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在具有长B嵌段的环氧乙烷和1,2 - 丁烯氧化物二嵌段共聚物的水性胶束溶液中溶解灰黄霉素。

Solubilisation of griseofulvin in aqueous micellar solutions of diblock copolymers of ethylene oxide and 1,2-butylene oxide with lengthy B-blocks.

作者信息

Ribeiro Maria Elenir N P, Cavalcante Igor Marques, Ricardo Nágila M P S, Mai Shao-Min, Attwood David, Yeates Stephen G, Booth Colin

机构信息

Department of Organic and Inorganic Chemistry, Polymer Laboratory, Federal University of Ceará, CX 12.200, CEP 60455-760, Fortaleza, Ceará, Brazil.

出版信息

Int J Pharm. 2009 Mar 18;369(1-2):196-8. doi: 10.1016/j.ijpharm.2008.10.030. Epub 2008 Nov 7.

Abstract

The influence of hydrophobic-block length on solubilisation capacity was examined for micelles of E(m)B(n) copolymers (E=oxyethylene, B=oxybutylene, subscripts denote number-average block lengths in repeat units) with B-block lengths in the range of 30-76 and with E-blocks of sufficient length to ensure the formation of spherical micelles. Griseofulvin was used as a model poorly-water-soluble drug known to be almost exclusively solubilised in the micellar core. Combination of solubilisation data with those of a previous study has shown that the amount of drug solubilised per gram of hydrophobe is essentially independent of B-block length when this exceeds about 15 B units, suggesting that core size is not a major influence on solubilisation.

摘要

对于E(m)B(n)共聚物(E = 氧化乙烯,B = 氧化丁烯,下标表示重复单元中的数均嵌段长度)的胶束,研究了疏水嵌段长度对增溶能力的影响,其中B嵌段长度范围为30 - 76,且E嵌段长度足够以确保形成球形胶束。灰黄霉素用作一种难溶性药物模型,已知其几乎完全溶解在胶束核心中。增溶数据与先前研究的数据相结合表明,当B嵌段长度超过约15个B单元时,每克疏水剂增溶的药物量基本与B嵌段长度无关,这表明核心尺寸对增溶作用不是主要影响因素。

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