nach oben

Clinical Pharmacokinetics

Erschienen in:

01.11.2015 | Review Article

Pharmacokinetics-Based Approaches for Bioequivalence Evaluation of Topical Dermatological Drug Products

verfasst von: Sam G. Raney, Thomas J. Franz, Paul A. Lehman, Robert Lionberger, Mei-Ling Chen

Erschienen in: Clinical Pharmacokinetics | Ausgabe 11/2015

Einloggen, um Zugang zu erhalten

Abstract

The pharmacokinetic approach has accelerated the development of high-quality generic medicines with extraordinary cost savings, transforming the pharmaceutical industry and healthcare system in the USA. While this is true for systemically absorbed drug products, the availability of generic versions of topical dermatological products remains constrained due to the limited methods accepted for bioequivalence evaluation of these products. The current review explores the possibility of developing appropriate bioequivalence approaches based on pharmacokinetic principles for topical dermatological products. This review focuses on the strengths and limitations of the three most promising pharmacokinetics-based methods to evaluate the performance and bioequivalence of topical dermatological products, which include in vivo skin stripping, in vivo microdialysis, and in vitro permeation testing (IVPT) with excised human skin. It is hoped that recent advances in pharmaceutical and regulatory science will facilitate the development of robust bioequivalence approaches for these dosage forms, enable more efficient methodologies to compare the performance of new drug products in certain pre-approval or post-approval change situations, and promote the availability of high-quality generic versions of topical dermatological products.

Drug products approved by the US FDA are coded to reflect the nature of their therapeutic equivalence (or lack thereof). According to the preface of the 34th edition of the Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations [7], the therapeutic equivalence rating of AB for a generic drug product indicates that it is considered to be therapeutically equivalent to its pharmaceutically equivalent reference listed drug product, and that actual or potential bioequivalence problems have been resolved with adequate in vivo and/or in vitro evidence supporting bioequivalence.

The Drug Price Competition and Patent Term Restoration Act of 1984 (Public Law 98-417). http://www.gpo.gov/fdsys/pkg/STATUTE-98/pdf/STATUTE-98-Pg1585.pdf. Accessed 12 Feb 2015.

Generic Pharmaceutical Association (GPhA). Generic drug savings in the U.S. Sixth annual edition. 2014. http://www.gphaonline.org/media/cms/GPhA_Savings_Report.9.10.14_FINAL.pdf. Accessed 12 Feb 2015.

Thayer AM. 30 years of generics. C&EN. 2014;92(39):8–16.CrossRef

IMS Institute for Healthcare Informatics. Medicine use and shifting costs of healthcare: a review of the use of medicines in the United States in 2013. http://www.imshealth.com/deployedfiles/imshealth/Global/Content/Corporate/IMS%20Health%20Institute/Reports/Secure/IIHI_US_Use_of_Meds_for_2013.pdf. Accessed 12 Feb 2015.

The Medicare Prescription Drug, Improvement and Modernization Act of 2003; Title XI—access to affordable pharmaceuticals. http://www.gpo.gov/fdsys/pkg/PLAW-108publ173/pdf/PLAW-108publ173.pdf. Accessed 12 Feb 2015.

United States Food and Drug Administration, Title 21 Code of Federal Regulations (CFR) Part 320, Section 1. http://www.accessdata.fda.gov/scripts/cdrh/cfdocs/cfcfr/CFRSearch.cfm?fr=320.1. Accessed 12 Feb 2015.

United States Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, Office of Generic Drugs. Orange book: approved drug products with therapeutic equivalence evaluations, 35th edn. 2014. http://www.fda.gov/downloads/Drugs/DevelopmentApprovalProcess/UCM071436.pdf. Accessed 12 Feb 2015.

United States Food and Drug Administration, Title 21 Code of Federal Regulations (CFR) Part 320, Section 24. http://www.accessdata.fda.gov/scripts/cdrh/cfdocs/cfcfr/CFRSearch.cfm?fr=320.24. Accessed 12 Feb 2015.

Chaurasia C, Muller M, Bashaw E, Benfeldt E, Bolinder J, Bullock R, et al. AAPS-FDA workshop white paper: microdialysis principles, application and regulatory perspectives. Pharm Res. 2007;24:1014–25.CrossRefPubMed

10.

Holmgaard R, Nielsen JB, Benfeldt E. Microdialysis sampling for investigations of bioavailability and bioequivalence of topically administered drugs: current state and future perspectives. Skin Pharmacol Physiol. 2010;23:225–43.CrossRefPubMed

11.

