Analysis of nifedipine absorption from soft gelatin capsules using PBPK modeling and biorelevant dissolution testing

Journal of Pharmaceutical Sciences

Volumn 99, Issue 6, 2010, Pages 2899-2904

  Thelen, Kirstin ^a   Jantratid, Ekarat ^a   Dressman, Jennifer B ^a   Lippert, Jörg ^b   Willmann, Stefan ^b  

^a GOETHE UNIVERSITY   (Germany)

^b BAYER AG   (Germany)

Author keywords

Absorption; Biorelevant media; Computational ADME; Dissolution; Nifedipine; PBPK modeling; Pharmacokinetics; PK sim; Precipitation; Solubility

Indexed keywords

GELATIN; NIFEDIPINE;

ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG SOLUBILITY; HUMAN; NORMAL HUMAN;

EID: 77951597966     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22026     Document Type: Article

References (32)

1. Schmitt W, Willmann S. 2005. Physiology-based pharmacokinetic modelling: Ready to be used. Drug Discov Today 2:125-132. (Pubitemid 40186349)
2. Willmann S, Lippert J, Sevestre M, Solodenko J, Fois F, Schmitt W. 2003. PK-Sim: A physiologically based pharmacokinetic 'whole-body' model. BIOSILICO 1:121-124.
3. Willmann S, Schmitt W, Keldenich J, Lippert J, Dressman JB. 2004. A physiological model for the estimation of the fraction dose absorbed in humans. J Med Chem 47:4022-4031. (Pubitemid 38970963)
4. Willmann S, Lippert J, Schmitt W. 2005. From physicochemistry to absorption and distribution: Predictive mechanistic modelling and computational tools. Expert Opin Drug Metab Toxicol 1:159-168.
5. Dressman JB, Amidon GL, Reppas C, Shah VP. 1998. Dissolution testing as a prognostic tool for oral drug absorption: Immediate release dosage forms. Pharm Res 15:11-22. (Pubitemid 28080861)
6. Vertzoni M, Dressman JB, Butler J, Hempenstall JM, Reppas C. 2005. Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds. Eur J Pharm Biopharm 60:413-417. (Pubitemid 40922839)
7. Bayer Vital GmbH. Fachinformation Adalat 5, 10 Kapseln, 2004. Rote Liste Service GmbH, 2006.
8. Bossert F, Vater W. 1971. Dihydropyridines, a new group of strongly effective coronary therapeutic agents. Naturwissenschaften 58:578.
9. Sorkin E, Clissold S, Brogden R. 1985. Nifedipine - A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in ischaemic heart disease, hypertension and related cardiovascular disorders. Drugs 30:182-274. (Pubitemid 15006051)
10. Bayer Schering Pharma AG. 2007. Adalat Homepage. www.adalat.com (accessed March 4, 2009).
11. Toal C. 2004. Formulation dependent pharmacokinetics - Does the dosage form matter for nifedipine? J Cardiovasc Pharmacol 44:82-86.
12. Amidon GL, Lennernas H, Shah VP, Crison JR. 1995. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12:413-420.
13. Food and Drug Administration. 2000. Guidance for Industry: Waiver of In vivo bioavailability and bioequivalence studies for immediate-release solid dosage forms based on a biopharmaceutics classification system. Rockville MD, USA: U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research.
14. Bode H, Brendel E, Ahr G, Fuhr U, Harder S, Staib A. 1996. Investigation of nifedipine absorption in different regions of the human gastrointestinal (GI) tract after simultaneous administration of 13C- and 12C-nifedipine. Eur J Clin Pharmacol 50:447-451. (Pubitemid 26163582)
15. Foster T, Hamann S, Richards V, Bryant P, Graves D, McAllister R. 1983. Nifedipine kinetics and bioavailability after single intravenous and oral doses in normal subjects. J Clin Pharmacol 23:161-170. (Pubitemid 13131441)
16. Guengerich F, Martin M, Beaune P, Kremers P, Wolff T, Waxman D. 1986. Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. J Biol Chem 261:5051-5060. (Pubitemid 17204301)
17. Guengerich F, Brian W, Iwasaki M, Sari M, Bäärnhielm C, Berntsson P. 1991. Oxidation of dihydropyridine calcium channel blockers and analogues by human liver cytochrome P-450 IIIA4. J Med Chem 34:1838-1844.
18. Raemsch K, Sommer J. 1983. Pharmacokinetics and metabolism of nifedipine. Hypertension 5:18-24.
19. Klein S, Dressman JB. 2006. The mini paddle apparatus - A useful tool in the early developmental stage? Experiences with immediate-release dosage forms. 33rd Annual Meeting and Exposition of the Controlled Release Society. Vienna, Austria.
20. Klein S, Shah VP. 2008. A standardized mini paddle apparatus as an alternative to the standard paddle. AAPS PharmSciTech 9:1179-1184.
21. Lydon A, Murray C, McGinley J, Plant R, Duggan F, Shorten G. 1999. Cisapride does not alter gastric volume or pH in patients undergoing ambulatory surgery. Can J Anaesth 46:1181-1184. (Pubitemid 30038721)
22. Maltby JR, Sutherland AD, Sale JP, Shaffer EA. 1986. Preoperative oral fluids: Is a five-hour fast justified prior to elective surgery? Anesth Analg 65:1112-1116.
23. Willmann S, Schmitt W, Keldenich J, Dressman JB. 2003. A physiologic model for simulating gastrointestinal flow and drug absorption in rats. Pharm Res 20:1766-1771. (Pubitemid 37449449)
24. Odou P, Ferrari N, Barthelemy C, Brique S, Lhermitte M, Vincent A, Libersa C, Robert H. 2005. Grapefruit juice-nifedipine interaction: Possible involvement of several mechanisms. J Clin Pharm Ther 30:153-158. (Pubitemid 41583610)
25. MedicinesComplete. 2006. Nifedipine: Clarke's analysis of drugs and poisons, http://www.medicinescomplete.com/mc/ (accessed July 17, 2007).
26. Kelly J, O'Malley K. 1992. Clinical pharmacokinetics of calcium antagonists - An update. Clin Pharmacokinet 22:416-433.
27. Valentin J. 2002. Annals of the ICRP-Basic anatomical and physiological data for use in radiological protection: Reference values. Oxford, UK: Pergamon. (Pubitemid 36637061)
28. Galetin A, Houston J. 2006. Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: Impact on prediction of first-pass metabolism. J Pharmacol Exp Ther 318:1220-1229. (Pubitemid 44268329)
29. Paine MF, Khalighi M, Fisher JM, Shen DD, Kunze KL, Marsh CL, Perkins JD, Thummel KE. 1997. Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 283:1552-1562. (Pubitemid 28016533)
30. Zhang Q, Kaminsky L, Dunbar D, Zhang J, Ding X. 2007. Role of small intestinal cytochromes P450 in the bioavailability of oral nifedipine. Drug Metab Dispos 35:1617-1623. (Pubitemid 47296056)
31. Banzet O, Colin J, Thibonnier M, Singlas E, Alexandre J, Corvol P. 1983. Acute antihypertensive effect and pharmacokinetics of a tablet preparation of nifedipine. Eur J Clin Pharmacol 24:145-150. (Pubitemid 13147702)
32. Taburet A, Singlas E, Colin J, Banzet O, Thibonnier M, Corvol P. 1983. Pharmacokinetic studies of nifedipine tablet - Correlation with antihypertensive effects. Hypertension 5:29-33. (Pubitemid 13026550)