摘要
目的:考察释放介质pH和离子强度对羧甲基魔芋胶小丸体外释药的影响,对其释药特性进行评价。方法:以盐酸小檗碱为模型药物,采用离子胶凝法制备羧甲基魔芋胶小丸,测定小丸在不同pH(分别为pH1.0,pH5.0,pH6.8,pH7.4)和离子强度(pH6.8PBS液中分别加2,4,6,8g/L的NaCl)释放介质中的药物释放、溶胀度和溶蚀度,并对释药数据进行数学方程拟合,探讨其释药机制。结果:随释放介质pH增加或离子强度降低,丸粒的溶胀度和溶蚀度增加,小丸释药加快;在HCl液中,药物释放符合零级方程,释药机制为膜控释放,在PBS液中,药物释放符合Peppas方程,释药机制为扩散和溶蚀协同作用。结论:羧甲基魔芋胶小丸的溶胀度和溶蚀度均与释放介质pH和离子强度有关,从而影响其药物释放速率和释药机制。
AIM ： To study the effects of pH and ionic strength of release media on in vitro berberine hydrochloride （BH） released from carboxymethyl konjac glucomannan（CMKGM） pellets and to evaluate its characteristics. METHODS： The CMKGM pellets were prepared by ionotropic gelation with BH as the model drug. In vitro drug release, dynamic swelling and erosion percent of the pellets were studied respectively in release media with different pH（ pH 1.0,pH 5.0 ,pH 6.8, pH 7.4） or different ionic strength（ pH 6.8 PBS with 2,4,6,8 g/L NaC1）. The amount of BH released were confirmed in different equation to evaluate BH release mechanism of the pellets. RE- SULTS： With the increased of pH value or the decreased of ionic strength of the release media, the swelling ratio and erosion percent of the pellets increased, the BH release rate increased. The release of BH in HCl solution was filmcontrolled and exhibited zero order kinetic equation; the release of BH in PBS was non-Fickian release that coupled diffusion and erosion of the pellets matrix, exhibited Peppas equation. CONCLUSION ： The swelling ratio and erosion percent of CMKGM pellets is related to pH and ionic strength of the release media, which influence BH released and release mechanism of the pellets.
出处
《中成药》
CAS
CSCD
北大核心
2008年第10期1446-1450,共5页
Chinese Traditional Patent Medicine
关键词
羧甲基魔芋胶小丸
PH
离子强度
体外释药
盐酸小檗碱
carboxymethyl konjae glucomannan pellets
pH
ionic strength
in vitro drug release
berberine hydrochloride