Franz TJ, Lehman PA, Raney SG. Use of excised human skin to assess the bioequivalence of topical products. Skin Pharmacol Physiol. 2009;22:276–86.PubMedCentralCrossRefPubMed

12.

Lehman PA, Raney SG, Franz TJ. Percutaneous absorption in man: in vitro-in vivo correlation. Skin Pharmacol Physiol. 2011;24:224–30.CrossRefPubMed

13.

United States Food and Drug Administration. Guidance for industry: topical dermatologic corticosteroids: in vivo bioequivalence. http://www.fda.gov/ohrms/dockets/dockets/04p0206/04p-0206-ref0001-08-FDA-Guidance-for-Industry-06-1995-vol3.pdf. Accessed 12 Feb 2015.

14.

Carroll CL, Feldman SR, Camacho FT, Manuel JC, Balkrishnan R. Adherence to topical therapy decreases during the course of an 8-week psoriasis clinical trial: commonly used methods of measuring adherence to topical therapy overestimate actual use. J Am Acad Dermatol. 2004;51:212–6.CrossRefPubMed

15.

Krejci-Manwaring J, Tusa MG, Carroll C, Camacho F, Kaur M, Carr D, et al. Stealth monitoring of adherence to topical medication: adherence is very poor in children with atopic-ádermatitis. J Am Acad Dermatol. 2007;56:211–6.CrossRefPubMed

16.

Hick J, Feldman SR. Eligibility creep: a cause for placebo group improvement in controlled trials of psoriasis treatments. J Am Acad Dermatol. 2007;57:972–6.CrossRefPubMed

17.

Shah VP, Maibach HI, editors. Topical drug bioavailability, bioequivalence and penetration. New York: Plenum Press; 1993.

18.

Maibach HI. Dermatologic research techniques. Boca Raton: CRC Press Inc.; 1996.

19.

Shah VP, Flynn GLFAU, Yacobi AF, Maibach HI, Bon CF, Fleischer NM, et al. Bioequivalence of topical dermatological dosage forms-methods of evaluation of bioequivalence. Pharm Res. 1998;15:167–71.CrossRefPubMed

20.

Pershing L, Silver B, Krueger G, Shah V, Skelley J. Feasibility of measuring the bioavailability of topical betamethasone dipropionate in commercial formulations using drug content in skin and a skin blanching bioassay. Pharm Res. 1992;9:45–51.CrossRefPubMed

21.

Pershing LK, Lambert LD, Shah VP, Lam SY. Variability and correlation of chromameter and tape-stripping methods with the visual skin blanching assay in the quantitative assessment of topical 0.05 % betamethasone dipropionate bioavailability in humans. Int J Pharm. 1992;86:201–10.CrossRef

22.

Pershing LK, Bakhtian S, Poncelet CE, Corlett JL, Shah VP. Comparison of skin stripping, in vitro release, and skin blanching response methods to measure dose response and similarity of triamcinolone acetonide cream strengths from two manufactured sources. J Pharm Sci. 2002;91:1312–23.CrossRefPubMed

23.

Wiedersberg S, Naik A, Leopold CS, Guy RH. Pharmacodynamics and dermatopharmacokinetics of betamethasone 17-valerate: assessment of topical bioavailability. Br J Dermatol. 2009;160:676–86.CrossRefPubMed

24.

Benfeldt E, Hansen SH, Volund A, Menne T, Shah VP. Bioequivalence of topical formulations in humans: evaluation by dermal microdialysis sampling and the dermatopharmacokinetic method. J Invest Dermatol. 2006;127:170–8.CrossRefPubMed

25.

United States Food and Drug Administration. Draft guidance for industry: topical dermatological drug product NDAs and ANDAs—in vivo bioavailability, bioequivalence, in vitro release, and associated studies. 1998. http://www.fda.gov/OHRMS/DOCKETS/98fr/3659bg.pdf. Accessed 12 Feb 2015.

26.

Draft guidance for industry on topical dermatological drug product NDAs and ANDAs-in vivo bioavailability, bioequivalence, in vitro release and associated studies; withdrawal (2002). Fed Reg. 2002;67:35122–3. https://www.federalregister.gov/articles/2002/05/17/02-12326/draft-guidance-for-industry-on-topical-dermatological-drug-product-ndas-and-andas-in-vivo. Accessed 12 Feb 2015.

27.

Pershing LK, Nelson JL, Corlett JL, Shrivastava SP, Hare DB, Shah VP. Assessment of dermatopharmacokinetic approach in the bioequivalence determination of topical tretinoin gel products. J Am Acad Dermatol. 2003;48:740–51.CrossRefPubMed

28.

