Computer simulations for bioequivalence trials: Selection of analyte in BCS drugs with first-pass metabolism and two metabolic pathways

European Journal of Pharmaceutical Sciences

Volumn 41, Issue 5, 2010, Pages 716-728

  Navarro Fontestad, Carmen ^a   Gonzalez Alvarez, Isabel ^b   Fernández Teruel, Carlos ^c   Garcia Arieta, Alfredo ^d   Bermejo, Marival ^b   Casabó, Vicente G ^a  

^a UNIVERSITY OF VALENCIA   (Spain)

^b MIGUEL HERNÁNDEZ UNIVERSITY   (Spain)

^c PHARMAMAR S A   (Spain)

^d Department of Human Use Medicines   (Spain)

Author keywords

Analyte; BCS; Bioequivalence; First pass metabolism; Sensitivity; Simulation

Indexed keywords

HERBACEOUS AGENT;

AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; COMPUTER SIMULATION; DRUG FORMULATION; DRUG PENETRATION; DRUG QUALITY; DRUG SOLUBILITY; FIRST PASS EFFECT; PRIORITY JOURNAL; SENSITIVITY ANALYSIS; SYSTEM ANALYSIS;

ALGORITHMS; AREA UNDER CURVE; BIOPHARMACEUTICS; COMPUTER SIMULATION; METABOLIC NETWORKS AND PATHWAYS; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; THERAPEUTIC EQUIVALENCY;

EID: 78349312941     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2010.09.017     Document Type: Article

References (17)

1. Blume H.H., Schug B.S. The biopharmaceutics classification system (BCS): class III drugs-better candidates for BA/BE waiver?. Eur. J. Pharm. Sci. 1999, 9:117-121.
2. Chen M.L., Jackson A.J. The role of metabolites in bioequivalency assessment. I. Linear pharmacokinetics without first-pass effect. Pharm. Res. 1991, 8:25-32.
3. Chen M.L., Jackson A.J. The role of metabolites in bioequivalency assessment. II. Drugs with linear pharmacokinetics and first-pass effect. Pharm. Res. 1995, 12:700-708.
4. el-Tahtawy A.A., Jackson A.J., Ludden T.M. Evaluation of bioequivalence of highly variable drugs using Monte Carlo simulations. I. Estimation of rate of absorption for single and multiple dose trials using Cmax. Pharm. Res. 1995, 12:1634-1641.
5. el-Tahtawy A.A., Tozer T.N., Harrison F., Lesko L., Williams R. Evaluation of bioequivalence of highly variable drugs using clinical trial simulations. II. Comparison of single and multiple-dose trials using AUC and Cmax. Pharm. Res. 1998, 15:98-104.
6. EMA Guideline on the Investigation of Bioequivalence 2010, Committee for Medicinal Products for Human Use (CHMP).
7. EMEA Note for Guidance on Modified Release Oral and Transdermal Dosage Forms: Section II 1999, Committee for Proprietary Medicinal Products (CPMP).
8. EMEA Points to Consider on the Clinical Requirements of Modified Release Products Submitted as a Line Extension of an Existing Marketing Authorisation 2003, Committee for Proprietary Medicinal Products (CPMP).
9. FDA Guidance for Industry. Bioavailability and Bioequivalence Studies for Orally Administered Drug Products-General Considerations 2003, Center for Drug Evaluation and Research (CDER).
10. Fernandez-Teruel C., Gonzalez-Alvarez I., Navarro-Fontestad C., Garcia-Arieta A., Bermejo M., Casabo V.G. Computer simulations of bioequivalence trials: selection of design and analyte in BCS drugs with first-pass hepatic metabolism. Part II. Non-linear kinetics. Eur. J. Pharm. Sci. 2009, 36:147-156.
11. Fernandez-Teruel C., Nalda Molina R., Gonzalez-Alvarez I., Navarro-Fontestad C., Garcia-Arieta A., Casabo V.G., Bermejo M. Computer simulations of bioequivalence trials: selection of design and analyte in BCS drugs with first-pass hepatic metabolism: linear kinetics (I). Eur. J. Pharm. Sci. 2009, 36:137-146.
12. Jackson A.J. Prediction of steady-state bioequivalence relationships using single dose data I-linear kinetics. Biopharm. Drug Dispos. 1987, 8:483-496.
13. Jackson A.J. Prediction of steady state bioequivalence relationships using single dose data II-nonlinear kinetics. Biopharm. Drug Dispos. 1989, 10:489-503.
14. Jackson A.J. The role of metabolites in bioequivalency assessment. III. Highly variable drugs with linear kinetics and first-pass effect. Pharm. Res. 2000, 17:1432-1436.
15. Rosenbaum S.E. Effects of variability in hepatic clearance on the bioequivalence parameters of a drug and its metabolite: simulations using a pharmacostatistical model. Pharm. Acta Helv. 1998, 73:135-144.
16. Tucker G.T., Rostami-Hodjegan A., Jackson P.R. Bioequivalence-a measure of therapeutic equivalence?. Bio-International: Bioavailability, Bioequivalence and Pharmacokinetics: International Conference of FIP Bio-International 92 1993, 35-46. Medpharm, Stuttgart. K.K. Midha, H.H. Blume (Eds.).
17. Tucker G.T., Rostami-Hodjegan A., Jackson P.R. Metabolite measurement in bioequivalence studies: theoretical considerations. Bio-International: Bioavailability, Bioequivalence and Pharmacokinetics: International Conference of FIP Bio-International 92 1993, 163-170. Medpharm, Stuttgart. K.K. Midha, H.H. Blume (Eds.).