Development and characterization of bicalutamide-poloxamer F68 solid dispersion systems.
The objective of the present work was to improve the dissolution rate of a poorly water-soluble drug, bicalutamide, by a solid dispersion technique. The solid dispersion systems of bicalutamide were prepared with poloxamer F68 in 1:1, 1:3, and 1:5 ratios using the melting method. The interaction of drug with polymer was evaluated by TLC, FTIR, and powder XRD. The results of powder XRD showed a significant decrease in the crystallinity of drug in the binary systems of bicalutamide. All binary systems of bicalutamide showed faster dissolution than pure drug alone (p < 0.001). However, among all binary systems studied, 1:1 proportion of bicalutamide : poloxamer was found to be excellent for dissolution enhancement (DP30: 99.98% +/- 3.9) of bicalutamide. The higher ratios of poloxamer F68 (1:3 and 1:5) had retarded the release of drug from their corresponding binary systems which might be due to its gelling property in higher concentration.
Sancheti
P P
PP
Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, India.
Vyas
V M
VM
Shah
M
M
Karekar
P
P
Pore
Y V
YV
D000813:Anilides / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D002855:Chromatography, Thin Layer; D005079:Excipients; D007700:Kinetics; D009570:Nitriles / Q000737:chemistry*; D020442:Poloxamer / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014105:Tosyl Compounds / Q000737:chemistry*; D014961:X-Ray Diffraction
D000813:Anilides; D005079:Excipients; D009570:Nitriles; D014105:Tosyl Compounds; D020442:Poloxamer; C053541:bicalutamide