Quigley JW, Bucks DAW. Reduced skin irritation with tretinoin containing polyolprepolymer-2, a new topical tretinoin delivery system: a summary of preclinical and clinical investigations. J Am Acad Dermatol. 1998;38:S5–10.CrossRefPubMed

29.

Franz TJ. Study #1, Avita gel 0.025 % vs Retin-A gel 0.025 %. Transcribed presentation to the Advisory Committee for Pharmaceutical Sciences Meeting, Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA), Rockville, MD, November 29, 2001. Presentation slides. http://www.fda.gov/ohrms/dockets/ac/01/slides/3804s2_03_franz.pdf. Accessed 12 Feb 2015.

30.

Conner DP. Differences in DPK methods. Transcribed presentation to the Advisory Committee for Pharmaceutical Sciences Meeting, Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA), Rockville, MD, November 29, 2001. Presentation slides. http://www.fda.gov/ohrms/dockets/ac/01/slides/3804s2_05_conner/index.htm. Accessed 12 Feb 2015.

31.

Weigmann H, Lademann J, Rv Pelchrzim, Sterry W, Hagemeister T, Molzahn R, et al. Bioavailability of clobetasol propionate—quantification of drug concentrations in the stratum corneum by dermatopharmacokinetics usingtape stripping. Skin Pharmacol Appl Skin Physiol. 1999;12:46–53.CrossRefPubMed

32.

N’Dri-Stempfer B, Navidi W, Guy R, Bunge A. Optimizing metrics for the assessment of bioequivalence between topical drug products. Pharm Res. 2008;25:1621–30.CrossRefPubMed

33.

N’Dri-Stempfer B, Navidi W, Guy R, Bunge A. Improved bioequivalence assessment of topical dermatological drug products using dermatopharmacokinetics. Pharm Res. 2009;26:316–28.CrossRefPubMed

34.

Parfitt NR, Skinner MF, Bon C, Kanfer I. Bioequivalence of topical clotrimazole formulations: an improved tape stripping method. J Pharm Sci. 2011;14:347–57.

35.

Kyle AA, Dahl MV. Topical therapy for fungal infections. Am J Clin Dermatol. 2004;5:443–51.CrossRefPubMed

36.

Bodenlenz M, Höfferer C, Magnes C, Schaller-Ammann R, Schaupp L, Feichtner F, et al. Dermal PK/PD of a lipophilic topical drug in psoriatic patients by continuous intradermal membrane-free sampling. Eur J Pharm Biopharm. 2012;81:635–41.CrossRefPubMed

37.

Kreilgaard M, Kemme MJ, Burggraaf JF, Schoemaker RC, Cohen AF. Influence of a microemulsion vehicle on cutaneous bioequivalence of a lipophilic model drug assessed by microdialysis and pharmacodynamics. Pharm Res. 2001;18:593–9.CrossRefPubMed

38.

Tettey-Amlalo RN, Kanfer IF, Skinner MF, Benfeldt E, Verbeeck RK. Application of dermal microdialysis for the evaluation of bioequivalence of a ketoprofen topical gel. Eur J Pharm Sci. 2009;36:219–25.CrossRefPubMed

39.

Rougier A, Lotte C, Corcuff P, Maibach HI. Relationship between skin permeability and corneocyte size according to anatomic site, age, and sex in man. J Soc Cosmet Chem. 1988;39:15–26.

40.

Lehman PA, Franz TJ. Assessing the bioequivalence of topical retinoid products by pharmacodynamic assay. Skin Pharmacol Physiol. 2012;25:269–80.CrossRefPubMed

41.

Garcia Ortiz P, Hansen SH, Shah VP, Sonne JF, Benfeldt E. Are marketed topical metronidazole creams bioequivalent? Evaluation by in vivo microdialysis sampling and tape stripping methodology. Skin Pharmacol Physiol. 2011;24:44–53.CrossRefPubMed

42.

Skelly J, Shah V, Maibach H, Guy R, Wester R, Flynn G, et al. FDA and AAPS report of the workshop on principles and practices of in vitro percutaneous penetration studies: relevance to bioavailability and bioequivalence. Pharm Res. 1987;4:265–7.CrossRef

43.

Bronaugh R. Protocol for in vitro percutaneous absorption studies. In vitro percutaneous absorption: principles, fundamentals and applications. Boca Raton: CRC Press; 1991.

44.

