Plasma pharmacokinetics and synovial concentrations of S-flurbiprofen plaster in humans
| Autor: | Yuichi Hoshino, Noboru Otsuka, Ichimaro Yamada, Isao Matsushita, Hideo Matsumoto, Kazuo Uebaba, Miho Kamezawa, Ikuko Yataba, Sigeru Sasaki |
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| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Adult
Male Administration Topical Flurbiprofen Transdermal Patch Pharmacology 03 medical and health sciences Young Adult 0302 clinical medicine Pharmacokinetics Deep tissue Healthy volunteers Medicine Humans Topical NSAIDs Pharmacology (medical) Single-Blind Method Synovial tissue Aged 030203 arthritis & rheumatology Aged 80 and over business.industry S-flurbiprofen Anti-Inflammatory Agents Non-Steroidal Synovial Membrane General Medicine Penetration (firestop) Middle Aged Osteoarthritis Knee Pharmacokinetics and Disposition musculoskeletal system Healthy Volunteers Tissue concentration medicine.anatomical_structure lipids (amino acids peptides and proteins) Female Synovial membrane Erratum business 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | European Journal of Clinical Pharmacology |
| ISSN: | 1432-1041 0031-6970 |
| Popis: | Purpose The purpose of this study is to investigate the pharmacokinetics and deep tissue penetration capability of the newly developed S-flurbiprofen plaster (SFPP) in humans. Methods Study 1: SFPP tape-type patch (2–60 mg) was applied to the lower back for 24 h in healthy adult volunteers. S-flurbiprofen (SFP) plasma concentration was measured over time to examine SFP pharmacokinetics. Study 2: SFPP (20 mg) was applied for 12 h to the affected knee of osteoarthritis (OA) patients who were scheduled for total knee arthroplasty. Deep tissues (synovial tissue and synovial fluid) were collected during surgery to compare SFP concentrations after application of SFPP or a commercially available flurbiprofen (FP) gel-type patch. Results Study 1: The plasma concentration of SFP was sustained during 24-h topical application of the SFPP, showing a high percutaneous absorption ratio of 51.4–72.2 %. Cmax and AUC0-∞ were dose-proportional. Study 2: After application of the SFPP for 12 h, SFP concentrations in the synovial tissue and synovial fluid were 14.8-fold (p = 0.002) and 32.7-fold (p |
| Databáze: | OpenAIRE |
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