Preparation of konjak gum-metronidazole matrix tablets and study on its drug-release properties in vitro | 魔芋胶-甲硝唑骨架片的制备及体外释药特性研究

中国人. ［目的］探讨骨架片体外药物释放的影响因素及其药物释放特性。［方法］以甲硝唑为模型药物，采用湿法制粒压片制备魔芋葡甘聚糖（KGM）-甲硝唑骨架片，以释放度为指标，研究了骨架材料含量、KGM粒度、释放介质pH值、离子强度以及不同转速对KGM-甲硝唑骨架片体外释药的影响。［结果］辅料片在蒸馏水中的溶胀度最大，在pH值为6.8的PBS中次之，在0.1 mol/L HCl中最小。KGM粒度对释药的影响不大。在10%~20%的范围内，骨架材料含量越高，缓释效果越好。骨架材料含量为20%时，12 h后药物的累积释放率为85%。在0.1 mol/L HCl中，2 h后KGM-甲硝唑骨架片中的药物几乎全部释放。药物释放速度随介质离子强度的增强而加快。转速大时，药物释放快，转速越小，药物控释越好。［结论］魔芋葡甘聚糖具有较好的缓、控释特性，是一种极有发展潜力的新型药物制剂辅料。

英语. ［Objective］The study aimed to discuss the influencing factors of drug-release in vitro from matrix tablets and their drug-release properties.［Method］With metronidazole as model drug, the konjak gum (KGM)_metronidazole matrix tablets were prepared by wetting granulating and compressing method. With release rate as index, the influences of the content of matrix material, particle size of KGM, pH and ionic strength of dissolution medium and different rotational speeds on the drug-release in vitro from KGM-metronidazole matrix tablets.［Result］The swelling degree of the adjunct was greatest in distilled water, secondary in PBS with pH value of 6.8 and least in 0.1 mol/L HCl. The particle size of KGM had little influence on drug-release. In the range of 10%-20%, the higher the content of matrix material was, the better the slow release effect was. When the content of matrix material was 20%, the accumulative release rate of drug was 85% after 12 h. In 0.1 mol/L HCl, the drug was released from KGM-metronidazole matrix tablets nearly completely after 2 h. The drug-release speed was increased as the ionic strength of medium was increased. When the rotation speed was high, the drug-release was fast and the less the rotation speed was, the better the controlled drug-release was.［Conclusion］The konjak glucomannan had relatively good slow and controlled release properties and it was a new type of pharmaceutical adjunct with very great development potential.