biopharmaceutics classification system (BCS);
Caco-2;
cells;
dissolution;
permeation;
in vitro/in vivo correlations (IVIVC);
food-effect-studies;
WATER-SOLUBLE DRUGS;
FOOD;
PERMEATION;
PREDICTION;
MICRONIZATION;
FORMULATIONS;
ENHANCEMENT;
SOLUBILITY;
DELIVERY;
HUMANS;
D O I:
10.1002/jps.21576
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
The usefulness of a dissolution/permeation (D/P) system to predict the in vivo performance of solid dosage forms containing the poorly Soluble drug, fenofibrate, was studied. Biorelevant dissolution media simulating the fasted and fed state conditions of the human gastrointestinal tract were used in order to simulate the effect of food on the absorption of fenofibrate. Moreover, the results obtained from the D/P system were correlated with pharmacokinetic parameters obtained following in. vivo studies in rats. The in vitro parameter (amount permeated in the D/P system) reflected well the in vivo performance in rats in terms of AUC and C-max of fenofibric acid. This study thus demonstrates the potential of the D/P system as valuable tool for absorption screening of dosage forms for poorly soluble drugs. (C) 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:2001-2009, 2009
机构:
Jimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Jimma Univ, Sch Pharm, POB 378, Jimma, Ethiopia
Univ Ghent, Fac Pharmaceut Sci, Drug Qual & Registrat DruQuaR Grp, Ottergemsesteenweg 460, B-9000 Ghent, BelgiumJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Belew, Sileshi
Suleman, Sultan
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机构:
Jimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Jimma Univ, Sch Pharm, POB 378, Jimma, EthiopiaJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Suleman, Sultan
Duguma, Markos
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机构:
Jimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Jimma Univ, Sch Pharm, POB 378, Jimma, EthiopiaJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Duguma, Markos
Teshome, Henok
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机构:
Jimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Jimma Univ, Sch Pharm, POB 378, Jimma, EthiopiaJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Teshome, Henok
Wynendaele, Evelien
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h-index: 0
机构:
Univ Ghent, Fac Pharmaceut Sci, Drug Qual & Registrat DruQuaR Grp, Ottergemsesteenweg 460, B-9000 Ghent, BelgiumJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Wynendaele, Evelien
Duchateau, Luc
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机构:
Univ Ghent, Fac Vet Med, Biometr Res Grp, Salisburylaan 133, B-9820 Merelbeke, BelgiumJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
Duchateau, Luc
De Spiegeleer, Bart
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h-index: 0
机构:
Univ Ghent, Fac Pharmaceut Sci, Drug Qual & Registrat DruQuaR Grp, Ottergemsesteenweg 460, B-9000 Ghent, BelgiumJimma Univ, Lab Drug Qual JuLaDQ, POB 378, Jimma, Ethiopia
机构:
AstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, EnglandAstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, England
Pepin, Xavier J. H.
Flanagan, Talia R.
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机构:
AstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, EnglandAstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, England
Flanagan, Talia R.
Holt, David J.
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机构:
AstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, EnglandAstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, England
Holt, David J.
Eidelman, Anna
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h-index: 0
机构:
Ardea Biosci, Pharmaceut Sci, 9390 Towne Ctr Dr, San Diego, CA 92121 USAAstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, England
Eidelman, Anna
Treacy, Don
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h-index: 0
机构:
Ardea Biosci, Pharmaceut Sci, 9390 Towne Ctr Dr, San Diego, CA 92121 USAAstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, England
Treacy, Don
Rowlings, Colin E.
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h-index: 0
机构:
Ardea Biosci, Pharmaceut Sci, 9390 Towne Ctr Dr, San Diego, CA 92121 USAAstraZeneca, Global Med Dev, Pharmaceut Dev, Silk Rd Business Pk,Charter Way, Macclesfield SK10 2NA, Cheshire, England