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目的:测定阿司匹林缓冲片的体外溶出速率、酸中和能力、单剂量和多剂量po的生物利用度及其对胃粘膜的刺激作用。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0.74min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;药-时曲线下面积AUC分别为1454(μgh)/ml和1343(μgh)/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
OBJECTIVE: To determine the in vitro dissolution rate, acid-neutralizing capacity, single-dose and multi-dose bioavailability of aspirin buffer tablets and their effects on gastric mucosa. Methods: In vitro dissolution was carried out by spin basket method. The bioavailability was measured by self-cross-controlled test in subjects with a dose of 0.9g. Gastric mucosal irritation was observed by gastric dissection at 2h after rat ig. Results: The time required to dissolve 50% of buffer tablets and tablets was 0.74 min and 3.67 min, respectively. The single-dose peak after po was 1.23h and 3.08h, respectively. The peak concentrations were 154μg / ml and 133μg / ml respectively. The area under the drug-time curve was 1454 (μgh) / ml and 1343 (Μgh) / ml; multiple dose steady-state peak concentrations were 297.5μg / ml and 270.8μg / ml respectively. Buffer tablets gastric irritation in rats less than the control. Conclusions: Aspirin buffer tablets dissolve rapidly and completely, and stimulate irritation of gastric mucosa, which is obviously better than ordinary tablets