Article

Solubility analysis of buspirone hydrochloride polymorphs: measurements and prediction.

Department of Chemical and Biochemical Engineering, The University of Western Ontario, London, Ontario N6A 5B9, Canada.
International Journal of Pharmaceutics (impact factor: 3.35). 07/2007; 338(1-2):55-63. DOI:10.1016/j.ijpharm.2007.01.022 pp.55-63
Source: PubMed

ABSTRACT In this paper, the solubility of two polymorphs of buspirone hydrochloride (BUS-HCl) in isopropanol, water and mixture of these two solvents has been investigated. The solubility of BUS-HCl Form 2 in water and isopropanol is higher than BUS-HCl Form 1. According to thermodynamic properties and Burger and Ramberger polymorphic rules (Bernstein, 2002), BUS-HCl Forms 1 and 2 are enantiotropes (Sheikhzadeh et al., 2007). Using the solubility data, transformation analysis has been done and the results confirm these two polymorphs are enantiotropes and Form 1 converts to Form 2 at 95 degrees C. The UNIQUAC binary adjustable parameters have been found and based on these parameters, the solubility of these molecules has been predicted and compared with the experimental solubility. The solubility prediction has been performed by using different UNIFAC equations for binary and ternary systems. The UNIQUAC and original UNIFAC showed better prediction capability. Different general solubility equations (GSE) have been used for estimation of solubility which works based on partial charge, hydrogen bond factors and partition coefficients.

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Keywords

95 degrees C
 
BUS-HCl Form 1
 
BUS-HCl Form 2
 
BUS-HCl Forms 1
 
Different general solubility equations
 
different UNIFAC equations
 
experimental solubility
 
Form 1 converts
 
Form 2
 
hydrogen bond factors
 
original UNIFAC
 
partial charge
 
prediction capability
 
solubility data
 
solubility prediction
 
ternary systems
 
transformation analysis
 
two polymorphs
 
two solvents
 
UNIQUAC binary adjustable parameters