بررسی روش های مختلف افزایش حل پذیری و سرعت انحلال داروی کارودیلول

Abstract

IntroductionSolubility measurement and dissolution rate of drugs in different solvents are the key elements of their characterizations during drug discovery processes.A number of methodologies can be adapted to improve that, further to improve its bioavailability.AimsDetermining the solubility ofcarvedilol (CVD), and checking the predictability of some mathematical methods are the most important aims of this research.Method and materialsIn this studythe solubility ofCVD a nonselective beta-blocker in binarymixtures of (ethanol + propylene glycol (PG)) at different temperatureswere reported. The modified versions of the vant Hoff and Gibbs equations were used to calculate the thermodynamic properties (enthalpy (H), entropy (S), and Gibbs energy (G) standard free energy changes of solutions) for CVD dissolved in (ethanol (1) + PG (2)) mixtures from the solubility data. Result and discussionThe solubility data of CVD in (ethanol (1) + PG (2)) at different temperatures were correlated using different mathematical models, i.e., the JouybanAcree model, a combination of the JouybanAcree model with the vant Hoff model, and two modified versions of the JouybanAcree model. Solubility data of drug were used to develop a quantitativestructureproperty relationship model for predicting solubility in solvent mixtures. In addition, enthalpyentropy compensation using H vs G and H vs TS which explains the mechanism of cosolvency at different temperatures was discussed.The last part of this thesis has been designed to serve as a quick reference for cardiovascular drugs solubility collected from literature.ConclusionThe solubility of CVD increased in the solvent mixtures in addition increased temperature lead to enhanced solubility. Also the measured data were used to evaluate the prediction capability and checking the previous mathematical methods.