The use of isothermal titration calorimetry to assess the solubility enhancement of simvastatin by a range of surfactants

被引：22

作者：

Patel, Rajesh ^{[1
]}

Buckton, Graham ^{[1
]}

Gaisford, Simon ^{[1
]}

机构：

[1] Univ London, Sch Pharm, London WC1N 1AX, England

来源：

THERMOCHIMICA ACTA | 2007年 / 456卷 / 02期

关键词：

isothermal titration calorimetry (ITC); solubility enhancement; surfactants; simvastatin; free energy of transfer;

D O I：

10.1016/j.tca.2007.01.011

中图分类号：

O414.1 [热力学];

学科分类号：

摘要：

Surfactants are commonly used to increase the solubility of poorly water soluble drugs but the interactions between drug and surfactant can be complex and quantitative relationships can be hard to derive. One approach is to quantify the thermodynamics of interaction and relate these parameters to known solubility or dissolution rate enhancement data. Isothermal titration calorimetry (ITC) was used to measure the enthalpy and free energy of transfer of a model drug (simvastatin) to a number of surfactant (SDS, HTAB, SDCH and Brij 35) micelles. These data were then compared with the solubility enhancements determined for each surfactant using HPLC assays. As expected, there was correlation between the free energy of transfer for the drug to each surfactant and the solubility enhancement of that surfactant. Although the data set is limited, the results suggest that ITC screening of a range of surfactants against a poorly water soluble drug may allow the selection of the best potential solubilising surfactants. (c) 2007 Published by Elsevier B.V.

引用

页码：106 / 113

页数：8

共 45 条

[1] SOLUBILIZATION AND WETTING EFFECTS OF BILE-SALTS ON THE DISSOLUTION OF STEROIDS [J].