YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Formulation and Pharmaceutical Properties of Transdermal Patch of Flurbiprofen

플루비프로펜 함유 경피 패취제의 제제설계 및 약제학적 성질

  • Published : 1999.08.01
Download PDF
⟨ Previous Next ⟩

Abstract

The purpose of this study is to prepare the adhesive type patch containing flurbiprofen, and to demonstrate the feasibility of flurbiprofen administration through the intact skin using adhesive type patch preparation. For this purpose, two pressure sensitive adhesives, Polyisobutylene(PIB) and $Gelva^{\circledR}737$, were selected from the chemical grade of polymers, and the adhesive type patches of flurbiprofen were prepared. The release rate of flurbiprofen from the PIB-based adhesive patch was higher than that from $Gelva^{\circledR}737$ based adhesive patch. The release rate of flurbiprofen from the PIB-based A-type patch with 1.0mm, 1.5mm or 2.0mm thicknesses followed the first order kinetics. In the skin permeation study, using male hairless mouse skin, a monophasic skin permeation profile was observed with 1% flurbiprofen loading dose. The inclusion of palmitic acid or SLS(0.25~0.5%) as an enhancer produced a remarkable enhancement in the skin permeation rate of flurbiprofen, and the percentile ratio of drug and enhancer appeared to be important for the effective enhancement. In the in vivo percutaneous absorption study, the plasma concentration of the optimal formulation was significantly (p<0.01) higher than that of the conventional cataplasma ($Bifen^{\circledR}$). These studies demonstrate a good feasibility of flurbiprofen administration through the intact skin using a transdermal patch, and show a possibility of the development of flurbiprofen patches.

Keywords

References

  1. J. Invest. Dermatol v.67 Precutaneous absorption; Controlled drug dilivery for topical or systemic therapy Shaw J. E.;Chandrasekaran S. K.;Camphell P.
  2. Drug. Metab. Rev v.8 Controlled topical delivery of drugs for systemic action Shaw J.;Chandrasekaran S. K.
  3. Br. J. Clin. Pharm v.21 Plasma and synovial fluid kinetics of flurbiprofen in rheumatiod arthritis Aarons L;Salisbury R.;Alam-Siddiol M.;Taylor L.;Gremman D. M.
  4. J. Clin. Pharmacol v.32 The pharma-cokinetics of flurbiprofen in younger and elderly patients with rheumatoid arthritis Kean W. E.;Antal E. J.;Grace E. M.;Cauvier R. H.;Rischke R. J.;Buchanan W. W.
  5. Drugs v.18 Flurbiprofen : A review of its pharmacological properties and therapeutic use in rheumatic diseases Brogden R. N.;Heel R. C.;Speight T. M.;Avery G. S
  6. J. Pharm. Sci v.74 Predictive relationships in the water solubility of salts of a nonsteroidal anti-inflammatory drug Anderson B. D.;Conradi R. A.
  7. Chem. Pharm. Bull v.18 Absorption and excretion of drugs, absorption of barbituric acid derivatives from rat stomach Kakemi K.;Arita T.;Hori T.;Konishi R.
  8. European Patent 0 328 806 A2 Estradiol transdermal delivery system Oliver, R.
  9. J. Pharm. Sci v.85 Controlled transdermal delivery of fentanyl : Characterizations of pressure-sensitive adhesives for matrix patch design Roy S. D.;Gutierrez M.;Flynn G. L.;Cleary G. W.
  10. Int. J. Pharm v.76 Effect of physicochemical properties of adhesive on the release, skin permeation and adhesiveness of adhesive-type transdermal drug delivery system (a-TDD) containing silicone-based pressure-sensitve adhesives Toddywala R. D.;Ulman K.;Walters P.;Chein Y. W.
  11. Int. J. Pharm v.82 Development of in vitro evaluation of griseofulvin gels using Franz diffusion cells Vlachou M. D.;Rekkas D. M.;Dallas P. P.;Choulis N. H.
  12. Int. J. Pharm v.82 In vitro release and permeation of levobunolol from various transdermal fromulations Ghosh T. K.;Chiago K.;C. S.;Gokhale R. D.
  13. Int. J. Pharm v.126 Effect of penetration enhancers of flurbiprofen permeation through rat skin Chi, S. C.;Park E. S.;Kim H.
  14. Pharma. Deevel. and Tech. v.1 no.3 Development of a transdermal patch of Methadone : In vitro Evaluation across hairless mouse and human cadaver skin Ghosh T. K.;Bagherian A.
  15. Int. J. Pharm v.88 Transdermal delivery of metoprolol Ⅰ : Comparison between hairless mouse and human cadaver skin and effect of n-decylmethyl sulfoxide Ghosh T. K.;Habib M. J.;Childs K.;AlexanderM.
  16. Int. J. Pharm v.43 Skin permeation enhancement by n-decylmethyl sulfoxide, effect of solvent systems and insights on mechanism of action Touitou E.
  17. Int. J. Pharm v.52 Unsaturated cyclic ureas as new non-toxic bioderadable transdermal penetration enhancers. Ⅱ. Evaluation study Wong O.;Tsuzuki N.;Ngheim B.;Kuehnhoff J.;Itoh T.;Masaki K.;J. Huntington;R. Konishi;J. H. Rytting;T. Higuchi
  18. Int. J. Pharm v.27 Effect of propylene glycol, Azone and n-decylemthyl sulfoxide on skin permeation kinetics of 5-fluoruracil Touitou E.;Abed L.
  19. Int. J. Pharm v.33 Enhancement of naloxone penetration through human skin in vitro using fatty acids, fatty alcohols, surfactants, sulfoxides and amides Aungst B. J.;Rogers N. J.;Shafter E.
  20. Inc. J. Pharm v.74 The influence of surfactants on drug release from acrylic matrices Buckton G.;Efentakis M.;Al-Hmoud H.;Rajan Z.
  21. Int. J. Pharm v.116 In vitro evaluation of series of Azone analogs as dermal penetration enhancers Ⅳ. Amines Michniak B. B.;Player M. R.;Godwin D. A.;Phillips C. A;Sowell Sr J. W.
  22. J. Pharm. Sci v.84 Tansdermal delovery of Metoprolol Ⅱ : In vitro skin permeation and bioavailability in hairless rats Goshi T. K.;Adir J.;Xiang S. L.;Onyilofur S.
  23. Chem. Pharm. Bull v.40 Release of sodium Guaiazurene-3-sulfonate from Polymer film dosage froms Danjo K.;Miyakawa Y.;Kitamura Y.;Otsuka A.
  24. J. Pharm. Sci v.80 Absorption of flurbiprofen through human buccal mucosa Gonzalez-Younes I.;Wagner J. G.;Gaines D. A.;Ferry J. J.;Hacceman J. M.
  25. J. Pharm. Sci v.80 no.6 Enhancing effect of pyrrolidone derivatives on transdermal penetration of 5-uracil, triamcinolone acetonide, indonetacin and flurbiprofen Sasaki H.;Kojima M.;Mori Y.;Nakamura J.;Shibasaki J.
  26. Transdermal drug delivery, developmental issues and research initiatives Hadgraft J.;Guy R. H.
  27. Transdermal Controlled Systemic Medications Chein Y. W.