盐酸丁螺环酮缓释片的制备及其体外释放研究

Buspirone Hydrochloride Sustained-release Tablets:Preparation and Release in Vitro

目的:制备盐酸丁螺环酮缓释片,并考察其释药行为及其影响因素。方法:采用羟丙基甲基纤维素(HPMC)为亲水凝胶骨架材料,乙基纤维素(EC)为阻滞剂,湿法制粒制备盐酸丁螺环酮缓释片。考察不同释放递质,HPMC、EC的不同含量及不同黏度对该缓释片体外释放的影响。结果:制备出的缓释片24h的释药量超过90%,释药速率符合Higuchi方程。HPMC、EC含量的增加均会减慢缓释片的释放;随着HPMC黏度的增大,片剂的释药速率减慢,而EC的黏度及释放递质对释药速率均无明显影响。结论:以HPMC和EC为骨架材料,能制备出持续释药24h的盐酸丁螺环酮缓释片。

OBJECTIVE： To prepare buspiron hydrochloride sustained - release tablets and to study its release characterization in vitro and the factors affecting drug release. METHODS： Buspiron hydrochloride sustained - release tablets were prepared with hydroxypropyl methylcellulose （HPMC） as hydrophilic gel-matrix material and ethylcellulose （EC） as retarder by wet granulation. The impacts of releasing transmitters, contents of HPMC and EC, and viscosity on the drug release in vitro of the tablets were studied. RESULTS： For the prepared sustained release tablets, the 24h drug release amount was over 90%, and the drug release curve conformed to Higuchi equation. The more contents of HPMC and EC and the higher viscosity of HPMC in the tablets, the slower drug release velocity was obtained; but the viscosity of EC and the releasing transmitters had no significant impacts on the drug release velocity. CONCLUSION： With HPMC and EC as matrix materials, the 24h continuous drug release is available for buspirone hydrochloride sustainedtablets.