Howes D, Guy R, Hadgraft J, Heylings J, Hoeck U, Kemper F, et al. Methods for assessing percutaneous absorption: the report and recommendations of ECVAM Workshop 13. Alternatives Lab Anim. 1996;24:81–106.

45.

Diembeck W, Beck H, Benech-Kieffer F, Courtellemont P, Dupuis J, Lovell W, et al. Test guidelines for in vitro assessment of dermal absorption and percutaneous penetration of cosmetic ingredients. Food Chem Toxicol. 1999;37:191–205.CrossRefPubMed

46.

European Commission, Health and Consumer Protection Directorate-General, Scientific Committee on Consumer Products (SCCP). Opinion on basic criteria for the in vitro assessment of dermal absorption of cosmetic ingredients. 2006. http://ec.europa.eu/health/ph_risk/committees/04_sccp/docs/sccp_s_03.pdf. Accessed 12 Feb 2015.

47.

Organization for Economic Co-operation and Development, Environment Directorate, Joint Meeting of the Chemicals Committee and the Working Party on Chemicals, Pesticides and Biotechnology Guidance document for the conduct of skin absorption studies. OECD Series on Testing and Assessment, Number 28. 2004. http://www.oecd.org/officialdocuments/publicdisplaydocumentpdf/?doclanguage=en&cote=env/jm/mono%282004%292. Accessed 12 Feb 2015.

48.

Organisation for Economic Cooperation and Development. OECD guideline for testing of chemicals, Section 4. Health effects. Test No. 428: skin absorption: in vitro method. 2004. http://www.oecd-ilibrary.org/docserver/download/9742801e.pdf?expires=1423780557&id=id&accname=guest&checksum=4891441FCF0A24E3C7491C93D140CBC1. Accessed 12 Feb 2015.

49.

Raabe H, Ward S, Harbell J. Report from an in vitro dermal absorption assay workshop. Presented at the 5th World Congress on Alternatives and Animal Use in Life Sciences, Berlin, Germany, August 21–25. 2005 In Vitro Percutaneous Absorption Expert Users Workshop, 20 and 21 July 2005, Gaithersburg Hilton, Gaithersburg, USA. http://www.iivs.org/workspace/assets/publications/116_iivs_poster_report-from-an-in-vitro-dermal-absorption-assay-workshop.pdf. Accessed 12 Feb 2015.

50.

Kielhorn J, Melching-Kollmus S, Mangelsdorf I.. Dermal absorption (Environmental Health Criteria 235), Geneva: International Programme on Chemical Safety, WHO, International Labour Organization, United Nations Environment Programme. 2006. http://www.inchem.org/documents/ehc/ehc/ehc235.pdf. Accessed 12 Feb 2015.

51.

In vitro dermal absorption rate testing of certain chemicals of interest to the occupational safety and health administration. United States Environmental Protection Agency, 40 CFR Parts and 799, [OPPT-2003-0006; FRL-7312-2], RIN 2070-AD422004. Fed Regist 2004;69(80):22402–41. http://www.gpo.gov/fdsys/pkg/FR-2004-04-26/pdf/04-9409.pdf. Accessed 27 May 2015.

52.

Requirements for submission of bioequivalence data; final rule. Fed Regist. 2009;74(11):2849–62. http://www.fda.gov/ohrms/dockets/98fr/E9-884.htm. Accessed 12 Feb 2015.

53.

European Medicines Agency. Guideline on quality of transdermal patches. EMA/CHMP/QWP/608924/2014. 2014. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2014/12/WC500179071.pdf. Accessed 12 Feb 2015.

54.

United States Food and Drug Administration. Critical path: opportunities for generic drugs. Section 4.3.3: bioequivalence of topical dermatological products. 2007. http://www.fda.gov/ScienceResearch/SpecialTopics/CriticalPathInitiative/CriticalPathOpportunitiesReports/ucm077250.htm#dermatological. Accessed 12 Feb 2015.

55.

Yacobi A, Shah VP, Bashaw ED, Benfeldt E, Davit B, Ganes D, et al. Current challenges in bioequivalence, quality, and novel assessment technologies for topical products. Pharm Res. 2014;31:837–46.CrossRefPubMed

56.

Haidar SH, Makhlouf F, Schuirmann DJ, Hyslop T, Davit B, Conner D, Yu LX. Evaluation of a scaling approach for the bioequivalence of highly variable drugs. AAPS J. 2008;10:450–4.PubMedCentralCrossRefPubMed

57.

