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. 2013:2013:109837.
doi: 10.1155/2013/109837. Epub 2012 Sep 19.

Preparation and Comparative Bioavailability Studies of Indomethacin-Loaded Cetyl Alcohol Microspheres

N Vishal Gupta  1 , D V Gowda  1 , V Balamuralidhara  1 , M S Khan  1
Affiliations

Preparation and Comparative Bioavailability Studies of Indomethacin-Loaded Cetyl Alcohol Microspheres

N Vishal Gupta et al. J Pharm (Cairo). 2013.

Abstract

The purpose of the present study was to compare the in vitro release and to find out whether the bioavailability of a 75 mg indomethacin capsule (Microcid SR) was equivalent to optimized formulation (indomethacin-loaded cetyl alcohol microspheres). Indomethacin-loaded cetyl alcohol microspheres were prepared by meltable emulsified cooling-induced technique. Surface morphology of microspheres has been evaluated using scanning electron microscopy. A single dose, randomized, complete cross over study of IM microspheres was carried out on 10 healthy male and female Albino sheep's under fasting conditions. The plasma was separated and the concentrations of the drug were determined by HPLC-UV method. Plasma indomethacin concentrations and other pharmacokinetic parameters obtained were statistically analyzed. The SEM images revealed the spherical shape of fat microspheres, and more than 98.0% of the isolated microspheres were in the size range 12-32 μm. DSC, FTIR spectroscopy and stability studies indicated that the drug after encapsulation with fat microspheres was stable and compatible. Both formulations were found to be bioequivalent as evidenced by in vivo studies. Based on this study, it can be concluded that cetyl alcohol microspheres and Microcid SR capsule are bioequivalent in terms of the rate and extent of absorption.

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Figures

Figure 1
Figure 1
SEM photograph of cetyl alcohol microspheres loaded with IM-formulation F3.
Figure 2
Figure 2
DSC thermograms of cetyl alcohol, pure indomethacin and indomethacin-loaded cetyl alcohol microspheres, peak a: cetyl alcohol, peak b: indomethacin, peak c: indomethacin-loaded cetyl alcohol microspheres (F3).
Figure 3
Figure 3
FTIR spectra of cetyl alcohol (peak a), indomethacin (peak b), and indomethacin-loaded cetyl alcohol microspheres (peak c:F3).
Figure 4
Figure 4
Drug release profile of indomethacin from microspheres and Microcid SR.
Figure 5
Figure 5
Mean plasma concentrations:time profiles of indomethacin from Microcid SR and formulation F3.
See this image and copyright information in PMC

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