Citation: ZHANG Jian-Jun, ZU Hui, GAO Yuan. Formation Thermodynamics of Adefovir Dipivoxil-Saccharin Co-Crystals[J]. Acta Physico-Chimica Sinica, ;2011, 27(03): 547-552. doi: 10.3866/PKU.WHXB20110330 shu

Formation Thermodynamics of Adefovir Dipivoxil-Saccharin Co-Crystals

ZHANG Jian-Jun ¹ ,
ZU Hui ^1, ,
GAO Yuan ^2,

1.
1. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, P. R. China;
2. Department of Chinese Medicine Pharmaceutics, China Pharmaceutical University, Nanjing 210009, P. R. China

Received Date: 25 September 2010
Available Online: 17 February 2011
Fund Project: 国家重大新药创制科技重大专项新制剂与新释药系统技术平台项目(2009ZX09310-004, 2011ZX09201-101-02)资助 (2009ZX09310-004, 2011ZX09201-101-02)

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 (K₁₁), and Gibbs free energy (ΔG⁰) 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 K₁₁ in ethanolic solution. K_sp decreased and K₁₁ 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.
- Adefovir dipivoxil,
- Saccharin,
- Cocrystal,
- Solubility,
- Thermodynamics
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