盐酸丁螺环酮缓释片的制备及其体外释放研究

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。

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

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 sustained-tablets.