κ-卡拉胶/魔芋胶骨架片的体外释药特性研究

Studies on in vitro release characteristics of drug from κ-carrageenan/konjac glucomannan matrix tablet

目的:通过κ-卡拉胶/魔芋胶骨架片的体外释放研究,探讨其释药特性。方法:将κ-卡拉胶和魔芋胶混合作为骨架材料,以盐酸青藤碱为模型药物,采用湿法制粒压片法制备骨架片,测定介质pH值、离子强度和搅拌转速对骨架片体外释药和溶蚀度的影响,分别采用Peppas方程和零级方程对骨架片的释药数据和释药过程中骨架溶蚀数据进行拟合。结果:骨架片在0.1mol/L盐酸液中药物释放最快,纯化水中次之,pH6.8PBS中最慢;随介质离子强度增加,药物释放减慢(P<0.05),但氯化钠浓度达到0.1mol/L后,释药受离子强度影响不明显(P>0.1);随搅拌转速增加,药物释放加快(P<0.01);释药机制为扩散和溶蚀释放相结合。结论:κ-卡拉胶与魔芋胶复配可作为骨架材料用于缓释骨架片的制备。

AIM： The drug release characteristics of κ-carrageenan/konjac glucomannan matrix tablet were elvated by in vitro dissolution experiment. METHODS： Sinomenine hydrochloride was used as model drug,the matrix tablet containing κ-carrageenan and konjac glucomannan as matrix material were prepared by wet granulation technique. Drug release and tablet erosion in different pH values,ionic strength of media and rotation speeds were studied by in vitro dissolution experiment. The data of drug release and matrix tablet erosion were confirmed in Peppas and zero order equation,respectively. RESULTS： Among the rate of drug release in different media,0. 1 mol/L HCl was the fastest,distilled water was the second,pH6. 8 PBS was the slowest. The rate of drug release decreased with increasing the ionic strength of media（P 0. 05）,but the rate did not increase when the concentration of NaCl was more than 0. 1 mol/L（P 0. 1）. The rate of drug release increased with increasing the rotation speeds（P 0. 01）. Drug release mechanism was non-Fickian release that coupled diffusion and erosion model. CONCLUSION： κ-carrageenan/konjac glucomannan can be used as matrix material to prepare sustained-release matrix tablet.