摘要
采用薄膜包衣法制备乙酰水杨酸肠溶微丸,以转篮法(100 r/min,37+0.5℃)测定了体外溶出速率。实验结果表明:本制剂2 h在人工胃液中的释放量不超过15%,转入人工肠液后在40min内完全释放(Kr=2.975 h^(-1))。体内试验选择了六名健康受试者(平行法单剂量给药900 mg)服用乙酰水杨酸普通片及肠溶微丸,测定了二种制剂在体内的经时过程。药动学参数的求算表明:普通片:Ka=0.309 h^(-1),K=0.309 h^(-1),Cls=1.598 L/h,AUC=563.30 h·μg/ml;肠溶微丸:Ka=0.415h^(-1),K=0.134 h^(-1),Cls=1.235 L/h,AUC=728.66 h·μg/ml。
Enteric aspirin pellets (EAP) were developed through a diffusion rate controlling membrane. The drug dissolution rate was measured by the rotary basket method (100 r/min, 37±0.5℃). Thc results showed that in the first two hours the aspirin released less than 15% in simulated gastric fluid and then all released in 40 min in artificial intestinal liquid (Kr = 2.975 h^(-1)). The plasma concentration-time curves of two preparations (900 mg) were obtained by six healthy voluntcers administrated the commcrcial aspirin tablet (CAT) and EAP. The pharmacokinetic parameters of Ka, K, Cls, AUC were calculated based on the average plasma level data: CAT, 0.309 h^(-1), 0.309 h^(-1), 1.598 L/h, 563.30 h·μg / ml; EAP, 0.415 h^(-1), 0.134 h^(-1), 1.235 L/h, 728.66 h·μg/ml, respectively.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1990年第3期147-150,共4页
Journal of China Pharmaceutical University
关键词
乙酰水杨酸
肠溶微丸
研制
药剂学
Aspirin
Enteric pellets
Dissolution
Pharmacokinetics
