Your browser doesn't support javascript.
loading
Plasma pharmacokinetics and synovial concentrations of S-flurbiprofen plaster in humans.
Yataba, Ikuko; Otsuka, Noboru; Matsushita, Isao; Kamezawa, Miho; Yamada, Ichimaro; Sasaki, Sigeru; Uebaba, Kazuo; Matsumoto, Hideo; Hoshino, Yuichi.
Afiliación
  • Yataba I; Development Headquarters, Taisho Pharmaceutical Co. Ltd, 3-24-1 Takada, Toshima-ku, Tokyo, 170-8633, Japan.
  • Otsuka N; Development Headquarters, Taisho Pharmaceutical Co. Ltd, 3-24-1 Takada, Toshima-ku, Tokyo, 170-8633, Japan. n-otsuka@so.taisho.co.jp.
  • Matsushita I; Development Headquarters, Taisho Pharmaceutical Co. Ltd, 3-24-1 Takada, Toshima-ku, Tokyo, 170-8633, Japan.
  • Kamezawa M; Mitsubishi Tanabe Pharma Corporation, Tokyo, Japan.
  • Yamada I; Mitsubishi Tanabe Pharma Corporation, Tokyo, Japan.
  • Sasaki S; Sapporo Tsukisamu Chuo Orthopedics, Sapporo, Japan.
  • Uebaba K; Faculty of Health Science, Teikyo Heisei University, Ichihara, Japan.
  • Matsumoto H; Institute for Integrated Sports Medicine, School of Medicine, Keio University, Tokyo, Japan.
  • Hoshino Y; Orthopedics Surgery, School of Medicine, Jichi Medical University, Shimotsuke, Japan.
Eur J Clin Pharmacol ; 72(1): 53-9, 2016 Jan.
Article en En | MEDLINE | ID: mdl-26438533
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 < 0.001) higher, respectively, than those achieved by the FP patch. CONCLUSIONS: Sustained plasma concentration of SFP and high percutaneous absorption ratio was observed after 24-h topical application of the SFPP. Compared to the FP patch, the SFPP showed superior percutaneous absorption and greater tissue penetration of SFP into the synovial tissue. Greater tissue penetration of the SFPP seemed to be primarily due to its formulation. Thus, SFPP is expected to show higher efficacy for the treatment of knee OA.
Asunto(s)
Palabras clave
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Membrana Sinovial / Antiinflamatorios no Esteroideos / Flurbiprofeno / Osteoartritis de la Rodilla Tipo de estudio: Clinical_trials Límite: Adult / Aged / Aged80 / Female / Humans / Male / Middle aged Idioma: En Revista: Eur J Clin Pharmacol Año: 2016 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Alemania
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Membrana Sinovial / Antiinflamatorios no Esteroideos / Flurbiprofeno / Osteoartritis de la Rodilla Tipo de estudio: Clinical_trials Límite: Adult / Aged / Aged80 / Female / Humans / Male / Middle aged Idioma: En Revista: Eur J Clin Pharmacol Año: 2016 Tipo del documento: Article País de afiliación: Japón Pais de publicación: Alemania