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广泛用于治疗心绞痛和对急症高血压危象有效的硝苯吡啶(NF),当前仅有口服制剂。本文报道的PEG基质制备NF 直肠栓剂,经8名男性健康受试者,按随机交叉方法设计实验,与口服软胶囊进行生物利用度比较。血浆中NF 浓度用GC 法测定。实验数据采用非线性最小二乘方回归计算机程序,根据AIC 规则选择隔室模型,得到T lag、Ka 和Kel 或β,用梯形面积法求得0～7 h 的AUC_(0～7),并进行t 检验比较它们之间的差异。结果表明,直肠给药可以避免因胃肠道代谢的首过效应,所以吸收比口服给药好。在给药后1.5 h,栓剂的血药浓度超过胶囊,在1.75 h 达67.8ng/ml,并保持
It is widely used in the treatment of angina pectoris and nifedipine (NF), which is effective in acute crisis of hypertensive crisis, currently only oral preparations. This article reports the preparation of NF rectal suppository with PEG matrix. Eight healthy male subjects were randomized to cross-test to compare their bioavailability with oral soft capsules. Plasma NF concentrations were measured by GC method. The experimental data were obtained by non-linear least-squares regression computer program. According to the AIC rule, the compartment model was selected to obtain T lag, Ka and Kel or β, and the AUC 0-7 was obtained from 0 to 7 h using the trapezoidal area method. T test was performed to compare the differences between them. The results show that rectal administration can avoid the first pass effect of gastrointestinal metabolism, so the absorption is better than oral administration. At 1.5 h after administration, the suppository’s plasma concentration exceeded that of the capsule, reaching 67.8 ng / ml at 1.75 h and remained