Abstract:

Poor aqueous solubility remains one of the major challenges in the context of oral bioavailability of the Biopharmaceutics Classification System (BCS) Class II drugs, where dissolution is the main rate-limiting step for the context of 1.2absorption. Strong dispersion technology has come as a viable solution to improve the dissolution rate of such drugs especially by the use of hydrophilic polymers. This paper explores the effect of the chosen hydrophilic polymers on the physicochemical properties and dissolution property of BCS Class II drug solid dispersions. In the present conceptual analysis, Eprosartan is assumed to be a prototypical BCS Class II antihypertensive agent that has low aqueous solubility and a dissolution-limited oral bioavailability, and thus, a good candidate to evaluate hydrophilic polymer-based solid dispersion systems. Polymeric solids that had been produced in solid dispersions were introduced into the evaporation of the solvents and the melt using polymers which included polyvinylpyrrolidone, hydroxypropyl methylcellulose, polyethylene glycol and Soluplus®. The interactions between drugs and polymers, crystal structure variation, thermal performance, wettability, and the increase of the dissolution rate were prepared. Findings indicate that hydrophilic polymers play highly significant roles in morphing drug, intermolecular hydrogen bonding, and wettability of surfaces thereby enhancing high rates of dissolution and stability of supersaturation. The comparative analysis demonstrates that polymer-specific changes influence the physical stability and dissolution performance, it is important to note that the polymer choice is crucial when designing solid dispersion. These results highlight the need to know more about the interactions between polymers and drugs to enhance formulation strategies to poorly soluble drugs.

Keywords:

BCS Class II drugs, solid dispersions, hydrophilic polymers, dissolution enhancement, physicochemical properties, amorphisation.

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