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一种新型儿科缓释茶碱片以整片或分服形式给药时的绝对生物利用度。

The absolute bioavailability of a new pediatric sustained release theophylline tablet, when given as whole or divided tablets.

作者信息

Jonkman J H, van der Boon W J, Schoenmaker R, Holtkamp A, Thürkow-Luikens A J

出版信息

Int J Clin Pharmacol Ther Toxicol. 1984 Sep;22(9):506-10.

PMID:6500770
Abstract

Absorption characteristics and absolute bioavailability of a new sustained release theophylline tablet for pediatric use were investigated in seven volunteers, both after administration of whole tablets and tablets broken into four equal parts. An intravenous infusion of 200 mg theophylline (as aminophylline) was also administered to the same panel of subjects. Theophylline plasma concentrations were measured frequently during a period of 33 h post dosing. Both after intake of the whole and the broken tablets steadily increasing theophylline plasma concentrations were found. The maximum concentration was found after 5.2 +/- 0.6 h (mean +/- S.D.) and 5.3 +/- 2.2 h and measured 2.00 +/- 0.28 mg.1-1 and 2.46 +/- 0.60 mg.1-1, respectively. The absorption process continued for a considerable period. As a consequence the theophylline plasma concentrations remained above 75% of the maximum value during a period of 8.9 +/- 2.1 h and 8.6 +/- 2.0 h. The absolute bioavailability of the whole tablets was 91.8 +/- 24.7% and that of the broken tablets was 95.8 +/- 9.7%.

摘要

在7名志愿者中研究了一种新型小儿用缓释茶碱片的吸收特性和绝对生物利用度,给药方式分别为整片服用和将片剂分成四等份服用。还对同一组受试者静脉输注200mg茶碱(以氨茶碱形式)。给药后33小时内频繁测量茶碱血浆浓度。服用整片和破碎片剂后均发现茶碱血浆浓度稳步上升。最大浓度分别在5.2±0.6小时(平均值±标准差)和5.3±2.2小时出现,测量值分别为2.00±0.28mg·L⁻¹和2.46±0.60mg·L⁻¹。吸收过程持续了相当长的时间。因此,茶碱血浆浓度在8.9±2.1小时和8.6±2.0小时内保持在最大值的75%以上。整片片剂的绝对生物利用度为91.8±24.7%,破碎片剂的绝对生物利用度为95.8±9.7%。

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