Macleod G S, Fell J T, Collett J H
School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Oxford Road, Manchester, UK.
Int J Pharm. 1999 Oct 15;188(1):11-8. doi: 10.1016/s0378-5173(99)00197-0.
The influence of disintegrant on the water uptake and subsequent disintegration force developed was investigated in a simple tablet formulation. The results indicated that a reasonable correlation existed between water uptake and disintegration force for the disintegrants screened with cross linked polyvinyl pyrrolidone (PVP XL) showing a proportionally higher disintegration force for the amount of water imbibed. Two tablet formulations, intended to promote accelerated drug release in the colon, were prepared, with and without PVP XL, and film coated with a mixture of pectin, chitosan and HPMC. The two systems showed different drug release rates which were influenced by the pH of the dissolution medium. In the presence of pectinolytic enzyme, drug release was faster when compared to release in buffer alone for both systems although the mechanism differed for each. Drug release in simulated gastrointestinal conditions showed a bimodal profile with the increased drug release rate being triggered by the action of pectinolytic enzymes.
在一种简单的片剂配方中,研究了崩解剂对吸水及随后产生的崩解力的影响。结果表明,对于用交联聚乙烯吡咯烷酮(PVP XL)筛选出的崩解剂,吸水与崩解力之间存在合理的相关性,所吸收的水量越大,崩解力相应越高。制备了两种旨在促进结肠中药物加速释放的片剂配方,一种含有PVP XL,另一种不含,并用果胶、壳聚糖和羟丙基甲基纤维素的混合物进行薄膜包衣。这两种体系显示出不同的药物释放速率,且受溶出介质pH值的影响。在存在果胶酶的情况下,与仅在缓冲液中释放相比,两种体系的药物释放都更快,尽管每种体系的机制不同。模拟胃肠道条件下的药物释放呈现双峰曲线,果胶酶的作用引发了药物释放速率的增加。