Marcelo Gomes Davanço, Miguel Fortuny, Alejandro Scasso, Jessica Meulman, Fernando Costa, Thalita Martins da Silva, Débora Renz Barreto Vianna, Leonardo de Souza Teixeira, Karini Bruno Bellorio, Ana Carolina Costa Sampaio, Celso Francisco Pimentel Vespasiano
{"title":"丁丙诺啡透皮给药系统:两种贴片配方的生物等效性评估和粘附性能。","authors":"Marcelo Gomes Davanço, Miguel Fortuny, Alejandro Scasso, Jessica Meulman, Fernando Costa, Thalita Martins da Silva, Débora Renz Barreto Vianna, Leonardo de Souza Teixeira, Karini Bruno Bellorio, Ana Carolina Costa Sampaio, Celso Francisco Pimentel Vespasiano","doi":"10.3390/pharmaceutics16101249","DOIUrl":null,"url":null,"abstract":"<p><p><b>Background and Objective:</b> Buprenorphine is an opioid drug indicated for the management of severe and persistent pain. The buprenorphine transdermal patch provides a non-invasive method of rate-controlled drug release, ensuring constant and predictable drug plasma levels over an extended period. This study aimed to assess the bioequivalence, skin adhesion non-inferiority, and tolerability of two buprenorphine transdermal patches to meet the regulatory requirements for the registration of a generic product in Brazil. <b>Methods:</b> A randomized, single-dose, two-period, two-sequence crossover trial was performed involving healthy subjects of both genders. The subjects received a single dose of either the test formulation or the reference formulation (Restiva<sup>®</sup>), separated by a 29-day washout period. For pharmacokinetic analysis, blood samples were collected up to 12 days post-dose and quantified using a validated bioanalytical method. Skin adhesion was assessed over a 7-day period (dosing interval) following patch application. Seventy-six subjects were enrolled and fifty-two completed the study. <b>Results and Conclusion:</b> The 90% confidence intervals for Cmax, AUC<sub>0-t</sub>, and partial AUCs were within the acceptable bioequivalence limits of 80 to 125%. Adhesion comparison showed the non-inferiority of the test formulation. Based on ANVISA's regulatory requirements, the test and reference formulations were considered bioequivalent and could be interchangeable in clinical practice.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":4.9000,"publicationDate":"2024-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11510105/pdf/","citationCount":"0","resultStr":"{\"title\":\"Buprenorphine Transdermal Delivery System: Bioequivalence Assessment and Adhesion Performance of Two Patch Formulations.\",\"authors\":\"Marcelo Gomes Davanço, Miguel Fortuny, Alejandro Scasso, Jessica Meulman, Fernando Costa, Thalita Martins da Silva, Débora Renz Barreto Vianna, Leonardo de Souza Teixeira, Karini Bruno Bellorio, Ana Carolina Costa Sampaio, Celso Francisco Pimentel Vespasiano\",\"doi\":\"10.3390/pharmaceutics16101249\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><b>Background and Objective:</b> Buprenorphine is an opioid drug indicated for the management of severe and persistent pain. 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Buprenorphine Transdermal Delivery System: Bioequivalence Assessment and Adhesion Performance of Two Patch Formulations.
Background and Objective: Buprenorphine is an opioid drug indicated for the management of severe and persistent pain. The buprenorphine transdermal patch provides a non-invasive method of rate-controlled drug release, ensuring constant and predictable drug plasma levels over an extended period. This study aimed to assess the bioequivalence, skin adhesion non-inferiority, and tolerability of two buprenorphine transdermal patches to meet the regulatory requirements for the registration of a generic product in Brazil. Methods: A randomized, single-dose, two-period, two-sequence crossover trial was performed involving healthy subjects of both genders. The subjects received a single dose of either the test formulation or the reference formulation (Restiva®), separated by a 29-day washout period. For pharmacokinetic analysis, blood samples were collected up to 12 days post-dose and quantified using a validated bioanalytical method. Skin adhesion was assessed over a 7-day period (dosing interval) following patch application. Seventy-six subjects were enrolled and fifty-two completed the study. Results and Conclusion: The 90% confidence intervals for Cmax, AUC0-t, and partial AUCs were within the acceptable bioequivalence limits of 80 to 125%. Adhesion comparison showed the non-inferiority of the test formulation. Based on ANVISA's regulatory requirements, the test and reference formulations were considered bioequivalent and could be interchangeable in clinical practice.
PharmaceuticsPharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍:
Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications, and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.