In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers

被引:17
作者
Al-Behaisi, S
Antal, I
Morovján, G
Szúnyog, J
Drabant, S
Marton, S
Klebovich, I
机构
[1] EGIS Pharmaceut Ltd, Res & Dev Directorate, H-1106 Budapest, Hungary
[2] Semmelweis Univ, Inst Pharmaceut, H-1092 Budapest, Hungary
关键词
deramciclane; dissolution; food effect; AUC(cum); in vitro-in vivo correlation;
D O I
10.1016/S0928-0987(01)00195-6
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The in vitro dissolution profiles of deramciclane 30 mg film-coated tablets, an acid-labile new 5-HT receptor antagonist, were studied under simulated fasting and fed conditions. Artificial gastric juice with pH adjusted to that of fasting conditions was applied either alone or after adding different dietary components. The use of the USP dissolution apparatus 11 (paddle method) showed that the presence of dietary components has markedly affected the amount of unchanged drug dissolved. As a similar tendency bad been observed in food-effect studies in healthy volunteers, cumulative area under the curve (AUC(cum)) for both fed and fasting conditions were compared and an in vitro-in vivo correlation (IVIVC) was evaluated. A linear relationship was established between logarithmic in vivo blood sampling tune and in vitro dissolution time assigned to equal AUC(cum) ratios (AUC(cum), (fed)/AUC(cum), (fasting)). Despite its limitations. in vitro modelling of in vivo conditions might help provide a base for predicting in vivo drug behaviour. (C) 2002 Published by Elsevier Science B.V.
引用
收藏
页码:157 / 162
页数:6
相关论文
共 35 条
[1]   A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].
AMIDON, GL ;
LENNERNAS, H ;
SHAH, VP ;
CRISON, JR .
PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420
[2]  
BALOGHNEMES K, 2000, J PHARM PHARMACOL, V52, P47
[3]  
BERENYI E, 1990, Drugs of the Future, V15, P1174
[4]  
DRABANT S, 2000, INFLUENCE FOOD ORAL
[5]   In vitro-in vivo correlations for lipophilic, poorly water-soluble drugs [J].
Dressman, JB ;
Reppas, C .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2000, 11 :S73-S80
[6]   Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms [J].
Dressman, JB ;
Amidon, GL ;
Reppas, C ;
Shah, VP .
PHARMACEUTICAL RESEARCH, 1998, 15 (01) :11-22
[7]  
*FDA CDER, 1997, GUID IND EXT REL OR
[8]  
*FDA CDER, 1997, GUID IND FOOD EFF BI
[9]  
*FDA CDER, 1999, GUID IND WAIV IN VIV
[10]  
Fuchs WS, 1998, ARZNEIMITTEL-FORSCH, V48, P552