Analysis of risk factors in human bioequivalence study that incur bioinequivalence of oral drug products

Molecular Pharmaceutics

Volumn 6, Issue 1, 2009, Pages 48-59

  Yamashita, Shinji ^a   Tachiki, Hidehisa ^b  

^a SETSUNAN UNIVERSITY   (Japan)

^b National Cerebral and Cardiovascular Center 30602   (Japan)

Author keywords

AUC dose; BCS; Bioinequivalence; Dose number; Human BE study; Human intestinal permeability

Indexed keywords

AMLODIPINE BESYLATE; AMPIROXICAM; AZELASTINE; AZITHROMYCIN; BENAZEPRIL; BETAXOLOL; BICALUTAMIDE; CARBOCISTEINE; CARVEDILOL; CEFCAPENE PIVOXIL; CEFDINIR; CEFDITOREN PIVOXIL; CEFIXIME; CEFPODOXIME PROXETIL; CEFTERAM PIVOXIL; CETIRIZINE; CIBENZOLINE SUCCINATE; CILAZAPRIL; CIPROFLOXACIN; CLARITHROMYCIN; DOXAZOSIN MESYLATE; EBASTINE; EPALRESTAT; ETODOLAC; FAMOTIDINE; GLIMEPIRIDE; IMIDAPRIL; ITOPRIDE; PARACETAMOL; UNINDEXED DRUG; DRUG;

AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG CLASSIFICATION; DRUG CLEARANCE; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUBILITY; HUMAN; INTESTINE MUCOSA PERMEABILITY; METABOLIC CLEARANCE RATE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RISK FACTOR; INTESTINE ABSORPTION; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS;

ADMINISTRATION, ORAL; HUMANS; INTESTINAL ABSORPTION; PHARMACEUTICAL PREPARATIONS; RISK FACTORS; THERAPEUTIC EQUIVALENCY;

EID: 62649147044     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp800140m     Document Type: Article

References (24)

1. Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System; FDA Guidance for Industry; FDA: Washington, DC, 2000.http://www.fda.gov/CDER/ GUIDANCE/3618fnl.pdf (accessed August 2008).
2. Aoyagi, N. Regulatory Response to BCS in Japan Harmonization, Globalization and Innovation in Pharmaceutical Science and Technology, September 26, 2005 (Japanese). http://www.nihs.go.jp/drug/section0/Yokohama050926.pdf (accessed August 2008).
3. Amidon, G. L.; Lennernas, H.; Shah, V. P.; Crison, J. R. A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability. Pharm. Res. 1995, 12, 413-420.
4. Karalis, V.; Macheras, P.; Van Peer, A.; Shah, V. P. Bioavailability and bioequivalence: focus on physiological factors and variability. Pharm. Res. 2008, 25, 1956-1962.
5. Gu, C. H.; Li, H.; Levons, J.; Lentz, K.; Gandhi, R. B.; Raghavan, K.; Smith, R. L. Predicting effect of food on extent of drug absorption based on physicochemical properties. Pharm. Res. 2007, 24, 1118-1130.
6. Davit, B. M.; Conner, D. P.; Fabian-Fritsch, B.; Haidar, S. H.; Jiang, X.; Patel, D. T.; Seo, P. R.; Suh, K.; Thompson, C. L.; Yu, L. X. Highly variable drugs: observations from bioequivalence data submitted to the FDA for new generic drug applications. AAPSJ. 2008, 10, 148-156.
7. Guidelines for Bioequivalence Studies of Generic Products (Japanese); 2006. http://www.nihs.go.jp/drug/be-guide/ GL061124-BE.pdf (accessed August 2008).
8. Regardh, C. G.; Borg, K. O.; Johansson, R.; Johnsson, G.; Palmer, L. Pharmacokinetic studies on the selective beta1-receptor antagonist metoprolol in man. J. Pharmacokinet. Biopharm. 1974, 2, 347-364.
9. The Japanese Pharmacopoeia Technical Information 2006 (Japanese); The Society of Japanese Pharmacopoeia: Tokyo, Japan, 2006; pp 31-33.
10. The database provided by TSRL Inc., http://www.tsrlinc.com/services/bcs/ search.cfm# (accessed August2008).
11. Q&A of Guidelines for Bioequivalence Studies of Generic Products (Japanese); 2006. http://www.nihs.go.jp/drug/be-guide/QA061124-BE. pdf (accessed August 2008).
12. Diletti, E.; Hauschke, D.; Steinijans, V. W. Sample Size Determination for Bioequivalence Assessment by Means of Confidence Intervals. Int. J. Clin. Pharmacol. Ther. Toxicol. 1991, 29, 1-8.
13. Yafune, A. Sample Size Determination for Bioequivalence Studies Based on Confidence Intervals. Jpn. J. Clin. Pharmacol. Ther. 2000, 31, 715-718 (Japanese).
14. Schuirmann, D. J. A Comparison of the Two One-Sided Tests Procedure and the Power Approach for Assessing the Equivalence of Average Bioavailability. J. Pharmacokinet. Biopharm. 1987, 15, 657-680.
15. Statistical Approaches to Establishing Bioequivalence; FDA Guidance for Industry; FDA: Washington, DC, 2001.http://www.fda.gov/Cder/guidance/3616fnl.pdf (accessed November 2008).
16. The Japanese Pharmacopoeia, 15th ed. (English); 2006.http:// jpdb.nihs.go.jp/jp15e/ (accessed August 2008).
17. WHO Expert Committee on Specifications for Pharmaceutical Preparations - WHO Technical Report Series, No. 863-Thirty- fourth Report, Annex 9-Multisource (generic) pharmaceutical products: guidelines on registration requirements to establish interchangeability; 1996. http://www.who.int/medicinedocs/en/d/ Js5516e/#Js5516e.19.5.1.2 (accessed August 2008).
18. Takagi, T.; Ramachandran, C.; Bermejo, M.; Yamashita, S.; Yu, L. X.; Amidon, G. L. A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan. Mol. Pharmaceutics 2006, 3, 631-643.
19. Japanese Orange Book 2007 (Japanese); 2007.http://www.jp- orangebook.gr.jp/ (accessed August 2008).
20. Endrenyi, L.; Yan, W. Variation of Cmax and Cmax/AUC in investigations of bioequivalence. Int. J. Clin. Pharmacol. Ther. Toxicol. 1993, 31, 184-189.
21. Hauck, W. W.; Parekh, A.; Lesko, L. J.; Chen, M. L.; Williams, R. L. Limits of 80%-125% for AUC and 70%-143% for Cmax. What is the impact on bioequivalence studies? Int. J. Clin. Pharmacol. Ther. 2001, 39, 350-355.
22. Interview forms of commercially drug products provided by Towa Pharmaceutical Co., Ltd. (Japanese). http://di.towayakuhin.co.jp/ towa5/search (accessed November 2008).
23. Yang, Y.; Faustino, P. J.; Volpe, D. A.; Ellison, C. D.; Lyon, R. C.; Yu, L. X. Biopharmaceutics classification of selected beta- blockers: solubility and permeability class membership. Mol. Pharmaceutics. 2007, 4, 608-614.
24. Lentz, K. A.; Hayashi, J.; Lucisano, L. J.; Polli, J. E. Development of a more rapid, reduced serum culture system for Caco-2 monolayers and application to the biopharmaceutics classification system. Int. J. Pharm. 2000, 200, 41-51.