Chemical & Pharmaceutical Bulletin 2012-01-01

Improved supersaturation and oral absorption of dutasteride by amorphous solid dispersions.

In-Hwan Beak, Min-Soo Kim

Index: Chem. Pharm. Bull. 60(11) , 1468-73, (2012)

Full Text: HTML

Abstract

In this study, amorphous solid dispersions containing dutasteride and various excipients, manufactured by spray-drying processes, were characterized to determine the effects on their ability to form supersaturated solutions and to identify the effects of supersaturation on increasing the bioavailability of dutasteride. The excipients included Eudragit E, hydroxypropyl-β-cyclodextrin (HP-β-CD), hydroxypropyl cellulose (HPC), hydroxypropylmethyl cellulose (HPMC), and polyvinylpyrrolidone (PVP K30). A solid dispersion with Eudragit E displayed a high maximum supersaturation with extended supersaturation, compared with a water-soluble polymer. The maximum concentration and the degree of supersaturation increased in the following order: PVP K30