Abstract

STUDY OF MICRONIZED GRADES OF TADALAFIL AND ITS EFFECT ON DISSOLUTION.

Kanekar H.*, Khan S. and Khale A.

Abstract

BCS class II and class IV drugs are having poor solubility which ultimately shows poor bioavailability. To enhance their aqueous solubility various techniques have been proposed amongst which are micronization, solid dispersion, co-crystallization and many more. Micronization is one of the techniques which is adopted by various pharmaceutical companies in order to enhance the solubility of the drug belonging to the class of Phosphodiesterase inhibitor (PDE 5) and to have quicker release formulations. Tadalafil is one such drug which is used to treat the erectile dysfunction and it acts by inhibition of cyclic GMP. The current study aimed to study micronized grades of Tadalafil having varying d (0.9) values and its effect on dissolution. All micronized grades are not suitable for formulation development and this study can help to decide the suitable micronized grade for conventional Tadalafil formulation. The particle size of the drug is selected based on its release in reported OGD medium for Tadalafil Immediate release dosage form. The study showed that the higher micronization of Tadalafil [having d(0.9) value in range of 10-30 microns] lowers effective surface available for dissolution and it may possess formulation challenges for development of Tadalafil solid dosage form.

Keywords: Micronization, PDE 5 Inhibitor, Tadalafil, Dissolution, Solid dosage form.