替米考星微囊的体外释放特性考察

Study on in vitro Release Behavior of Tilmicosin Microcapsules

关键词:  替米考星  微囊  缓释  体外释放

Key words:  Tilmicosin  Microcapsule  Sustained-release  In vitro release

摘要:

采用篮法考察替米考星微囊在磷酸盐缓冲液(pH=6.8)中的释放特性,并与市售制剂进行比较；进而对替米考星微囊的释药模型进行拟合。结果表明,1 h时,市售替米考星微囊中的药物几近释放完全,而自制替米考星微囊样品1、2和3的药物累积释放率分别为35％、50％和26％。4 h时,样品1和样品2的药物也已经基本释放完全(约90％)；而样品3的药物累积释放率才达到50％。模型拟合结果表明,自制替米考星微囊的体外释药曲线与Ritger-Peppas方程拟合度最好,样品1和样品3的拟合方程分别为lnQ = 0.543 6lnt-0.949 4(R2=0.9991)和lnQ = 0.539 1lnt-1.387 6(R2 =0.997 3)。由此可见,自制的替米考星微囊表现出一定的缓释作用,而且药物释放符合Ritger-Peppas方程。

Abstract:

The in vitro release behavior of tilmicosin microcapsules was investigated in phosphate buffer solution (pH=6.8) through basket method and compared with two kinds of commercial tilmicosin microcapsules. The release model of tilmicosin microcapsules was also fitted. It was found that the cumulative release percentages of sample 1, 2 and 3 of self-prepared tilmicosin microcapsules were respectively about 35％, 50％ and 26％ at 1 h, which was significantly lower than that of commercial tilmicosin microcapsules. After 4 h, the cumulative release percentage of sample 3 reached 82 %, while sample 1 and 2 were almost totally released (about 90%). The release profile of sample 1 and 3 of self-prepared tilmicosin microcapsules conformed to Ritger-Peppas equations which were lnQ = 0.543 6lnt-0.949 4 (R2=0.999 1) and lnQ = 0.539 1lnt-1.387 6 (R2=0.997 3), respectively. In conclusion, the self-prepared tilmicosin microcapsules exhibited sustained release effect, and the release profile conformed to Ritger-Peppas equation.