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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

Mean plasma concentrations:time profiles of indomethacin from Microcid SR and formulation F3.
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Related In: Results  -  Collection


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fig5: Mean plasma concentrations:time profiles of indomethacin from Microcid SR and formulation F3.

Mentions: The mean plasma concentration as a function of time is shown in Figure 5 and the calculated pharmacokinetic parameters of Microcid SR and F3 formulations are given in Table 4. After oral administration of both products, more mean Cmax value was observed for Microcid SR 75 mg capsule (2134  ±  29.6 ng/mL) than formulation F3 (1989  ±  20.30 ng/mL). However, the difference in the Cmax values obtained for Microcid SR 75 mg capsule and formulation F3 was statistically insignificant. Mean plasma concentrations of IM for both products in all experimental conditions were within the therapeutic concentration range (300–3000 ng/mL) [9]. The Cmax values for both products do not exceed the above limit in all animals. It was observed the plasma concentration of IM falls below detection limit (50 ng/mL) after 24 h in all animals following administration of either product. On the basis of the therapeutic concentration range of IM, it could be concluded that the therapeutic effects of both formulations would be probably be maintained for about 12 h following a single dose administration. Thus it could be predicted that the two controlled release formulations included in this study are associated with a similar onset of therapeutic response following a single dose administration under fasting conditions. Furthermore, it could be predicted that both controlled release formulations in this study are associated with a similar onset of therapeutic response, following a single dose administration under fasting conditions.


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

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

Mean plasma concentrations:time profiles of indomethacin from Microcid SR and formulation F3.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig5: Mean plasma concentrations:time profiles of indomethacin from Microcid SR and formulation F3.
Mentions: The mean plasma concentration as a function of time is shown in Figure 5 and the calculated pharmacokinetic parameters of Microcid SR and F3 formulations are given in Table 4. After oral administration of both products, more mean Cmax value was observed for Microcid SR 75 mg capsule (2134  ±  29.6 ng/mL) than formulation F3 (1989  ±  20.30 ng/mL). However, the difference in the Cmax values obtained for Microcid SR 75 mg capsule and formulation F3 was statistically insignificant. Mean plasma concentrations of IM for both products in all experimental conditions were within the therapeutic concentration range (300–3000 ng/mL) [9]. The Cmax values for both products do not exceed the above limit in all animals. It was observed the plasma concentration of IM falls below detection limit (50 ng/mL) after 24 h in all animals following administration of either product. On the basis of the therapeutic concentration range of IM, it could be concluded that the therapeutic effects of both formulations would be probably be maintained for about 12 h following a single dose administration. Thus it could be predicted that the two controlled release formulations included in this study are associated with a similar onset of therapeutic response following a single dose administration under fasting conditions. Furthermore, it could be predicted that both controlled release formulations in this study are associated with a similar onset of therapeutic response, following a single dose administration under fasting conditions.

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