دورية أكاديمية
أعرض في EDS

Cutaneous pharmacokinetics-based bioequivalence: A clinical dermal open flow microperfusion verification study using lidocaine and prilocaine combination topical products.

التفاصيل البيبلوغرافية
العنوان: Cutaneous pharmacokinetics-based bioequivalence: A clinical dermal open flow microperfusion verification study using lidocaine and prilocaine combination topical products.
المؤلفون: Tiffner KI; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria., Ramezanli T; Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, MD, USA., Boulgaropoulos B; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria; Division of Endocrinology and Diabetology, Department of Internal Medicine, Medical University of Graz, Auenbruggerplatz 15, 8036, Graz, Austria., Birngruber T; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria., Bodenlenz M; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria., Lackner BC; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria., Raml R; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria., Jiang Y; Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, MD, USA., Raney SG; Office of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, MD, USA., Sinner F; Institute for Biomedical Research and Technologies (HEALTH), Joanneum Research Forschungsgesellschaft m.b.H, Neue Stiftingtalstrasse 2, 8010, Graz, Austria; Division of Endocrinology and Diabetology, Department of Internal Medicine, Medical University of Graz, Auenbruggerplatz 15, 8036, Graz, Austria.
المصدر: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2024 Sep 01; Vol. 200, pp. 106827. Date of Electronic Publication: 2024 Jun 08.
نوع المنشور: Journal Article; Randomized Controlled Trial
اللغة: English
بيانات الدورية: Publisher: Elsevier Science B.V Country of Publication: Netherlands NLM ID: 9317982 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-0720 (Electronic) Linking ISSN: 09280987 NLM ISO Abbreviation: Eur J Pharm Sci Subsets: MEDLINE
أسماء مطبوعة: Publication: Amsterdam : Elsevier Science B.V
Original Publication: Amsterdam ; New York : Elsevier, c1993-
مواضيع طبية MeSH: Therapeutic Equivalency* , Administration, Cutaneous* , Anesthetics, Local*/pharmacokinetics , Anesthetics, Local*/administration & dosage , Skin Absorption* , Skin*/metabolism, Humans ; Male ; Adult ; Female ; Young Adult ; Lidocaine, Prilocaine Drug Combination/pharmacokinetics ; Lidocaine, Prilocaine Drug Combination/administration & dosage ; Lidocaine/pharmacokinetics ; Lidocaine/administration & dosage ; Skin Cream/pharmacokinetics ; Skin Cream/administration & dosage ; Prilocaine/pharmacokinetics ; Prilocaine/administration & dosage ; Perfusion/methods
مستخلص: Background: Using accurate, sensitive, reproducible and efficient in vivo cutaneous pharmacokinetics (PK)-based bioequivalence (BE) approaches can promote the development of topical generic drug products. A clinical dermal open flow microperfusion (dOFM) study has previously demonstrated the BE of topical drug products containing a hydrophilic drug. However, the utility of dOFM to evaluate the topical BE of drug products containing moderately lipophilic drugs, more representative of most topical drugs, has not yet been established.
Objective: To evaluate the ability of a clinical dOFM study to assess BE of topical products containing two moderately lipophilic drugs that have only minor differences in chemical and physical properties.
Methods: The study included 20 healthy subjects. Four application sites on each thigh were treated with fixed dose lidocaine/prilocaine combination products, and dermal drug concentrations were monitored with two dOFM probes per application site for 12 h. A reference cream was compared to itself and to an approved generic cream (both serving as positive controls for BE), and to a gel (negative control). BE was established based on AUC 0to12h and C max using the scaled-average-BE approach. Systemic exposure of both drugs was assessed throughout the study.
Results: BE was successfully demonstrated for the positive controls, and not for the negative control, for both drugs. The systemic exposure of both drugs was negligible.
Conclusions: dOFM accurately demonstrated BE between bioequivalent topical creams, sensitively discriminated between different formulations and differentiated the cutaneous PK of both study drugs, even though they differ only slightly in chemical and physical properties. These results support the utility of dOFM as a cutaneous PK-based BE approach for topical lipophilic drugs, including lidocaine and prilocaine.
(Copyright © 2024. Published by Elsevier B.V.)
معلومات مُعتمدة: U01 FD005861 United States FD FDA HHS; U01 FD007669 United States FD FDA HHS
فهرسة مساهمة: Keywords: Bioequivalence; Cutaneous pharmacokinetics; Dermal open flow microperfusion; Lidocaine; Prilocaine; Topical
المشرفين على المادة: 0 (Anesthetics, Local)
0 (Lidocaine, Prilocaine Drug Combination)
98PI200987 (Lidocaine)
046O35D44R (Prilocaine)
تواريخ الأحداث: Date Created: 20240610 Date Completed: 20240728 Latest Revision: 20240728
رمز التحديث: 20240729
DOI: 10.1016/j.ejps.2024.106827
PMID: 38857708
قاعدة البيانات: MEDLINE
الوصف
تدمد:1879-0720
DOI:10.1016/j.ejps.2024.106827