Cross-linked high amylose starch derivatives for drug release II. Swelling properties and mechanistic study

被引:50
作者
Mulhbacher, J [1 ]
Ispas-Szabo, P [1 ]
Mateescu, MA [1 ]
机构
[1] Univ Quebec, Dept Chem & Biochem, Montreal, PQ H3C 3P8, Canada
关键词
high amylose starch derivatives; polymeric networks; controlled release mechanisms; swelling properties;
D O I
10.1016/j.ijpharm.2004.03.008
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Acetate (Ac-), aminoethyl (AE-), and carboxymethyl (CM-) high amylose starch cross-linked 6 (HASCL-6) derivatives were previously shown to control the release of drugs over 20 It from monolithic tablets highly loaded (up to 60% drug). This report describes the swelling characteristics, which allow a better understanding of the mechanisms involved in the control of the drug release from the said polymeric matrices. The tablet swelling of HASCL-6, Ac-HASCL-6, and AE-HASCL-6 was found to not be affected by the ionic strength and by the pH between 1.2 (gastric) and 7 (intestinal), whereas the swelling of CM-HASCL-6 was shown to depend on both ionic strength and pH of the release medium. For all the studied polymers the drug loading did not change the equilibrium swelling ratio but affected the initial swelling velocity, seemingly due to the competition between drug and polymer for water uptake, a phenomenon probably influenced by the loading and the drug Solubility. It was also shown that the increase of ionic strength would slightly increase the drug release time probably by decreasing the amount of free water still available to solubilize the drug present into the matrix. (C) 2004 Elsevier B.V. All rights reserved.
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页码:231 / 238
页数:8
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