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

Gupta NV, Gowda DV, Balamuralidhara V, Khan MS - J Pharm (Cairo) (2012)

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Sri Shivarathreeshwara Nagar, Karnataka, Mysore 570015, India.

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.

No MeSH data available.


Related in: MedlinePlus

Drug release profile of indomethacin from microspheres and Microcid SR.
© Copyright Policy - open-access
Related In: Results  -  Collection


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fig4: Drug release profile of indomethacin from microspheres and Microcid SR.

Mentions: From the release studies depicted in Figure 4, it was observed that there is no significant release of drug at gastric pH from fat microspheres. At the end of 8th h, in vitro drug release from F3 (96.32%) was slower than Microcid SR (98.98%) in the intestinal environment. Drug was released in a biphasic manner consisting of initial fast release followed by a slow release in intestinal pH from the CA microspheres [2, 10, 12, 18]. The decreased in vitro drug release from CA microspheres might be due to more hydrophobicity and influence of molecular weight of CA. In vitro drug release was considerably retarded from the CA microspheres when compared to Microcid SR. The rate of drug release followed first order release kinetics and numerical data fitted into Peppas model showed that the mechanism of drug release from CA microspheres was fickian diffusion (F1-0,412, F2-0.415, F3-0.398, F4-0.421, F5-0.431, and Microcid SR-0.476). After an initial burst effect, the subsequent release of drug from microspheres was slow.


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

Gupta NV, Gowda DV, Balamuralidhara V, Khan MS - J Pharm (Cairo) (2012)

Drug release profile of indomethacin from microspheres and Microcid SR.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595941&req=5

fig4: Drug release profile of indomethacin from microspheres and Microcid SR.
Mentions: From the release studies depicted in Figure 4, it was observed that there is no significant release of drug at gastric pH from fat microspheres. At the end of 8th h, in vitro drug release from F3 (96.32%) was slower than Microcid SR (98.98%) in the intestinal environment. Drug was released in a biphasic manner consisting of initial fast release followed by a slow release in intestinal pH from the CA microspheres [2, 10, 12, 18]. The decreased in vitro drug release from CA microspheres might be due to more hydrophobicity and influence of molecular weight of CA. In vitro drug release was considerably retarded from the CA microspheres when compared to Microcid SR. The rate of drug release followed first order release kinetics and numerical data fitted into Peppas model showed that the mechanism of drug release from CA microspheres was fickian diffusion (F1-0,412, F2-0.415, F3-0.398, F4-0.421, F5-0.431, and Microcid SR-0.476). After an initial burst effect, the subsequent release of drug from microspheres was slow.

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Sri Shivarathreeshwara Nagar, Karnataka, Mysore 570015, India.

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.

No MeSH data available.


Related in: MedlinePlus