Preparation, evaluation and bioavailability studies of indomethacin-bees wax microspheres.
The present study envisages the preparation of microspheres containing indomethacin (IM) as model drug and bees wax as carrier, and to compare the in vitro release and pharmacokinetics of prepared IM formulation with commercially available oral formulation MicrocidSR. The microsphere formulations were prepared by meltable emulsified dispersion and cooling induced solidification. Surface morphology of microspheres has been evaluated using scanning electron microscopy (SEM). The SEM images revealed the spherical shape of microspheres and more than 98.0% of the isolated microspheres were in the size range 115-855 mum. Differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy studies indicated that the drug after encapsulation with bees wax was stable and compatible. A single dose randomized complete cross over study of IM (75 mg) microspheres was carried out on 8 healthy Albino sheeps. Plasma IM concentrations and other pharmacokinetic parameters obtained were statistically analyzed. The T (max), C (max), AUC(O-24) and T (1/2) values of MicrocidSR and optimized formulation were 3.0 h, 2038 +/- 51.31 ng/ml, 9528 +/- 129.65 ng/ml h(-1), and 2.59 +/- 0.02 h(-1); and 3.2 h, 1940 +/- 22.61 ng/ml, 8751 +/- 41.32 ng/ml h(-1), and 2.68 +/- 0.02 h(-1), respectively. Beeswax microspheres showed controlled release and it can be concluded that both the prepared formulation and MicrocidSR are bioequivalent.
Gowda
D V
DV
Department of Pharmaceutics, J.S.S College of Pharmacy, 570015 Mysore, India.
Ravi
Valluru
V
Shivakumar
H G
HG
Hatna
Siddaramaiah
S
D000284:Administration, Oral; D000818:Animals; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods; D004353:Drug Evaluation, Preclinical; D005260:Female; D007213:Indomethacin / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D008863:Microspheres; D012756:Sheep; D014885:Waxes / Q000737:chemistry*
D003692:Delayed-Action Preparations; D014885:Waxes; C038228:beeswax; D007213:Indomethacin