIVE To prepare melatonin sustained release tablets. Melatonin sustained release tablets were used as ref erence preparation, which have been licensed overseas. And the release behavior similarity was investigated between reference preparation tablets and sel^prepared preparation in release mediums with different pH, the in vitro drug release mechanism al so was investgated. METHODS The release tests were carried out with rotating basket, HPLC method was used to determine the release of melatonin sustained release tablets, the .f2 similarity factor was used to evaluate the sinfilarity of release curves. RESULTS In different release mediums, the release curves of melatonin sustained release tablets from self-prepared prepara tion compared with reference preparation, similar factor（f2 ） are all more than 50; In witro drug release of melatonin sustained release tablets was consistent with first class equation, Higuchi equation and Peppas equation in 4 kinds of medium. CONCLU- SION The release behavior of self-prepared preparation and reference preparation were similar in release mediums with differ- ent pH, the release mechanism was diffusion drug release.