Formation Thermodynamics of Adefovir Dipivoxil-Saccharin Co-Crystals

被引：4

作者：

Zhang Jian-Jun ^{[1
]}

Zu Hui ^{[1
]}

Gao Yuan ^{[2
]}

机构：

[1] China Pharmaceut Univ, Dept Pharmaceut, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Dept Chinese Med Pharmaceut, Nanjing 210009, Peoples R China

来源：

ACTA PHYSICO-CHIMICA SINICA | 2011年 / 27卷 / 03期

关键词：

Adefovir dipivoxil; Saccharin; Cocrystal; Solubility; Thermodynamics;

D O I：

10.3866/PKU.WHXB20110330

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

The solubilities of adefovir dipivoxil (AD) in saccharin (SAC) ethanolic solutions at different temperatures and in SAC aqueous solutions at constant temperature were determined to investigate the thermodynamic characteristics of AD-SAC co-crystals. The solubility products (K-sp), complexation constants (K-11), and Gibbs free energy (Delta G(0)) were calculated. Ternary phase diagrams of the AD-SAC-ethanol systems at various temperatures were established. We demonstrate that temperature has significant influence on the K-sp and K-11 in ethanolic solution. K-sp decreased and K-11 increased with a decrease in temperature. Dissolution of the co-crystals in ethanol is an endothermic process. Co-crystal formation is a spontaneous and endothermic process. A decrease in temperature favors complexation between the AD and SAC in ethanol. In aqueous solutions of SAC, the solubility of AD shows a three-stage profile with a platform.

引用

页码：547 / 552

页数：6

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