DESIGN AND EVALUATION OF SOLID DISPERSED TADALAFIL TABLETSAbstract
Tadalafil (TD), a PDE-5 inhibitor, belongs to BCS class II. It is poorly soluble in water and requires enhancement in solubility and dissolution rate for increasing its oral bioavailability. In the present investigation, solid dispersed systems of tadalafil with poloxamer188 and sodium starch glycolate were prepared using solvent evaporation technique. The dissolution rate of the drug and poloxamer188 based solid dispersion was significantly higher than the sodium starch glycolate (SSG) based preparations and pure drug which reaches closer to the dissolution profile of marketed product. This was due to an increase in surface area of drug available for dissolution. Characterization of binary systems with FTIR 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/poloxamer188 showed rapid dissolution of tadalafil (DE30 56.68 %). In the binary systems, tested (1:0.5) proportion of tadalafil/poloxamer188 showed rapid dissolution of tadalafil. In contrast, higher proportion of polaxmer188 (1:1) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characters of the polymer at its higher concentration, which might have retard the release rate of tadalafil. The tablets were prepared for the optimized formula of solid dispersion, by wet granulation technique. The solid dispersion tablets were evaluated and compared with tadalafil marketed product.
T. Vani Prasanna*, B. Nisha Rani , A. Sambasiva Rao and T.E.G.K. Murthy
Department of Pharmaceutics, Sri Indu Institute of Pharmacy, Sheriguda, R.R. District, Andhra Pradesh, India
06 August, 2012
30 September, 2012
24 November, 2012
01 December, 2012