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.
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收藏
页码：547 / 552
页数：6
相关论文
共 13 条
  • [1] Modeling and prediction of cocrystal phase diagrams
    Ainouz, Abigail
    Authelin, Jean-Rene
    Billot, Pascal
    Lieberman, Harvey
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 374 (1-2) : 82 - 89
  • [2] The utility of a ternary phase diagram in the discovery of new co-crystal forms
    Chadwick, Keith
    Davey, Roger
    Sadiq, Ghazala
    Cross, Wendy
    Pritchard, Robin
    [J]. CRYSTENGCOMM, 2009, 11 (03): : 412 - 414
  • [3] Making co-crystals - The utility of ternary phase diagrams
    Chiarella, Renato A.
    Davey, Roger J.
    Peterson, Matthew L.
    [J]. CRYSTAL GROWTH & DESIGN, 2007, 7 (07) : 1223 - 1226
  • [4] Gao YA, 2010, PROG CHEM, V22, P829
  • [5] Role of Cocrystal and Solution Chemistry on the Formation and Stability of Cocrystals with Different Stoichiometry
    Jayasankar, Adivaraha
    Reddy, L. Sreenivas
    Bethune, Sarah J.
    Rodriguez-Hornedo, Nair
    [J]. CRYSTAL GROWTH & DESIGN, 2009, 9 (02) : 889 - 897
  • [6] Cocrystals definitions
    Lara-Ochoa, F.
    Espinosa-Petrez, G.
    [J]. SUPRAMOLECULAR CHEMISTRY, 2007, 19 (08) : 553 - 557
  • [7] MARTIN A, 1993, PHYS PHARMACY, P265
  • [8] Phase solubility diagrams of cocrystals are explained by solubility product and solution complexation
    Nehm, SJ
    Rodríguez-Spong, B
    Rodríguez-Hornedo, N
    [J]. CRYSTAL GROWTH & DESIGN, 2006, 6 (02) : 592 - 600
  • [9] PATRICK MN, 2003, ENGL J MED, V348, P808
  • [10] Rodriguez-Hornedo N., 2005, MOL PHARM, V3, P362
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