结肠定位盐酸小檗碱羧甲基魔芋胶小丸体外释药的影响因素

Influence factors on in vitro release of berberine hydrochloride from carboxymethyl konjac glucomannan pellets

目的:研究影响盐酸小檗碱羧甲基魔芋胶小丸体外释药的因素,评价其释药特性。方法:采用离子胶凝法制备羧甲基魔芋胶小丸,测定小丸在不同释放介质(β-甘露聚糖酶浓度和离子强度)条件下的药物释放、丸粒溶胀和溶蚀情况,并对药物释放和丸粒溶蚀与介质参数进行相关性分析。结果:与在不含酶介质相比,羧甲基魔芋胶小丸在含酶介质中的药物释放和丸粒溶蚀明显加快,随酶浓度增加,药物释放及丸粒溶蚀程度增加,药物释药符合Peppas方程,其中释药指数n大于1;随介质离子强度降低,小丸溶胀程度、药物释放和丸粒溶蚀程度增加。结论:盐酸小檗碱羧甲基魔芋胶小丸体外释药与介质中酶浓度和离子强度有关,释药过程为酶降解溶蚀释放,具有结肠定位释药的可行性。

Objective：The factors which influence in vitro release of berberine hydrochloride（BH） from carboxymethyl konjac glucomannan（CMKGM） pellets were studied to elevate drug release characteristics of the CMKGM pellets.Methods： CMKGM pellets were prepared by ionotropic gelation technique.The effects of β-mannase concentration and ionic strengthen of dissolution media on the release of BH,the swelling and erosion properties of the pellets were studied.The correlations between release of BH,erosion properties of the pellets and parameters of the dissolution media were studied.Results： Compared with the dissolution media without enzyme,the release of BH and the erosion of the pellets were increased obviously in the media withβ-mannase.With the increased of β-mannase concentration,the release of BH and the erosion of the pellets increased.The release of BH followed Peppas equation,the n value was more than 1.With the decreased of ionic strength,the release of BH,the swelling and erosion of the pellets increased.Conclusion： The release of BH from CMKGM pellets is related toβ-mannase concentration and ionic strength of dissolution media,drug release mechanism is enzymatic erosion-controlled,which indicates the potential of the pellets to serve as a colon-specific drug delivery system.