Senn S. Change from baseline and analysis of covariance revisited. Stat Med. 2006;25:4334–44.CrossRefPubMed

58.

Laird N. Further comparative analyses of pretest-posttest research designs. Am Stat. 1983;37:329–30.

59.

Bustad A, Terziivanov D, Leary R, Port R, Schumitzky A, Jelliffe R. Parametric and nonparametric population methods: their comparative performance in analysing a clinical data set and two Monte Carlo simulation studies. Clin Pharmacokinet. 2006;45:365–83.CrossRefPubMed

60.

Jelliffe R, Bayard D, Milman M, Van Guilder M, Schumitzky A. Achieving target goals most precisely using nonparametric compartmental models and “multiple model” design of dosage regimens. Ther Drug Monit. 2000;22:346–53.CrossRefPubMed

61.

Jelliffe RW, Schumitzky A, Van Guilder M, Liu M, Hu L, Maire P, et al. Individualizing drug dosage regimens: roles of population pharmacokinetic and dynamic models, bayesian fitting, and adaptive control. Ther Drug Monit. 1993;15:380–93.CrossRefPubMed

62.

Jelliffe RW, Schumitzky A, Bayard D, Fu X, Neely M. Describing assay precision-reciprocal of variance is correct, not CV percent: its use should significantly improve laboratory performance. Ther Drug Monit. 2015;37:389–94.CrossRefPubMed

63.

Chang RK, Raw A, Lionberger R, Yu L. Generic development of topical dermatologic products: formulation development, process development, and testing of topical dermatologic products. AAPS J. 2013;15:41–52.PubMedCentralCrossRefPubMed

64.

Chang RK, Raw A, Lionberger R, Yu L. Generic development of topical dermatologic products, part II: quality by design for topical semisolid products. AAPS J. 2013;15:674–83.PubMedCentralCrossRefPubMed

65.

Shah VP, Maibach HI, Jenner J, editors. Topical drug bioavailability, bioequivalence, and penetration. 2nd ed. New York: Springer; 2014.

66.

Franz TJ. Study #1, Avita gel 0.025 % vs Retin-A gel 0.025 %. Transcribed presentation to the Advisory Committee for Pharmaceutical Sciences Meeting, Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA), Rockville, MD, November 29, 2001. Transcript of presentation. pp. 47–61. http://www.fda.gov/ohrms/dockets/ac/01/transcripts/3804t2_01_Morning_Session.pdf. Accessed 12 Feb 2015.

67.

Conner DP. Differences in DPK methods. Transcribed presentation to the Advisory Committee for Pharmaceutical Sciences Meeting, Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA), Rockville, MD, November 29, 2001. Transcript of presentation. pp. 71–75. http://www.fda.gov/ohrms/dockets/ac/01/transcripts/3804t2_01_Morning_Session.pdf. Accessed 12 Feb 2015.

Titel: Pharmacokinetics-Based Approaches for Bioequivalence Evaluation of Topical Dermatological Drug Products
verfasst von: Sam G. Raney
Thomas J. Franz
Paul A. Lehman
Robert Lionberger
Mei-Ling Chen
Publikationsdatum: 01.11.2015
Verlag: Springer International Publishing
Erschienen in: Clinical Pharmacokinetics / Ausgabe 11/2015
Print ISSN: 0312-5963
Elektronische ISSN: 1179-1926
DOI: https://doi.org/10.1007/s40262-015-0292-0

Live-Webinar "Chronische Unterbauch- und Viszeralschmerzen in der Praxis managen"

Springer Medizin

Pharmacokinetics-Based Approaches for Bioequivalence Evaluation of Topical Dermatological Drug Products

Abstract

Live-Webinar "Chronische Unterbauch- und Viszeralschmerzen in der Praxis managen"

Springer Medizin

Abstract

Bitte loggen Sie sich ein, um Zugang zu diesem Inhalt zu erhalten

Weitere Artikel der Ausgabe 11/2015

Investigation of Saliva as an Alternative to Plasma Monitoring of Voriconazole

The Impact of Sertraline Co-Administration on the Pharmacokinetics of Olanzapine: A Population Pharmacokinetic Analysis of the STOP-PD

How to Improve the Safe and Effective Use of Doxorubicin in Children with Cancer

Ticagrelor: Pharmacokinetic, Pharmacodynamic and Pharmacogenetic Profile: An Update

Age-Dependent Pharmacokinetics of Doxorubicin in Children with Cancer

Clinical Pharmacokinetics and Pharmacodynamics of Monoclonal Antibodies Approved to Treat Rheumatoid Arthritis