چاپ صفحه |  صفحه نخست سامانه |  نویسندگان |  اطلاعات تفضیلی |  دانلود مقاله | دانشگاه علوم پزشکی تبریز |
| نویسنده | نفر چندم مقاله |
|---|---|
| ابوالقاسم جویبان | دوم |
| علی شایان فر | دوم |
| الهه رحیم پور | دوم |
| آیدا هاتفی | اول |
| عنوان | متن |
|---|---|
| کلمات کلیدی | Solubility, Ketoconazole, 1‐Propanol, Binary solvent mixture, Jouyban-Acree model, Jouyban-Acreevan’t Hoff |
| خلاصه مقاله | Introduction Solubility is one of the most important thermodynamic properties in drug discovery, and a major parameter to be considered in pharmaceutics in order to achieve suitable formulations for desired pharmacological response. Various methods have been developed to increase the aqueous solubility of a poorly soluble drugs such as cosolvency that is the most common and easy-to-use method in the pharmaceutical industry. In addition to the exhaustive experimental approaches for determination of solubility in different mixed solvents at various temperatures, a number of mathematical models have been developed for predicting of solubility and other physicochemical property such as density.The mathematical methods are good alternatives to experimental determinations, for the purpose of finding suitable cosolvent concentrations to maximize the drug solubiliy.The objectives of this work were to (1) determine the solubility and density of saturated solutions of ketoconazole in the binary solvent mixtures of 1-propanol and water at temperatures ranging from (293.2 to 313.2) K; (2) correlate the experimental density data with the Jouyban– Acree model; and (3) calculate the mixing thermodynamic properties of ketoconazole dissolved in mixtures of 1propanol and water. Methods In this study, the solubility of ketoconazole was measured in binary mixtures of {1-propanol + water} by a simple shake-flask method at temperature range of 293.2-313.2 K.The experimental solubility data of ketoconazole in 1propanol+water were correlated by some developed cosolvency methods.Furthermore, the apparent thermodynamic properties of dissolution process of ketoconazole in all the mixed solvents were calculated according to van’t Hoff and Gibbs equations. Results According to solubility data, the highest solubility value for the studied mixed solvents is obtained in neat 1propanol at 313.2 K (2.17 × 10-1 mol∙L-1), whereas the lowest value is observed in neat water at 293.2 K (2.11 × 10-5 mol∙L-1). Moreover, it can be seen that ketoconazole solubility data shows an increase in solubility with an increase in temperature, and at all temperatures, the solubility rises as the 1- propanol proportion in the solvent mixtures increases and reaches a maximum value in neat 1-propanol. Conclusion This study reports the measured solubility data for ketoconazole in the mixtures of 1-propanol and water at temperatures of 293.2, 298.2, 303.2, 308.2 and 313.2 K. Eight cosolvency models including van’t Hoff, the double log-log, the mixture response surface, Yalkowsky, Jouyban-Acree, Jouyban-Acree-van’t Hoff, modified JouybanAcree-van’t Hoff, and the modified Wilson models are employed to mathematically representation of solubility data. The mean relative deviations calculated for each model show that Jouyban-Acree, andJouyban-Acree-van’t Hoff models show accurate results for the prediction of drug solubility at various temperatures and solvent composition.Furthermore, apparent thermodynamic parameters for ketoconazole in the investigated mixed solvent illustrate that ketoconazole dissolution is always endothermic and not spontaneous. |
| نام فایل | تاریخ درج فایل | اندازه فایل | دانلود |
|---|---|---|---|
| certificate.pdf | 1398/09/17 | 1037798 | دانلود |
| ticket.pdf | 1398/09/17 | 826397 | دانلود |
| abstract.png | 1398/09/17 | 473127 | دانلود |
| 2.docx | 1398/12/02 | 15699 | دانلود |
| 1 (1).docx | 1398/12/02 | 14327 | دانلود |
| Screenshot (19).png | 1398/12/02 | 375645 | دانلود |
