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扩展的希尔德布兰德溶解度方法:沙硝唑在二氧六环与水的混合物中的情况

Extended hildebrand solubility approach: satranidazole in mixtures of dioxane and water.

作者信息

Rathi P B, Mourya V K

机构信息

Department of Pharmaceutics, Shri Bhagwan College of Pharmacy, N-6, CIDCO, Aurangabad-431 003, India.

出版信息

Indian J Pharm Sci. 2011 May;73(3):315-9. doi: 10.4103/0250-474X.93518.

Abstract

The extended Hildebrand solubility parameter approach is used to estimate the solubility of satranidazole in binary solvent systems. The solubility of satranidazole in various dioxane-water mixtures was analyzed in terms of solute-solvent interactions using a modified version of Hildebrand-Scatchard treatment for regular solutions. The solubility of satranidazole in the binary solvent, dioxane-water shows a bell-shaped profile with a solubility maximum well above the ideal solubility of the drug. This is attributed to solvation of the drug with the dioxane-water mixture, and indicates that the solute-solvent interaction energy is larger than the geometric mean (δ(1)δ(2)) of regular solution theory. The new approach provides an accurate prediction of solubility once the interaction energy is obtained. In this case, the energy term is regressed against a polynomial in δ(1) of the binary mixture. A quartic expression of W in terms of solvent solubility parameter was found for predicting the solubility of satranidazole in dioxane-water mixtures. The method has potential usefulness in preformulation and formulation studies during which solubility prediction is important for drug design.

摘要

扩展的希尔德布兰德溶解度参数方法用于估算沙硝唑在二元溶剂体系中的溶解度。使用针对正规溶液的希尔德布兰德-斯卡查德处理的改进版本,从溶质-溶剂相互作用的角度分析了沙硝唑在各种二氧六环-水混合物中的溶解度。沙硝唑在二元溶剂二氧六环-水中的溶解度呈现钟形曲线,其最大溶解度远高于药物的理想溶解度。这归因于药物与二氧六环-水混合物的溶剂化作用,表明溶质-溶剂相互作用能大于正规溶液理论的几何平均值(δ(1)δ(2))。一旦获得相互作用能,新方法就能准确预测溶解度。在这种情况下,能量项根据二元混合物δ(1)中的多项式进行回归。发现了一个用溶剂溶解度参数表示的W的四次表达式,用于预测沙硝唑在二氧六环-水混合物中的溶解度。该方法在药物制剂前研究和制剂研究中具有潜在用途,在此期间溶解度预测对药物设计很重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1d0/3309655/978fa3777e54/IJPhS-73-315-g004.jpg

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