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AN UPDATED REVIEW ON TECHNICAL ADVANCES TO ENHANCE DISSOLUTION RATE OF HYDROPHOBIC DRUGS

Keywords: Solubility , Dissolution rates , Bioavailability , Hydrophobic Drugs , Solid dispersion , Hydrophilic carriers.

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Abstract:

The dissolution behavior of drugs continues to be one of the challenging aspects in formulation development. The advent of combinatorial chemistry and high throughput screening increased the number of hydrophobic compounds significantly. The Biopharmaceutical classification scheme (BCS) takes into account three major factors: solubility, intestinal permeability, and dissolution rate and all the three govern the rate and extent of oral absorption and hence bioavailability. Especially for BCS Class II substances the bioavailability of a poorly soluble drug may be enhanced by increasing the solubility and dissolution rate of it in the gastro-intestinal fluids. Drug substances whose highest dose is soluble in less than 250 ml of water over a range of pH from 1.0 to 7.5 are considered as highly soluble. In contrast, the drug compounds with solubility below 1mg mL-1 face significant dissolution or bioavailability problems. With the introduction of advanced technologies it could be possible to overcome the problems. The article provides an overview on the theoretical definitions and technical approaches broadly covering technologies and hydrophilic carriers or excipients used. Further part of the manuscript is committed to the formulation, analytical methods for the characterization of samples, dissolution or release kinetics and model fittings.

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