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难溶性药物卡马西平在普朗尼克胶束中的增溶作用:分子特性、温度及添加盐对增溶能力的影响

Solubilization of poorly water-soluble drug carbamezapine in pluronic micelles: effect of molecular characteristics, temperature and added salt on the solubilizing capacity.

作者信息

Kadam Yogesh, Yerramilli Usha, Bahadur Anita

机构信息

Department of Chemistry, VN South Gujarat University, Surat, Gujarat, India.

出版信息

Colloids Surf B Biointerfaces. 2009 Aug 1;72(1):141-7. doi: 10.1016/j.colsurfb.2009.03.027. Epub 2009 Apr 5.

Abstract

The solubilization of a poorly water-soluble antiepileptic drug, carbamazepine (CBZ), in a series of micelle-forming PEO-PPO-PEO block copolymers with combinations of blocks having different molecular weight was studied. The drug solubility and micelle-water partition coefficient (P) were determined using UV-vis spectroscopy. Dynamic light scattering on copolymer solutions was used to measure size and polydispersity of nanoaggregates. Solubilization of carbamezapine increased with the rise in temperature and concentration of block copolymers, but no significant increase was observed with added salt (NaCl). The solubilization is also discussed from a thermodynamics viewpoint, by considering the standard free energy of solubilization (DeltaG degrees ).

摘要

研究了难溶性抗癫痫药物卡马西平(CBZ)在一系列具有不同分子量嵌段组合的形成胶束的聚环氧乙烷-聚环氧丙烷-聚环氧乙烷(PEO-PPO-PEO)嵌段共聚物中的增溶情况。使用紫外-可见光谱法测定药物溶解度和胶束-水分配系数(P)。通过对共聚物溶液进行动态光散射来测量纳米聚集体的尺寸和多分散性。卡马西平的增溶作用随嵌段共聚物温度和浓度的升高而增加,但添加盐(NaCl)时未观察到显著增加。还从热力学角度,通过考虑增溶标准自由能(ΔG°)对增溶作用进行了讨论。

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