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替马西泮软胶囊的生物利用度。

Bioavailability of temazepam in soft gelatin capsules.

作者信息

Fuccella L M

出版信息

Br J Clin Pharmacol. 1979;8(1):31S-35S. doi: 10.1111/j.1365-2125.1979.tb00452.x.

Abstract

1 Healthy volunteers received single doses of temazepam 30 mg in conventional gelatin capsules, suppositories or in solution. They experienced marked sedation and sleepiness. The onset of sleepiness was prompt after the administration of the solution; this latter showed the fastest absorption and gave the highest peak plasma levels. This observation led to the development of the soft gelatin capsule. 2 To assess bioavailability of the formulation, plasma levels of temazepam were determined in healthy volunteers after single oral administration of soft and hard capsules, and after seven consecutive night-time doses of the soft capsule. Absorption from the soft gelatin capsule was faster and produced earlier and higher peak plasma levels. There were no differences in relative availability. 3 The apparent half-life of temazepam after night-time administration was shorter than after morning administration, but no change was observed between the first and seventh night-time doses.

摘要
  1. 健康志愿者分别单次服用30毫克替马西泮,剂型为传统明胶胶囊、栓剂或溶液。他们出现了明显的镇静和嗜睡症状。服用溶液后很快就出现了嗜睡症状;溶液吸收最快,血浆峰值水平最高。这一观察结果促使了软胶囊的研发。2. 为评估该制剂的生物利用度,在健康志愿者单次口服软胶囊和硬胶囊后,以及连续七个夜间剂量服用软胶囊后,测定替马西泮的血浆水平。软胶囊的吸收更快,血浆峰值水平出现得更早且更高。相对生物利用度没有差异。3. 夜间给药后替马西泮的表观半衰期比早晨给药后短,但在第一个和第七个夜间剂量之间未观察到变化。

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Bioavailability of temazepam in soft gelatin capsules.替马西泮软胶囊的生物利用度。
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