Brown G R, Fraser D G, Castile J A, Gaudreault P, Platt D R, Friedman P A
Int J Clin Pharmacol Ther Toxicol. 1986 Jun;24(6):283-6.
Although nifedipine is commonly administered sublingually in the clinical setting, a comparison of the serum concentrations obtained by this route vs oral administration has not been previously made. Nifedipine serum concentrations were measured in 6 healthy subjects following sublingual or oral administration of one nifedipine 10 mg capsule. Serum nifedipine concentrations were measured at regular intervals and demonstrated that sublingual administration produced measurable nifedipine concentrations sooner than oral administration. Peak nifedipine serum concentrations were less following sublingual administration (41.9 +/- 24.9 ng/ml) than following oral administration (99.6 +/- 49.8 ng/ml, p less than 0.05). The time to peak nifedipine serum concentration was also longer following sublingual administration than with the oral dose (74 +/- 24 minutes vs 40 +/- 14 minutes, p less than 0.05). Despite these differences, the areas under the serum concentration-time curve of the two routes of administration were similar. These differences in nifedipine concentrations may be an important consideration when choosing the route of administration of nifedipine.
尽管硝苯地平在临床中通常采用舌下给药,但此前尚未对该给药途径与口服给药所获得的血清浓度进行比较。对6名健康受试者分别舌下含服和口服一粒10毫克硝苯地平胶囊后的血清硝苯地平浓度进行了测定。定期测量血清硝苯地平浓度,结果表明舌下给药比口服给药更快产生可测量的硝苯地平浓度。舌下给药后的硝苯地平血清峰值浓度(41.9±24.9纳克/毫升)低于口服给药(99.6±49.8纳克/毫升,p<0.05)。舌下给药后达到硝苯地平血清峰值浓度的时间也比口服给药更长(74±24分钟对40±14分钟,p<0.05)。尽管存在这些差异,但两种给药途径的血清浓度-时间曲线下面积相似。在选择硝苯地平给药途径时,这些硝苯地平浓度的差异可能是一个重要的考虑因素。