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药物释放模块的组装:组装系统中模块形状和位置对漂浮行为和释放速率的影响。

Assemblage of drug release modules: effect of module shape and position in the assembled systems on floating behavior and release rate.

机构信息

Department of Pharmaceutical Technology, University of Ankara, Ankara, Turkey.

出版信息

Eur J Pharm Biopharm. 2011 Jan;77(1):116-21. doi: 10.1016/j.ejpb.2010.11.006. Epub 2010 Nov 16.

DOI:10.1016/j.ejpb.2010.11.006
PMID:21087663
Abstract

The aim of this work was to study the clindamycin release kinetics from floating delivery systems consisting of two modules assembled in void configuration, according to the modified release technology platform known as Dome Matrix®. Two modules differently shaped, i.e., female and male, formulated as swellable matrices and containing clindamycin, were assembled by friction interlocking. Then, by stacking additional female modules without drug on the assembled two-module floating system, modulation of clindamycin release rate and kinetics was attained. The additional modules stacked on the assembled system acted as a transient barrier to clindamycin release from the void configuration. Inertness, dissolution/erosion or swelling behavior characterized their performance as matrices in simulated gastric fluid. In particular, we found that stacking additional barrier modules on the bases of void configuration, the drug release rate and kinetics of the assembled system were modified in dependence on the composition of module added. In particular, the quickly soluble module exerted an influence on the release rate in the late time of delivery. The swellable module produced a significant reduction in release rate of void assembly, but the release mechanism remained the same. Finally, the inert module led to a substantial linearization of the release profile with a minimal reduction in release rate.

摘要

本工作旨在研究由两个模块以中空构型组装而成的、基于称为 Dome Matrix®的改良释放技术平台的漂浮型给药系统中克林霉素的释放动力学。两种不同形状的模块(即女式和男式)被制成可溶胀基质并包含克林霉素,通过摩擦互锁组装在一起。然后,通过在组装的两模块漂浮系统上堆叠不含药物的额外女式模块,可以调节克林霉素的释放速率和动力学。堆叠在组装系统上的额外模块充当从中空构型释放克林霉素的瞬时屏障。惰性、溶解/侵蚀或溶胀行为表征了它们在模拟胃液中的基质性能。特别是,我们发现,在中空构型的基础上堆叠额外的屏障模块会根据添加的模块组成来改变组装系统的药物释放速率和动力学。特别是,快速可溶性模块对输送后期的释放速率有影响。可溶胀模块显著降低了中空组装体的释放速率,但释放机制保持不变。最后,惰性模块导致释放曲线的显著线性化,同时释放速率的降低最小。

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