YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Formulation and Skin Permeation Characteristics of Ketoprofen Patches

케토프로펜 패취제의 제제설계 및 피부 투과 특성

  • Published : 2001.10.01
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Abstract

Ketoprofen (KP) was formulated as a transdermal patch using the percutaneous penetration enhancers sorbitan monmmleate(SMO), polyvinylpyrrolidone(PVP). The control patch without penetration enhancers showed a KP flux of 8.9$\pm$0.75$\mu\textrm{g}$/$\textrm{cm}^2$/h The flux was increased in proportion to the concentration of SMO added. Furthermore, lag times were decreased upon addition of SMO. Conversely; the skin flux of KP was decreased in proportion to the concentration of PVP added. Pharmacokinetic parameters including $C_{max}$, $T_{max}$, and AUC were increased when SMO was added. However, $C_{mas}$ significantly decreased by the addition of PVP. $T_{max}$ was not significantly different in 2%, 4%, and 8% PVP patches. Patches containing 4% PVP showed the highest AUC value (19.158$\mu\textrm{g}$.h/ml). We found that the effectiveness of the two percutaneous penetration enhancers for topical KP patches was similar, with the addition of appropriate amounts of HPC modifying both skin flux and lag time of KP in the patches. In conclusion, it is possible to manufacture KP patches exhibiting high AUC, high skin flux, and short lag time using percutaneous penetration enhancers of SMO and PVP.

Keywords

References

  1. Pharmacotherapy v.6 no.93 Ketoprofen;A review of its pharma-cological and clinical properties Kanto,T.G.
  2. Scan.J.Rheumatol.Suppl. v.14 no.33 Ketoprofen.Main pharmacological properties-Outline of toxicological and pharmaco-kinetic data Julou,L.;Guyonnet,J.C.;Ducrot,R.;Fournel,J.;Pasquet,J.
  3. Clin.Pharmacokinetics v.12 no.214 Clinical Pharmacokin of ketoprofen arter single intravenous adminstration as a bolous or in fusion Debruyne,D.;de Ligny,B.H.;Ryckelynck,J.;Albessard,F.;Moulin,M.
  4. Drug Res. v.39 no.812 Pharmacokinetics of ketoprofen in man after repeated percutaneous administration Flouvat,B.;Roux,A.;Dellhotal-Landes,B.
  5. J.Pharm.Sci. v.79 no.460 Ketoprofen pharmacokinetics in humans:Evidence of enantiomeric inversion and lack of interaction Jamali,F.;Russell,A.S.;Foster,R.T.;Lemko,C.
  6. Eur.J.Clin.Pharmacol. v.18 no.407 Pharmacokinetics of ketoprofen following single oral,intramuscular and rectal doses and after repeated oral administration Ishizaki,T.;Sasaki,T.;Suganima,T.;Horai,Y.;Chiba,K.;Watanabe,M.;Asuke,W.;Hoshi,H.
  7. J.Pharm.Sci. v.69 no.1254 Negligible excretion of unchanged ketoprofen,naproxen or probenecid in urine Upton,R.A.;Buskin,J.N.;Williams,R.L.;Holford,N.H.G.;Riegelman,S.
  8. Anti-Inflammatory and Anti-Rheumatic Drugs v.1 Inflammation Mechanism and Actions of Traditional Durgs Rainsford,K.O.
  9. Anti-Inflammatory and Anti-Rheumatic Drugs v.Ⅱ Newer Anti-Inflammatory Drugs Rainsford,K.O.
  10. Nonsteroidal Anti Inflammatory Drugs.Mechanism and Clinical Use Lewis,A.J.;Furst,D.W.
  11. Anti-inflammatory and Anti-rheumatic Drugs v.Ⅱ Harris,R.H.;Vavra,IKetoprofen.In Rainsford,K.D.
  12. Therapeutic Research. v.6 no.591 Tissue penetration of ketoprofen after cutaneous application of HKP-210 in patients Sugawara,S.
  13. Arzneim.Forsch v.33 no.1497 Pharmacokinetics of a slow-release preparation of ketoprofen lysine in man Borsa,M.;Tonon,G.C.;Ronchi,C.;Zanolo,G.;Canali,S.
  14. Drugs Exp.Clin.Res. v.13 no.294 Effectiveness and tolerability of ketoprofen lysine,once a day,in patients with rheumatic disorders Chevallard,M.;Mele,G.;Borsa,M.;Tonon,G.C.
  15. J.Int.Med.Res. v.10 no.229 Bioavailability study on a new slow release formulation of ketoprofen Caruso,I.;Frigerio,E.;Fumagalli,M.;Liverta,C.;Moro,L.;Tamassia,V.
  16. Chem.Drug. v.218 no.382 New developments in delayed-release delivery Hagan,K.H.
  17. Int.J.Pharm. v.17 no.273 Rectal absorption of flurbiprofen,ketoprofen and indomethacin in polyacrylic acid aqueous gel preparation in rats Kamiya,E.;Morimoto,K.;Takeeda,T.;Nakamoto,Y.;Morisaka,K.
  18. Oyo Yakuri v.20 no.833 Pharmacological studies of ketoprofen gel-type ointment (KPG)(1),Anti-inflammatory and analgesic activities of KPG by topical application Saita,M.;Takenoshita,H.;Taniguchi,Y.;Fruta,K.;Aoki,T.;Shimozono,Y.;Toda,A.;Mizoquchi,T.;Nakagawa,A.;Matsuura,K.;Tsuji,M.
  19. Oyo Yakuri v.29 no.969 Anti-inflammatory activity of ketoprofen cream in topical application Kyuki,K.;Tsurukmi,K.;Fujimura,H.
  20. Yakuri to Chiryo v.13 no.4115 Pharmacological studies of ketoprofen ointment Fujimura,H.;Hiramatsu,V.;Tamura,Y.;Maekawa,K.;Yokota,H.
  21. Yakuzaigaku. v.49 no.254 Effect of various additives on the skin permeation of ketoprofen from the film flrming transdermal formulation Yukawa,H.;Sugibayashi,K.;Morimoto,V.
  22. Int.J.Pharm. v.99 no.109 Effect of fatty acids and urea on the penetration of ketoprofen through rat skin Lim,C.L.;Kim,J.J.;Choi,S.C.;Shim,C.K.
  23. Pharm.Res. v.8 no.17 Terpenes and the lipid-protein-partitioning theory of skin peretration enhancement Williams,A.C.;Barry,B.W.
  24. Trans-dermal and Topical Dug Delivery Systems Ghosh,T.K.;Pfister,W.R.;Yum,S.I.