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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

Infrared spectra 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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fig2: Infrared spectra 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: IR spectra of oxatomide and its inclusion complexes with β-cyclodextrin prepared by different methods are presented in Figure 2. Oxatomide is characterized by the absorption of the carbonyl (C=O) group at 1702 cm−1; in the spectra of the inclusion complex, this band was shifted towards higher frequencies at 1727 cm−1 in case of coevaporated solid complex and to lower frequencies at 1682 cm−1 in spray-dried solid complex and decreased in intensity in freeze-dried complex. The absorption of N–H group in oxatomide at 3172 cm−1 was shifted toward lower frequencies at 2936–2924 cm−1 in all types of solid complexes. As spectral changes always concern C–OH, –CH2, and CH groups of the β-CD, it should be suggested that the host-guest interactions are dominated by hydrogen bonds among the above-mentioned groups.


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

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

Infrared spectra 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

fig2: Infrared spectra 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: IR spectra of oxatomide and its inclusion complexes with β-cyclodextrin prepared by different methods are presented in Figure 2. Oxatomide is characterized by the absorption of the carbonyl (C=O) group at 1702 cm−1; in the spectra of the inclusion complex, this band was shifted towards higher frequencies at 1727 cm−1 in case of coevaporated solid complex and to lower frequencies at 1682 cm−1 in spray-dried solid complex and decreased in intensity in freeze-dried complex. The absorption of N–H group in oxatomide at 3172 cm−1 was shifted toward lower frequencies at 2936–2924 cm−1 in all types of solid complexes. As spectral changes always concern C–OH, –CH2, and CH groups of the β-CD, it should be suggested that the host-guest interactions are dominated by hydrogen bonds among the above-mentioned groups.

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