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A perspective for biowaivers of human bioequivalence studies on the basis of the combination of the ratio of AUC to the dose and the biopharmaceutics classification system.
Mol Pharm. 2011 Aug 01; 8(4):1113-9.MP

Abstract

The ratio of AUC to the dose (AUC/dose) was previously found as a parameter that predicts a risk of bioinequivalence of oral drug products. On the basis of the combination of this parameter and the biopharmaceutics classification system (BCS), a perspective for biowaivers of human bioequivalence studies is discussed. Databases of bioequivalence studies using immediate-release solid oral dosage forms were disclosed by 6 Japanese generic pharmaceutical companies, and the number of subjects required for demonstrating bioequivalence between generic and reference products was plotted as a function of AUC/dose for each BCS category. A small variation in the number of subjects was constantly observed in bioequivalence studies using dosage forms containing an identical BCS class 1 or class 3 drug, even though formulations of the generic product differ between companies. The variation was extremely enlarged when the drugs were substituted with BCS class 2 drugs. Rate-determining steps in oral absorption of highly water-soluble BCS class 1 and class 3 drugs are independent of formulations when there is no significant difference in the in vitro dissolution profiles between formulations. The small variation observed for both BCS categories indicates that the number of subjects converges into one value for each drug. Our analysis indicates the appropriateness of biowaiver of bioequivalence studies for immediate-release solid oral dosage forms containing not only BCS class 1 drugs but also class 3 drugs.

Authors+Show Affiliations

Faculty of Pharmaceutical Sciences, Setsunan University, 45-1, Nagaokatoge-cho, Hirakata, Osaka 573-0101, Japan. sakuma@pharm.setsunan.ac.jpNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

21630662

Citation

Sakuma, Shinji, et al. "A Perspective for Biowaivers of Human Bioequivalence Studies On the Basis of the Combination of the Ratio of AUC to the Dose and the Biopharmaceutics Classification System." Molecular Pharmaceutics, vol. 8, no. 4, 2011, pp. 1113-9.
Sakuma S, Tachiki H, Uchiyama H, et al. A perspective for biowaivers of human bioequivalence studies on the basis of the combination of the ratio of AUC to the dose and the biopharmaceutics classification system. Mol Pharm. 2011;8(4):1113-9.
Sakuma, S., Tachiki, H., Uchiyama, H., Fukui, Y., Takeuchi, N., Kumamoto, K., Satoh, T., Yamamoto, Y., Ishii, E., Sakai, Y., Takeuchi, S., Sugita, M., & Yamashita, S. (2011). A perspective for biowaivers of human bioequivalence studies on the basis of the combination of the ratio of AUC to the dose and the biopharmaceutics classification system. Molecular Pharmaceutics, 8(4), 1113-9. https://doi.org/10.1021/mp100421j
Sakuma S, et al. A Perspective for Biowaivers of Human Bioequivalence Studies On the Basis of the Combination of the Ratio of AUC to the Dose and the Biopharmaceutics Classification System. Mol Pharm. 2011 Aug 1;8(4):1113-9. PubMed PMID: 21630662.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A perspective for biowaivers of human bioequivalence studies on the basis of the combination of the ratio of AUC to the dose and the biopharmaceutics classification system. AU - Sakuma,Shinji, AU - Tachiki,Hidehisa, AU - Uchiyama,Hitoshi, AU - Fukui,Yasunobu, AU - Takeuchi,Naohiro, AU - Kumamoto,Kazuo, AU - Satoh,Tomonori, AU - Yamamoto,Yoshinobu, AU - Ishii,Emi, AU - Sakai,Yoshiyuki, AU - Takeuchi,Susumu, AU - Sugita,Masaru, AU - Yamashita,Shinji, Y1 - 2011/06/17/ PY - 2011/6/3/entrez PY - 2011/6/3/pubmed PY - 2012/1/27/medline SP - 1113 EP - 9 JF - Molecular pharmaceutics JO - Mol Pharm VL - 8 IS - 4 N2 - The ratio of AUC to the dose (AUC/dose) was previously found as a parameter that predicts a risk of bioinequivalence of oral drug products. On the basis of the combination of this parameter and the biopharmaceutics classification system (BCS), a perspective for biowaivers of human bioequivalence studies is discussed. Databases of bioequivalence studies using immediate-release solid oral dosage forms were disclosed by 6 Japanese generic pharmaceutical companies, and the number of subjects required for demonstrating bioequivalence between generic and reference products was plotted as a function of AUC/dose for each BCS category. A small variation in the number of subjects was constantly observed in bioequivalence studies using dosage forms containing an identical BCS class 1 or class 3 drug, even though formulations of the generic product differ between companies. The variation was extremely enlarged when the drugs were substituted with BCS class 2 drugs. Rate-determining steps in oral absorption of highly water-soluble BCS class 1 and class 3 drugs are independent of formulations when there is no significant difference in the in vitro dissolution profiles between formulations. The small variation observed for both BCS categories indicates that the number of subjects converges into one value for each drug. Our analysis indicates the appropriateness of biowaiver of bioequivalence studies for immediate-release solid oral dosage forms containing not only BCS class 1 drugs but also class 3 drugs. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/21630662/A_perspective_for_biowaivers_of_human_bioequivalence_studies_on_the_basis_of_the_combination_of_the_ratio_of_AUC_to_the_dose_and_the_biopharmaceutics_classification_system_ L2 - https://doi.org/10.1021/mp100421j DB - PRIME DP - Unbound Medicine ER -