Preparation and Evaluation of Flurbiprofen- and Flurbiprofen Axetil-loaded Microemulsion

플루비프로펜 및 플루비프로펜 악세틸이 함유된 마이크로에멀젼의 제조 및 평가

  • Published : 1997.10.01

Abstract

Flurbiprofen- and flurbiprofen axetil-loaded microemulsions composed of soybean oil, poloxamer 407, glycerine and water were prepared by generator-type homgenizer and ultrasoni c probe system. The particle size of microemulsions was measured by the dynamic light scattering method. The pharmacokinetics and organ distribution of flurbiprofen were investigated after intravenous injection of flurbiprofen solution, flurbiprofen-loaded microemulsion and flurbiprofen axetil-loaded microemulsions equivalent to 10mg/kg of flurbiprofen to rats. Blood samples were collected from the anterior ciliary artery of rats for 24hr, and flurbiprofen in plasma and organs was analyzed by HPLC. Stable microemulsions were prepared. Even though there is a little change in droplet size just after the preparation, no creaming and no separation were occured during the storage period for 6 months at 4, 21, 37 and 45$^{\circ}C$. Pharmacokinetic parameters and organ distribution of flurbiprofen after intravenous injection of flurbiprofen- and flurbiprofen axetil-loaded microemulsions emulsified with poloxamer 407 were not significantly different from those of commercial lipid microemulsion emulsified with lecithin. Therefore, it is concluded that flurbiprofen- and flurbiprofen axetil-loaded microemulsion prepared with poloxamer 407 could be used as a parenteral formulation.

Keywords

References

  1. J. Pharm. Sci. v.83 Structural studies of commercial fat emulsions used in parenteral nutrition. Jianmin L.;Caldwell, K. D.
  2. Pharm. Res. v.11 Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating mediumchain glycerides. Constantinides, P. P.;Scalart, J.-P.;Lancaster, C.;Marcello, J.;Marks, G.;ellens, H.;Smith, P. L.
  3. J. Pharm. Sci. v.82 Investigation of the particle size distribution of model intravenous emulsion. Westesen, K.;Wehler, T.
  4. Int. J. Pharm. v.23 the influence of emulsifying agents on the phagocytosis of lipid emulsions by macrophages. Davis, S. S.;Hansrani, P.
  5. Int. J. Pharm. v.108 Pharmacokinetics and tissue distribution of methotrexate after intravenous injection of differently charged liposome-entrapped methotrexate to rats. Kim, C.-K.;Lee, M.-K.;Han, J.-H.;Lee, B. J.
  6. Int. J. Pharm. v.42 A novel use of intralipid for the parenteral delivery perilla ketone (NSC-348407), an investigational cytotoxic drug with a high affinity for plastic. Paborji, M.;Riley, C. M.;Stella, V. J.
  7. Int. J. Pharm. v.12 Blood clearance and organ disposition of intravenously administered colloidal particles. The effect of particle size, nature and shape. Illum, L.;Davis, S. S.;Wilson, C. G.;Thomas, N. W.;Frier, M.;Hardy, J. G.
  8. Int. J. Pharm. v.83 Differenes in the molecular weight profile of poloxamer 407 affect its ability to redirect intravenously administered colloids to the marrow. Porter, C. J. H.;Moghimi, S. M.;Davies, M. C.;Davis, S. S.;Illum, L.
  9. Int. J. Pharm. v.100 Effects on splenic, hepatic, hematological, and growth parameters following high-dose poloxamer 407 administration to rats. Johnston, T. P.;Beris, H.;wout, Z. G.;Kennedy, J. L.
  10. Int. J. Pharm. v.29 The effect of hydrophilic coatings on the uptake of colloidal particles by liver and by peritoneal macrophages. Illum, L.;Hunneyball, I. M.;Davis, S. S.
  11. Microbiol. v.32 Phagocytosis as a surface phenomenon. Annu Rev. Van Oss, C. J.
  12. Int. J. Pharm. v.29 The effect of hydrophilic coatings on the uptake of colloidal particlesby the liver and by peritoneal macrophages. Illum, L.;Hunneyball, I. M.;Davis, S. S.
  13. Curr. Med. Res. Opin. v.5 Inhibition of prostaglandin synthesis and leucocyte migration by flurbiprofen. Adams, S. S.;Burrow, C. A.;Skeldon, N.;Tastes, D. B.
  14. The analysis of the polyoxyethylene-polyoxypropylene block copolymers Lutrol F-68 and Lutrol F-127 and their pharmaceutical application. DFC/en.8639 BASF Wyandotte Co. Report
  15. v.1 Pharmaceutical Dosage forms: disperse Systems. Lieberman, H. A.;Rieger, M. M.;Banker, G. S.