洛伐他汀缓释片的体外释放度和生物利用度

Sduty on the in vitro release and bioavailability of lovastatin sustained-release tablets

目的 :考察洛伐他汀缓释片的体内外性质 ,评价其缓释性能。方法 :测定制剂的体外释放度 ,考察不同因素的影响 ;测定制剂在比格犬体内的血药浓度 ,以洛伐他汀胶囊为参比制剂 ,计算相对生物利用度等药动学参数。结果 :制剂在 pH7.0的十二烷基硫酸钠溶液中可持续释药 2 4h ,释放规律符合零级动力学和Higuchi方程 ,不同的压片压力、转篮转速对药物释放有明显影响。缓释片的相对生物利用度为 (111.5± 16 .9) %。结论 :缓释片与参比制剂在吸收程度方面具有生物等效性 ,在吸收速度方面差异有显著性 。

OBJECTIVE To study the in vitro and in vivo characters of Lovastatin sustained-releasing tablets.METHODS The various factors affecting the in vitro release were investigated,a simple a nd sensitive HPLC method with UV detection was developed, and the Pharmacokineti cs in vivo also were studied.RESULTS It kept releasing for 24 h in sodium lauryl sulfate solution at pH= 7.0. The releasing rate conformed zero degree dynamic equation and Higuchi equation. The different compaction pressures and rotational speeds made significant differ ences to the releasing rate.CONCLUSION The sustained- release tablets and the normal capsules were bioequivalent.