Formulation of Sustained-Release Tablets of Flurbiprofen

서방출성 플루르비프로펜 정제의 제제설계

  • Published : 1995.04.01

Abstract

Flurbiprofen, one of potent nonsteroidal antiinflammatory drugs, has several systemic side effects due to dose dumping effect following oral administration of its conventional solid dosage forms. To reduce these side effects and to sustain therapeutic concentration of the drug, matrix tablets of flurbiprofen were prepared and evaluated for sustained release from the tablets. The matrix tablets of flurbiprofen were prepared with Eudragit, Pluronic, (anhydrous) lactose and colloidal silicon dioxide employing two different preparation methods, wet granulation and direct compression. The dissolution rates of the tablets were evaluated using KP 2 method. Formulation factors that affected dissolution rates of flurbiprofen were the type and content of Eudragit, the type and content of Pluronic, and the tablet preparation method. Several formulations of the matrix tablets showed dissolution patterns close to the simulated profile using pharmacokinetic parameters of flurbiprofen.

Keywords

References

  1. Curr. Ther. Res. v.33 Flurbiprofen in rheumatoid arthritis: A long-term experience Marcolongo,R.;Giordano,N.;Fioravanti,A.;Benvenuti,C.;Longoni,A.
  2. Curr. Ther. Res. v.34 Multicentre study on effectiveness and safety of flurbiprofen versus alternative therapy in 738 rheumatic patients Benvenuti,C.;Longoni,L.
  3. Am. J. Med. v.80 no.Sup.3A Flurbiprofen in the treatment of ankylosing spondylitis: A comparison with indomethacin Lomen,P.L.;Turner,L.F.;Lamborn,K.R.;Brinn,E.L.
  4. Int. J. Clin. Pharmacol. Ther. Toxicol. v.27 Singel-dose pharmacokinetics of flurbiprofen granules and tablets in healthy volunteers Benvenuti,C.;Gambaro,V.;Lodi,E.;Scaroni,C.;Bandi,G.;Valenti,M.
  5. Am. J. Med. v.80 no.Sup.3A Pharmacokinetics of flurbiprofen Kaiser,D.G.;Brooks,C.D.;Lomen,P.L.
  6. Br. J. Clin. Pract. no.Sup.9 Study of the gastric mucosa in rheumatic patients before and after the administration of flubiprofen Vasconcelos-Teixeira,A.;Pocas,L.;Serrao,D.
  7. Drugs v.18 Flubiprofen: A review of its pharmacological properties and therapeutic uses in rheumatic diseases Brogden,R.N.;Hell,R.C.;Speight,T.M.;Avery,G.S.
  8. Acta Pharm. Technol. v.36 Effects of additives on flurbiprofen controlled release preparations Efentakis,M.;Al-Hmoud,H.;Choulis,N.
  9. Int. J. Pharm. v.70 The influence of surfactants on drug release from a hydrophobic matrix Efentakis,M.;Al-Hmoud,H.;Buckton,G.;Rajan,Z.
  10. Int. J. Pharm. v.85 no.R1 Release kinetics of flurbiprofen from hydrophobic heterogeneous matrices containing surfactants Efentakis,M.
  11. Technical Data on Pluronic Polyols BASF Wyandotte Corp.
  12. Int. J. Pharm. v.21 Surface and transport properties of acrylic ploymers influencing drug release from porous matrices CArli,F.;Capone,G.;Colombo,I.;Magarotto,L.;Motta,A.
  13. J. Pharm. Sci. v.77 Stereoselective pharmacokinetics of flurbiprofen in humans and rats Jamali,F.;Berry,B.W.;Tehrani,M.R.;Russell,A.S.
  14. Eur. J. Clin. Pharmacol v.27 Pharmacokinetics of oral and rectal flurbiprofen in children Scaroni,C.;Mazzoni,P.L.;Amico,E.D.;Benvenuti,C.;Hind I.D.
  15. Biopharm. Drug Dispos. v.8 Pharmacokinetics of flurbiprofen in men Ⅰ. Area/dose relationship Szpunar,G.J.;Albert,K.S.;Bole,G.G.;Dreyfus,J.N.;Lockwood,G.F.;Wagner,J.G.
  16. Pharmacokinetics(2nd Ed.) Gibaldi,M.;Perrier,D.
  17. Drug Dev. Ind. Pharm. v.16 Polyacrylate(Eudragit retard) microspheres for oral controlled release of nifedipine.Ⅰ. Formulation design and process optimization Barkai,A.;Pathak,Y.V.;Benita,S.
  18. Drug Dev. Ind. Pharm. v.10 A new approach for controlling the release rate of pheniramine aminosalicylate via solid dispersion in different types of Eudragit El-Fattah,S.A.;Salib,N.N.;El-Massik,M.
  19. Drug Dev. Ind. Pharm. v.17 In-vitro evalution of sustained-release dyphylline tablets EL-said,Y.;Hashem,F.
  20. Int. J. Pharm. v.74 The influence of surfactants on drug release from acrylic matrices Buckton,G.;Efentakis,M.;Al-Hmoud,H.;Rajan,Z.