阿司匹林缓冲片的溶出度和生物利用度

 目的：测定阿司匹林缓冲片的体外溶出速率、酸中和能力、单剂量和多剂po的生物利用度及其对胃粘膜的剌激作用。方法：体外溶出采用转篮法；生物利用度测定采用受试者自身交叉对照试验，剂量为0.9g；胃粘膜刺激作用采用大鼠ig后2h的胃体解剖镜窥检进行。结果：缓冲片和普通片溶出50%所需时间分别为0.74 mill和3.67min。单剂量po后峰时分别为1.23h和3.08h,有极显著差异；峰浓分别为154μg/ml和133μg/ml;葯-时曲线下面积AUC分别为1 454 (fxg?h)/ml和1343(fig?h)/ml；多剂量稳态峰浓分别为297.5μg/ml和270.8μg/ml。缓冲片对大鼠胃刺激性小于对照片。结论：阿司匹林缓冲片溶出吸收迅速、完全，对胃粘膜刺激性减轻，明显优于普通片。

Thedissolutionandbioavailabilityofbuferedaspirintablet

OBJECTIVE:To determine the in vitro dissolution rate and acidnentralizing capacity,single dose and multiple dose bioavailabilities and irritation on gastric mucosa of the buffered aspirin tablet in our Lab. were designed. METHOD:The rotating basket method was used for dissolution test. The bioavailablity was evaluated by cross-over design with a dose of 0.9 g. The examination of the irritation on stomach mucosa was carried under a dissecting microscope 2 hours after adminitration of the drug to rats. RESULTS:The times for 50% aspirin dissolution from buffered and conventional tablets were 0.74 min and 3.76 min,respectively. The peak time after single dose administration were 1.23 h and 3.08 h,respectively,which showed significant difference. The peak levels were 154μg/ml and 133μg/ml,and the areas under the curve were 1454 (μg?h)/ml and 1343 (fxg?h)/ml,respectively. The peak levels at steady state after multiple dose were 297.5μg/ml and 270.8 fxg/ml repectively. The gastric erosion following administration of buffered tablet was reduced compared with conventional tablet. CONCLUSION:The buffered aspirin tablet causes less gastric irritation, dissolves more reapidly, and is absorbed much better than conventional tablet.