Acta Pharm. 59 (2009) 453-461

full paper

Short communication

Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

VIKRANT VYAS, PANKAJKUMAR SANCHETI, POONAM KAREKAR, MANALI SHAH and YOGESH PORE

yogeshvpore@rediffmail.com

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra-415124, India

Accepted September 14, 2009

Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and powder XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE₃₀ 70.9 ± 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug from corresponding binary systems indicating altered rheological characteristics of the polymer, at its higher concentration, which might have retarded the release rate of tadalafil.

Keywords: tadalafil, solid dispersion, poloxamer 407, dissolution