泰国持续性哮喘儿童中缓释茶碱口服制剂药代动力学特征的比较研究。

Comparative study of the pharmacokinetic characteristics of slow release theophylline oral preparations in Thai children with persistent asthma.

作者信息

Trakultivakorn M, Kanthawatana S, Tontayapiwat A, Jiraporncharoen K

机构信息

Department of Pediatrics, Chiang Mai University, Thailand.

出版信息

Asian Pac J Allergy Immunol. 1999 Dec;17(4):255-9.

PMID:10698464

Abstract

Significant differences in the rate and extent of absorption exist between slow release theophylline (SRT) preparations. The pharmacokinetic characteristics of Xanthium were compared with those of Theo-Dur in twelve Thai children with stable persistent asthma by randomized, double blind, crossover study. Serum theophylline concentrations (STCs) were determined by fluorescence polarization immunoassay. The pharmacokinetic parameters were estimated by using a computer program (Topfit 2.0). The STCs, at steady state after different doses, were predicted by using the modified Wagner-Nelson Equation. The mean resident time (MRT) and apparent T1/2 were significantly larger for Xanthium, but the Cmax and AUC0-infinity of Xanthium were significantly lower than those of Theo-Dur. The Frel of Xanthium was 80.1% relative to Theo-Dur. The appropriate dosing interval of both preparations for Thai children was twice a day.

摘要

缓释型茶碱（SRT）制剂在吸收速率和程度上存在显著差异。通过随机、双盲、交叉研究，比较了12名患有稳定持续性哮喘的泰国儿童中，黄嘌呤与茶喘平的药代动力学特征。血清茶碱浓度（STCs）通过荧光偏振免疫测定法测定。药代动力学参数通过计算机程序（Topfit 2.0）估算。使用改良的Wagner-Nelson方程预测不同剂量后稳态下的STCs。黄嘌呤的平均驻留时间（MRT）和表观T1/2显著更长，但黄嘌呤的Cmax和AUC0-无穷大显著低于茶喘平。相对于茶喘平，黄嘌呤的相对生物利用度（Frel）为80.1%。两种制剂对泰国儿童的合适给药间隔均为每日两次。