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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

Differential scanning calorimetric thermograms of oxatomide (1), β-cyclodextrin (2), physical mixture (3), kneaded mixture (4), coevaporated (5), freeze-dried (6), and spray-dried (7) inclusion complexes of equimolar ratio of oxatomide and β-cyclodextrin.
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fig3: Differential scanning calorimetric thermograms of oxatomide (1), β-cyclodextrin (2), physical mixture (3), kneaded mixture (4), coevaporated (5), freeze-dried (6), and spray-dried (7) inclusion complexes of equimolar ratio of oxatomide and β-cyclodextrin.

Mentions: The thermal behavior of oxatomide β-cyclodextrin inclusion complexes was studied using DSC to confirm the formation of the solid complexes. When guest molecules are incorporated in the cyclodextrin cavity or in the crystal lattice, their melting, boiling, and sublimation points usually shift to a different temperature or disappear within the temperature range at which the cyclodextrin lattice is decomposed [19]. The DSC curves for all the complexes are represented in Figure 3. The DSC thermogram of oxatomide exhibited one endothermic peak at 159.95°C. The DSC thermogram of β-cyclodextrin shows a very broad endothermic peak around 95°C corresponding to the release of water molecules. The thermogram of the physical mixture showed the melting endothermic peak characteristic of pure oxatomide and the broad peak corresponding to the dehydration of β-CD as if this thermogram was the superposition of those components, indicating the absence of interaction between oxatomide and β-cyclodextrin in such mixture.


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

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

Differential scanning calorimetric thermograms of oxatomide (1), β-cyclodextrin (2), physical mixture (3), kneaded mixture (4), coevaporated (5), freeze-dried (6), and spray-dried (7) inclusion complexes of equimolar ratio of oxatomide and β-cyclodextrin.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig3: Differential scanning calorimetric thermograms of oxatomide (1), β-cyclodextrin (2), physical mixture (3), kneaded mixture (4), coevaporated (5), freeze-dried (6), and spray-dried (7) inclusion complexes of equimolar ratio of oxatomide and β-cyclodextrin.
Mentions: The thermal behavior of oxatomide β-cyclodextrin inclusion complexes was studied using DSC to confirm the formation of the solid complexes. When guest molecules are incorporated in the cyclodextrin cavity or in the crystal lattice, their melting, boiling, and sublimation points usually shift to a different temperature or disappear within the temperature range at which the cyclodextrin lattice is decomposed [19]. The DSC curves for all the complexes are represented in Figure 3. The DSC thermogram of oxatomide exhibited one endothermic peak at 159.95°C. The DSC thermogram of β-cyclodextrin shows a very broad endothermic peak around 95°C corresponding to the release of water molecules. The thermogram of the physical mixture showed the melting endothermic peak characteristic of pure oxatomide and the broad peak corresponding to the dehydration of β-CD as if this thermogram was the superposition of those components, indicating the absence of interaction between oxatomide and β-cyclodextrin in such mixture.

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