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Determination of liposome/water partition coefficients of salmeterol and budesonide and study on their influencing factors

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Author:
No author available
Journal Title:
ACTA PHARMACEUTICA SINICA
Issue:
4
DOI:
10.3321/j.issn:0513-4870.2006.04.005
Key Word:
脂质体/水分配系数;沙美特罗;布地奈德;透析

Abstract: 目的测定沙美特罗和布地奈德的脂质体/水分配系数(PL/w),考察影响两种药物PL/w的因素,揭示药物与磷脂双分子层的作用机制.方法用平衡透析法测定两种药物在不同脂质体组成和不同介质中的PL/w.结果两种药物PL/w随脂质体中胆固醇含量及磷脂饱和程度增加而减小;脂质体表面负电荷、介质pH值及离子强度增加,沙美特罗的PL/w增加.脂质体表面电荷、介质pH值及离子强度对布地奈德的PL/w影响较小.结论药物PL/w受药物性质、脂质体磷脂种类、饱和程度、胆固醇含量和表面电荷以及介质pH和离子强度等因素影响,在测定时应选择与生物膜环境相近的PL/w测定条件,以反映药物在生物膜中的分配.

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