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In Vitro and In Vivo Evaluation of Oxatomide β -Cyclodextrin Inclusion Complex.

Hashem FM, Mostafa M, Shaker M, Nasr M - J Pharm (Cairo) (2012)

Bottom Line: The coevaporated complex prepared in presence of PVP-K15 showed a prompt drug release and significantly increased % dissolution efficiency (P < 0.05) compared to the pure oxatomide.Moreover, the results of bioavailability evaluation of this complex in rabbits compared to commercial drug product indicated a 73.15% increase in the oral bioavailability of oxatomide.In conclusion, inclusion complex of oxatomide with β-cyclodextrin prepared by coevaporation in presence of PVP-K15 not only results in an enhancement of the oxatomide dissolution rate but also improves the bioavailability of oxatomide.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo 11790, Egypt.

ABSTRACT
The objective of this study was to evaluate the influence of oxatomide β-cyclodextrin inclusion complex on the physicochemical properties and bioavailability of the drug. Oxatomide β-cyclodextrin solid complex was prepared with equimolar ratio of both oxatomide and β-cyclodextrin in presence or absence of water soluble polymers using different techniques. The coevaporated complex prepared in presence of PVP-K15 showed a prompt drug release and significantly increased % dissolution efficiency (P < 0.05) compared to the pure oxatomide. Moreover, the results of bioavailability evaluation of this complex in rabbits compared to commercial drug product indicated a 73.15% increase in the oral bioavailability of oxatomide. In conclusion, inclusion complex of oxatomide with β-cyclodextrin prepared by coevaporation in presence of PVP-K15 not only results in an enhancement of the oxatomide dissolution rate but also improves the bioavailability of oxatomide.

No MeSH data available.


Related in: MedlinePlus

Phase solubility diagrams of oxatomide in different concentrations of β-cyclodextrin in distilled water and in presence of 0.1% HPMC, 0.25% PVP-K15. Each point represents the mean of measurements from three samples.
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fig1: Phase solubility diagrams of oxatomide in different concentrations of β-cyclodextrin in distilled water and in presence of 0.1% HPMC, 0.25% PVP-K15. Each point represents the mean of measurements from three samples.

Mentions: The phase solubility studies for oxatomide with β-cyclodextrin were carried out according to the method described by Higuchi and Connors [18]. The phase solubility diagrams of oxatomide in different concentration of β-cyclodextrin in distilled water, 0.1% HPMC solution, and 0.25% PVP solution are presented in Figure 1. The phase solubility profile of oxatomide β-cyclodextrin complex showed a typical Bs-type solubility curve, where the initial ascending portion is followed by a plateau region and then a decrease in total oxatomide solubility accompanied by precipitation of a microcrystalline complex [18].


In Vitro and In Vivo Evaluation of Oxatomide β -Cyclodextrin Inclusion Complex.

Hashem FM, Mostafa M, Shaker M, Nasr M - J Pharm (Cairo) (2012)

Phase solubility diagrams of oxatomide in different concentrations of β-cyclodextrin in distilled water and in presence of 0.1% HPMC, 0.25% PVP-K15. Each point represents the mean of measurements from three samples.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595936&req=5

fig1: Phase solubility diagrams of oxatomide in different concentrations of β-cyclodextrin in distilled water and in presence of 0.1% HPMC, 0.25% PVP-K15. Each point represents the mean of measurements from three samples.
Mentions: The phase solubility studies for oxatomide with β-cyclodextrin were carried out according to the method described by Higuchi and Connors [18]. The phase solubility diagrams of oxatomide in different concentration of β-cyclodextrin in distilled water, 0.1% HPMC solution, and 0.25% PVP solution are presented in Figure 1. The phase solubility profile of oxatomide β-cyclodextrin complex showed a typical Bs-type solubility curve, where the initial ascending portion is followed by a plateau region and then a decrease in total oxatomide solubility accompanied by precipitation of a microcrystalline complex [18].

Bottom Line: The coevaporated complex prepared in presence of PVP-K15 showed a prompt drug release and significantly increased % dissolution efficiency (P < 0.05) compared to the pure oxatomide.Moreover, the results of bioavailability evaluation of this complex in rabbits compared to commercial drug product indicated a 73.15% increase in the oral bioavailability of oxatomide.In conclusion, inclusion complex of oxatomide with β-cyclodextrin prepared by coevaporation in presence of PVP-K15 not only results in an enhancement of the oxatomide dissolution rate but also improves the bioavailability of oxatomide.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo 11790, Egypt.

ABSTRACT
The objective of this study was to evaluate the influence of oxatomide β-cyclodextrin inclusion complex on the physicochemical properties and bioavailability of the drug. Oxatomide β-cyclodextrin solid complex was prepared with equimolar ratio of both oxatomide and β-cyclodextrin in presence or absence of water soluble polymers using different techniques. The coevaporated complex prepared in presence of PVP-K15 showed a prompt drug release and significantly increased % dissolution efficiency (P < 0.05) compared to the pure oxatomide. Moreover, the results of bioavailability evaluation of this complex in rabbits compared to commercial drug product indicated a 73.15% increase in the oral bioavailability of oxatomide. In conclusion, inclusion complex of oxatomide with β-cyclodextrin prepared by coevaporation in presence of PVP-K15 not only results in an enhancement of the oxatomide dissolution rate but also improves the bioavailability of oxatomide.

No MeSH data available.


Related in: MedlinePlus