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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

Dissolution profiles of spray dried (a), coevaporated (b), and freeze-dried (c) oxatomide β cyclodextrin inclusion complexes prepared in with or without water soluble polymer in distilled water (pH 6.8).
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Related In: Results  -  Collection


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fig6: Dissolution profiles of spray dried (a), coevaporated (b), and freeze-dried (c) oxatomide β cyclodextrin inclusion complexes prepared in with or without water soluble polymer in distilled water (pH 6.8).

Mentions: Regarding Q5, the inclusion complexes prepared by spray drying, freeze drying, and coevaporation (Figure 5) showed a prompt drug release compared to pure oxatomide (P < 0.05). The complex prepared by coevaporation in presence of PVP-K15 showed the highest release with Q5% and Q90% values of 98.33 ± 1.02% and 100%, respectively (Table 1 and Figure 6(b)). All inclusion complexes significantly increased the %DE5 min and %DE60 min (P < 0.05) compared to the pure drug (Table 1). Also, the complex prepared by coevaporation in presence of PVP-K15 showed the highest %DE. The increase in dissolution of drug in presence of both β-cyclodextrin and water soluble polymers may be attributed to both improvement of drug wettability and formation of readily soluble complexes in dissolution medium. When oxatomide β-cyclodextrin inclusion complexes come in contact with an aqueous dissolution medium, the hydrophilic carrier dissolves and results in precipitation of the embedded drug into fine particles, which increase the dissolution surface available [23].


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

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

Dissolution profiles of spray dried (a), coevaporated (b), and freeze-dried (c) oxatomide β cyclodextrin inclusion complexes prepared in with or without water soluble polymer in distilled water (pH 6.8).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig6: Dissolution profiles of spray dried (a), coevaporated (b), and freeze-dried (c) oxatomide β cyclodextrin inclusion complexes prepared in with or without water soluble polymer in distilled water (pH 6.8).
Mentions: Regarding Q5, the inclusion complexes prepared by spray drying, freeze drying, and coevaporation (Figure 5) showed a prompt drug release compared to pure oxatomide (P < 0.05). The complex prepared by coevaporation in presence of PVP-K15 showed the highest release with Q5% and Q90% values of 98.33 ± 1.02% and 100%, respectively (Table 1 and Figure 6(b)). All inclusion complexes significantly increased the %DE5 min and %DE60 min (P < 0.05) compared to the pure drug (Table 1). Also, the complex prepared by coevaporation in presence of PVP-K15 showed the highest %DE. The increase in dissolution of drug in presence of both β-cyclodextrin and water soluble polymers may be attributed to both improvement of drug wettability and formation of readily soluble complexes in dissolution medium. When oxatomide β-cyclodextrin inclusion complexes come in contact with an aqueous dissolution medium, the hydrophilic carrier dissolves and results in precipitation of the embedded drug into fine particles, which increase the dissolution surface available [23].

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