Prediction of benzodiazepines solubility using different cosolvency models

Nokhodchi, A, Shokri, J, Barzegar-Jalali, M and Ghafourian, T (2002) Prediction of benzodiazepines solubility using different cosolvency models. Farmaco, 57 (7). pp. 555-557. ISSN 0014-827X

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Abstract

The solubility of four benzodiazepines (BZPs) including diazepam (DIZ), lorazepam (LRZ) clonazepam (CLZ), and chlordiazepoxide (CHZ) in water-cosolvent (ethanol propylene glycol and polyethylene glycol 200) binary systems were studied. In general, increasing the volume fraction of cosolvents resulted in an increase in the solubility of benzodiazepines. The mole fraction solubilities were fitted to the various cosolvency models, namely extended Hildebrand approach (EHA), excess free energy (EFE), combined nearly ideal binary solvent/Redlich-Kister (CNIBS/R-K), general single model (GSM), mixture response surface (MR-S), double log-log (DL-L), and linear double log-log (LDL-L). The results showed that DL-L model was the best model in predicting the solubility of all drugs in all the water-cosolvent mixtures (OAE=4.71). The minimum and maximum errors were observed for benzodiazepine's solubility in water-propylene glycol and water-ethanol mixtures which were 2.67 and 11.78, respectively. Three models (EFE, CNIBS/R-K and LDL-L) were chosen as general models for solubility descriptions of these structurally similar drugs in each of the solvent systems. Among these models, the EFE model was the best in predicting the solubility of benzodiazepines in binary solvent mixtures (OAE=11.19). © 2002 �ditions scientifiques et médicales Elsevier SAS. All rights reserved.

Item Type: Article
Additional Information: cited By 9
Keywords: alcohol; benzodiazepine derivative; chlordiazepoxide; clonazepam; diazepam; drug solvent; lorazepam; macrogol 200; propanediol derivative; water; anxiolytic agent; benzodiazepine derivative; chlordiazepoxide; clonazepam; diazepam; lorazepam; solvent, conference paper; drug solubility; error; model; prediction; article; chemical model; chemistry; prediction and forecasting; solubility, Anti-Anxiety Agents, Benzodiazepine; Benzodiazepines; Chlordiazepoxide; Clonazepam; Diazepam; Lorazepam; Models, Chemical; Predictive Value of Tests; Solubility; Solvents; Anti-Anxiety Agents; Chlordiazepoxide; Clonazepam; Diazepam; Lorazepam; Predictive Value of Tests; Solubility; Solvents
Schools and Departments: School of Life Sciences > Biochemistry
Depositing User: Taravat Ghafourian
Date Deposited: 28 Nov 2017 13:54
Last Modified: 28 Nov 2017 13:54
URI: http://sro.sussex.ac.uk/id/eprint/64165

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