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可生物降解甲壳素微胶囊的制备及释放特性:I. 用相分离法制备6-巯基嘌呤微胶囊

Preparation and release properties of biodegradable chitin microcapsules: I. Preparation of 6-mercaptopurine microcapsules by phase separation methods.

作者信息

Mi F L, Tseng Y C, Chen C T, Shyu S S

机构信息

Department of Chemical Engineering, National Central University, Chung-Li, Taiwan, ROC.

出版信息

J Microencapsul. 1997 Jan-Feb;14(1):15-25. doi: 10.3109/02652049709056464.

Abstract

Chitin [poly-(N-acetyl-1,4-beta-D-glucopyranosamine)] microcapsules were prepared by the simple desolvation and the non-solvent addition phase separation methods. In the simple desolvation method, chitin droplets were dropped into the desolvation agent (water, ethanol, or acetone) and microcapsules soon formed. Several solvent-nonsolvent pairs: N,N-dimethylacetamide (DMAc)-water, DMAc-ethanol, DMAc-propanol, DMAc-n-butanol, and DMAc-acetone with different solubility parameter difference, (delta delta) were chosen to prepare chitin microcapsules containing 6-mercaptopurine by using the non-solvent-addition phase separation method. The results showed that the surface morphology and release behaviour of the microcapsules were greatly affected by different solvent-nonsolvent pairs. The surface of microcapsules prepared from the system of high delta delta was more smooth than those from the systems of low delta delta. The drug content using the simple desolvation method increased with decreasing delta delta because of the higher film formation rate of the microcapsules. On the other hand, the drug content using the nonsolvent addition method was lower than that using the simple desolvation method because of the dispersion forces, applied by mechanical stirring. Microcapsules prepared by the simple desolvation method had a narrower size distribution and larger mean size than those prepared by the nonsolvent addition method.

摘要

几丁质[聚(N - 乙酰基 - 1,4 - β - D - 吡喃葡萄糖胺)]微胶囊通过简单的去溶剂化法和非溶剂添加相分离法制备。在简单去溶剂化法中,将几丁质液滴滴入去溶剂化剂(水、乙醇或丙酮)中,微胶囊很快形成。选择了几种具有不同溶解度参数差(δδ)的溶剂 - 非溶剂对:N,N - 二甲基乙酰胺(DMAc) - 水、DMAc - 乙醇、DMAc - 丙醇、DMAc - 正丁醇和DMAc - 丙酮,采用非溶剂添加相分离法制备含6 - 巯基嘌呤的几丁质微胶囊。结果表明,不同的溶剂 - 非溶剂对极大地影响了微胶囊的表面形态和释放行为。由高δδ体系制备的微胶囊表面比低δδ体系制备的微胶囊表面更光滑。由于微胶囊的成膜速率较高,采用简单去溶剂化法时药物含量随δδ减小而增加。另一方面,由于机械搅拌施加的分散力,采用非溶剂添加法时药物含量低于采用简单去溶剂化法时的药物含量。采用简单去溶剂化法制备的微胶囊比采用非溶剂添加法制备的微胶囊具有更窄的尺寸分布和更大的平均尺寸。

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