European Journal of Biomedical and Pharmaceutical Sciences

EXPLORING DRY CO-GRINDING APPROACH AS A TOOL TO IMPROVE THE DISSOLUTION RATE OF POORLY SOLUBLE DRUG

Alaa Y. Bazeed*, Ahmed Nouh, Ebtessam A. Essa and Gamal M. El Maghraby

ABSTRACT

Nateglinide is a non-sulphonylurea which was approved for treatment of type II diabetes mellitus. It shows a pH dependent solubility that resulted in a variable and incomplete oral bioavailability, that may put the diabetic patient at risk. This work introduces dry co-grinding of the drug with inert carrier as a method for enhanced dissolution rate of nateglinide. Aerosil 200 was used as an inert excipient. Three formulations were prepared at different molar ratios (1:1, 1:2 and 1:3 drug to aerosil 200). Drug dissolution was monitored before and after processing. The developed formulations showed significant increase in drug dissolution compared to the unprocessed nateglinide. This study introduced the dry co-grinding process as a solvent free technique, which can be performed during the regular production process, as a promising tool to improve dissolution rate of poorly soluble drugs.

Keywords: Nateglinide, Aerosil 200, colloidal silicon dioxide, co-processing.