Journal of Pharmaceutical Investigation

  • 제38권5호
  • /
  • Pages.331-334
  • /
  • 2008
  • /
  • 2093-5552(pISSN)
  • /
  • 2093-6214(eISSN)
한국약제학회 (The Korean Society of Pharmaceutical Sciences and Technology)
권호 표지
DOI QR코드

DOI QR Code

Pharmacokinetics and Oral Bioavailability of Paclitaxel Microemulsion in Rats

  • 발행 : 2008.10.20
PDF 다운로드
⟨ 이전 논문 다음 논문 ⟩

초록

The objectives of this study were to formulate oral paclitaxel microemulsion and to compare the bioavailability of paclitaxel in the microemulsion formulation from the commercially available $Taxol^{(R)}$ formulation. Paclitaxel microemulsion was formulated with much less amount of Cremophor $EL^{TM}$ as compared with $Taxol^{(R)}$ to reduce severe adverse reactions produced by Cremophor $EL^{TM}$. The area under the plasma concentration-time curve from 0 hr to 24 hr ($AUC_{0-24}$), maximum plasma concentration ($C_{max}$), and relative bioavailability of palcitaxel microemulsion were increased as compared with $Taxol^{(R)}$ after oral administration. The time required to reach $C_{max}\;(T_{max})$ of palcitaxel microemulsion was significantly shorter than $Taxol^{(R)}$ following oral administration. These results suggest the faster intestinal absorption and the enhanced oral bioavailability of paclitaxel in the microemulsion formulation.

키워드

참고문헌

  1. J.S. Choi, H.K. Choi and S.C. Shin, Enhanced bioavailability of paclitaxel after oral coadministration with flavone in rats, Int. J. Pharm., 275, 165-170 (2004) https://doi.org/10.1016/j.ijpharm.2004.01.032
  2. M. Martin, J. Catalin, M.F. Blachon and A. Durand, Assay of paclitaxel (Taxol) in plasma and urine by high-performance liquid chromatography, J. Chromatogr. B., 709, 281-288 (1998) https://doi.org/10.1016/S0378-4347(98)00060-7
  3. S. Yang, R.N. Gursoy, G. Lambert and S. Benita, Enhanced oral absorption of paclitaxel in a novel self-microemulsifying drug delivery system with or without concomitant use of Pglycoprotein inhibitors, Pharm. Res., 21, 261-270 (2004) https://doi.org/10.1023/B:PHAM.0000016238.44452.f1
  4. G.J. Fetterly and R.M. Straubinger, Pharmacokinetics of paclitaxel-containing liposomes in rats, AAPS PharmSci., 5, E32, 1-11 (2003)
  5. J.S. Woo, C.H. Lee, C.K. Shim and S.J. Hwang, Enhanced oral bioavailability of paclitaxel by coadministration of the P-glycoprotein inhibitor KR30031, Pharm. Res., 20, 24-30 (2003) https://doi.org/10.1023/A:1022286422439
  6. J.A. Straub, D.E. Chickering, J.C. Lovely, H. Zhang, B. Shah, W.R. Waud and H. Bernstein, Intravenous hydrophobic drug delivery: a porous particle formulation of paclitaxel (AI-850), Pharm. Res., 22, 347-355 (2005) https://doi.org/10.1007/s11095-004-1871-1
  7. R.T. Dorr, Pharmacology and toxicology of cremophor EL diluent, Ann. Pharmacothera., 28, S11-S17 (1994) https://doi.org/10.1177/10600280940280S503
  8. Y. Dong and S.S. Feng, Poly (D.L-lactide-o-glycolide)/montmorillonite nanoparticles for oral delivery of anticancer drugs, Biomaterials, 26, 6068-6076 (2005) https://doi.org/10.1016/j.biomaterials.2005.03.021
  9. T. Cresteil, B. Monsarrat, P. Alvinerie, J.M. Treluyer, I. Vieira and M. Wright, Taxol metabolism by human liver microsomes : identification of cytochrome P450 isozymes involved in its biotransformation, Cancer Res., 54, 386-392 (1994)
  10. G.A. Fisher and B.I. Sickic, Clinical studies with modulators of multidrug resistance, Hematol. Oncol. Clin. North Am., 9, 363-382 (1995) https://doi.org/10.1016/S0889-8588(18)30099-6
  11. S. Charman, W. Charman, M. Rogge, T. Wilson, F. Dutko and C. Pouton, Self-emulsifying drug delivery systems: formulation and biopharmaceutics evaluation of an investigations lipophilic compound, Pharm. Res., 9, 87-93 (1992) https://doi.org/10.1023/A:1018987928936
  12. P.P. Constantinides, J.P. Scalart, C. Lancaster, J. Marcello, G. Marks, H. Ellens and P.L. Smith, Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycetides, Pharm. Res., 11, 1386-1390 (1994)
  13. J. Kovarik, E. Muelle, J. Van Bree, W. Tetzloff and K. Kutz, Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation, J. Pharm. Sci., 83, 444-446 (1994) https://doi.org/10.1002/jps.2600830336
  14. N. Shah, M. Carvajal, C. Patel, M. Infeld and A. Malick, Selfemulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs, Int. J. Pharm., 106, 15-23 (1994) https://doi.org/10.1016/0378-5173(94)90271-2
  15. B. Matuszewska, L. Hettrick, J. Bondi and D. Storey, Comparative bioavailability of L-683, 453, a 5a-reductase inhibitor, from a self-emulsifying drug delivery system in beagle dogs, Int. J. Pharm., 136, 147-154 (1996) https://doi.org/10.1016/0378-5173(96)04496-1
  16. P.K. Ghosh, R.J. Majithiya, M.L. Umrethia and R.S.R. Murthy, Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability, AAPS PharmSciTech., 7, Article 77, E1-E6 (2006)
  17. S.H. Lee, S.D. Yoo, and K.H. Lee, Rapid and sensitive determination of paclitaxel in mouse plasma by high-performance liquid chromatography, J. Chromatogr. B., 724, 357-363 (1999) https://doi.org/10.1016/S0378-4347(98)00566-0
  18. M.M. Malingre, J.H.M. Schellens, O. Van Tellingen, M. Ouwehand, H.A. Bardelmeijer, H. Rosing, F.J. Koopman, S.E. Jansen, M.E. Schot, W.W. Ten Bokkel Huinink and J.H. Beijnen, The co-solvent cremophor EL limits absorption of orally administered paclitaxel in cancer patients, Br. J. Cancer, 85, 1472-1477 (2001) https://doi.org/10.1054/bjoc.2001.2118
  19. F. Kees, M. Bucher, F. Schweda, H. Gschaidmeier, J. Burhenne, G. Mikus and L. Faerber, Comparative bioavailability of the microemulsion formulation of cyclosporine with a generic dispersion formulation in young healthy male volunteers, Ther. Drugmonit, 28, 312-320 (2006) https://doi.org/10.1097/01.ftd.0000211804.89440.74