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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
pharmacology, toxicology and pharmaceutics
Evaluation of carboxymethyl-β-cyclodextrin with acid function: Improvement of chemical stability, oral bioavailability and bitter taste of famotidine
International Journal of Pharmaceutics, Volume 397, No. 1-2, Year 2010
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Description
The objective of the present study was to evaluate the potential influence of carboxymethyl-β-cyclodextrin (CM-β-CyD) on the aqueous solubility, chemical stability and oral bioavailability of famotidine (FMT) as well as on its bitter taste. We examined the effect of the CM-β-CyD on the acidic degradation of FMT compared with that for sulfobutyl-ether-β-cyclodextrin (SBE-β-CyD). The potential use of CM-β-CyD for orally disintegrating tablets (ODTs) was evaluated in vitro and in vivo. A taste perception study was also carried out. A strong stabilizing influence of CM-β-CyD was observed against the acidic degradation, in sharp contrast to SBE-β-CyD which induced a weird destabilizing effect on FMT. 13C NMR was used to investigate the interaction mode between FMT and the 2 CyDs. In vivo study of ODTs indicated a significant increase in Cmax, AUC and oral bioavailability in the case of FMT-CM-β-CyD tablets, compared with plain drug tablets. However, no significant difference in Tmax and t1/2 was observed. CM-β-CyD complexation appears to be an acceptable strategy for enhancing the oral bioavailability of FMT owing to its dramatic effect on the aqueous solubility and chemical stability of the drug. In addition, it has a pronounced effect on masking the bitter taste of FMT. © 2010 Elsevier B.V.
Authors & Co-Authors
Mady, Fatma Mohammed
Egypt, Minya
Faculty of Pharmacy
Japan, Kumamoto
Kumamoto University
Abou-Taleb, Ahmed E.
Egypt, Asyut
Faculty of Pharmacy
Khaled, Khaled Ali
Egypt, Minya
Faculty of Pharmacy
Yamasaki, Keishi
Japan, Kumamoto
Sojo University
Iohara, Daisuke
Japan, Kumamoto
Sojo University
Taguchi, Kazuaki
Japan, Kumamoto
Kumamoto University
Anraku, Makoto
Japan, Fukuyama
Fukuyama University
Hirayama, Fumitoshi
Japan, Kumamoto
Sojo University
Uekama, Kaneto
Japan, Kumamoto
Sojo University
Otagiri, Masaki
Japan, Kumamoto
Kumamoto University
Japan, Kumamoto
Sojo University
Statistics
Citations: 54
Authors: 10
Affiliations: 5
Identifiers
Doi:
10.1016/j.ijpharm.2010.06.018
ISSN:
03785173
Research Areas
Health System And Policy