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某些茶碱缓释剂型的体外溶出行为。

In-vitro dissolution behavior of some sustained-release theophylline dosage forms.

作者信息

Lin S Y, Yang J C

出版信息

Pharm Acta Helv. 1989;64(8):236-40.

PMID:2780758
Abstract

In-vitro dissolution of theophylline from six commercially sustained-release (SR) preparations (Euphyllin retard, Euphyllin retard mite, Theovent L.A. 125 mg, Theovent L.A. 250 mg, Phyllocontin and Uniphyllin) was determined by using rotating basket and rotating bottle apparatus. The effect of pH and rotating speed on the dissolution rate of these SR products was also studied. Scanning electron microscope was used to observe the change of surface topograph and inner texture of these products before, during and after dissolution. The results indicates that the dissolution behavior was pH-dependent which corresponding to the types of SR products. The rotating bottle method was only suitable for the evaluation of release rate of spansule-type SR products and was not suitable for matrix-type SR tablets due to the sticking occurred on the bottle surface leading to faster dissolution and larger variation. The release mechanism of these six SR products can be deduced into three models. Fickian transport (Phyllocontin), non-Fickian transport (Euphyllin, Theovent L.A. 250 mg and Uniphyllin) and zero order transport (Theovent L.A. 125 mg).

摘要

采用转篮法和转瓶法测定了6种市售缓释(SR)制剂(优菲林缓释片、优菲林缓释微粒、茶新那敏控释片125mg、茶新那敏控释片250mg、菲洛可定和单硝酸异山梨酯缓释片)中茶碱的体外溶出度。还研究了pH值和转速对这些SR产品溶出速率的影响。利用扫描电子显微镜观察了这些产品在溶出前、溶出过程中和溶出后的表面形貌和内部结构变化。结果表明,溶出行为与pH值有关,这与SR产品的类型相对应。转瓶法仅适用于评价小丸型SR产品的释放速率,不适用于骨架型SR片剂,因为瓶表面会发生黏附,导致溶出加快且变化较大。这6种SR产品的释放机制可归纳为三种模型。菲克扩散(菲洛可定)、非菲克扩散(优菲林、茶新那敏控释片250mg和单硝酸异山梨酯缓释片)和零级释放(茶新那敏控释片125mg)。

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