Zylber-Katz E, Koren G, Granit L, Levy M
Biopharm Drug Dispos. 1984 Apr-Jun;5(2):109-15. doi: 10.1002/bdd.2510050204.
In a random cross-over study, eight healthy volunteers received single 10 mg doses of either nifedipine capsule (Adalat, Bayer) or nifedipine tablets (Taro) after an overnight fast. The areas under the serum concentration time curves were not significantly different (AUC0----infinity 319.8 +/- 28.0 (SEM) ng ml-1 h-1 for capsules, 260.8 +/- 15.3 ng ml-1 h-1 for tablets). The peak serum levels and the time of their occurrence were 162.4 +/- 23.4 ng ml-1 at 30 min for capsules and 43.0 +/- 3.0 ng ml-1 at 1-2 h for tablets, indicating that the absorption of nifedipine from the capsule is faster than from the tablet form. Clinical symptoms of vasodilation corresponded with the nifedipine peak levels. We conclude that although the bioavailability in general of the two preparations is similar, the therapeutic equivalence may differ. Depending on the therapeutic indication each preparation may have its merits.
在一项随机交叉研究中,8名健康志愿者在禁食过夜后,单次服用10毫克剂量的硝苯地平胶囊(拜耳公司的心痛定)或硝苯地平片(塔罗公司生产)。血清浓度-时间曲线下面积无显著差异(胶囊的AUC0-无穷大 为319.8±28.0(SEM)纳克/毫升·小时,片剂为260.8±15.3纳克/毫升·小时)。血清峰值水平及其出现时间分别为:胶囊在30分钟时为162.4±23.4纳克/毫升,片剂在1-2小时时为43.0±3.0纳克/毫升,这表明硝苯地平从胶囊中的吸收比片剂更快。血管舒张的临床症状与硝苯地平峰值水平相符。我们得出结论,虽然两种制剂的总体生物利用度相似,但治疗等效性可能不同。根据治疗指征,每种制剂可能都有其优点。