CONTROLLED RELEASE OF THEOPHYLLINE FROM CROSS-LINKED AMYLOSE TABLETS

被引：91
作者：
LENAERTS, V
DUMOULIN, Y
MATEESCU, MA
机构：
[1] Faculté de Pharmacie, Université de Montréal, Montréal, Que. H3C 3J7
来源：
JOURNAL OF CONTROLLED RELEASE | 1991年 / 15卷 / 01期
基金：
加拿大自然科学与工程研究理事会;
关键词：
CONTROLLED RELEASE OF THEOPHYLLINE; CROSS-LINKED AMYLOSE; POLYHYDROXYLIC POLYMERS; BIOCOMPATIBLE POLYMERS;
D O I：
10.1016/0168-3659(91)90101-I
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Amylose cross-linked (CLA) by epichlorohydrin treatment is introduced as a matrix for controlled release of drugs. Different reticulation degrees were obtained by varying the ratio of epichlorohydrin to amylose. A linear release of theophylline from the CLA tablets was observed in all cases. Linear increase of the cross-linking degree of the CLA used for tablet preparation generated non-linear diminution of the release time. For tablets obtained from CLA-7.5 (the lowest reticulation degree, realized by cross-linking of 100 g of amylose with 7.5 g of epichlorohydrin) containing theophylline up to 20% (w/w), a close to linear release was found over a period up to 15 h. For moderate increase of the cross-linking degree (CLA-12 and CLA-20) the release time was drastically decreased to 1-2 h. Release retardation in CLA-7.5 tablets seems to be related to the high amylose hydrogen interchain associations. Equilibrium swelling experiments in water and in 8 M urea support this hypothesis. The duration of the near-linear slow release was related to the duration of tablet swelling. The analysis of the data indicates that an anomalous release mechanism controls the transport of the drug; this includes neither Fickian diffusion nor glassy/rubbery transition. A hypothesis of a type of release controlled by hydrogen association is advanced.
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页码：39 / 46
页数：8
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