Browse > Article

Preparation and Evaluation of Propofol Microemulsion for Parenteral Use  

이종화 (충남대학교 약학대학)
박선영 (충남대학교 약학대학)
김동우 (충남대학교 약학대학)
조미현 (충남대학교 약학대학)
조인숙 (충남대학교 약학대학)
이계원 (건양대학교)
박목순 (충남대학교 약학대학)
지웅길 (충남대학교 약학대학)
Publication Information
YAKHAK HOEJI / v.46, no.5, 2002 , pp. 337-342 More about this Journal
Abstract
Propofol(2,6-diisopropyl phenol) is a phenol derivative that is chemically distinct from other intravenous sedative hypnotics. It has been extensively used as a short term anesthetic agent, because of the rapid onset and short duration of action. Propofol microemulsion system was prepared with different concentrations of ethyl oleate, $Solutol^{(R)}$ HS 15 and $Kollidon^{(R)}$ 17 PF. Propofol microemulsions were studied by transmittance, viscosity, particle size, in vitro release and pharmacokinetics. The range of transmittance of A group with 4% ethyl oleate and that of B group with 5% ethyl oleate were 92.6~95.1 and 91.3~94.2%, respectively. Transmittance 1~2% decreased as concentration of $Kollidon^{(R)}$ 17 PF was increased and increased 0.8~3.3% when 10 times diluted with normal saline. The viscosity of A and B group were in the range of 3.9~4.1 mPaㆍsec and 4.4~5.3 mPaㆍsec, respectively. The particle sizes of A and B group increased as amount of $Kollidon^{(R)}$ 17 PF. Also, release of propofol was slowly increased as the amount of $Kollidon^{(R)}$ 17 PF was increased. Propofol plasma concentration by i.v injection showed 2-compartment model. Pharmacokinetics of A-5 was similar to that of commercial emuision(POFOL).
Keywords
Propofol; microemulsion; pharmacokinetics;
Citations & Related Records
연도 인용수 순위
  • Reference
1 Sarciaux, J. M., Acar, L. and Sado, P. A. : Invited Review : Using microemulsion formulations for oral drug delivery of therapeutic peptides, Int. J. Pharm. 120(2), 127 (1995)
2 Yegareh, M. H. and Ramzan, L. : Determination of propofol in rat whole blood and plasma by high performance liquid chromatography, J Chromatogr. B 691, 478 (1997)
3 Ghiani, C. A., Tuligi, G., Maciocco, E., Serra, M., Sanna, E. and Biggio, G. : Biochemical evaluations of the effects of loreclezole and propofol on the GABA(A) receptor in rat brain, Biochem. Pharmacol. 51(11), 1527 (1996)
4 Muhannad, J.and Bernd, W. : The stabilization of parenteral fat emulsion using non-ionic ABA copolymer surfactant, Int. J. Pharm. 174, 29 (1998)
5 Lehner, D., Lindner, H. and Glatter, O. : Determination of the translational and rotational diffusion coefficients of rodlike particles using depolarized dynamic light scattering, Langmuir 16(4), 1689 (2000)
6 Kanto, J. and Gepts, E. : Pharmacokinetic implications for the clinical use of propofol, Clin. Pharmacokinet. 17(5), 308 (1989)
7 Vree, T. B., Lagerwerf, A. J. and Bleeker, C. P. : Direct high-performance liquid chromatography determination of propofol and its metabolite quinol with their glucuronide conjugates and preliminary pharmacokinetics in plasma and urine of man, J. Chromatogr. B 721, 217 (1999)
8 Mark, S. L. and Rennie, C. H. : Propofol : A review of its pharmacodynamic and pharmacokinetic properties and use as an intravenous anesthetic, Drugs 35, 334 (1988)
9 Laia, CAT., Brown, W., Almgren, M. and Costa, SMB. : Light scattering study of water-in-oil AOT microemulsions with poly(oxy)ethylene, Langmuir 16(2), 465 (2000)
10 Sandeep, D. and Ebling, W. F. : Formulation-dependent Pharmacokinetics and Pharmacodynamics of Propofol in Rat, J. Pharm. Pharmacol. 50, 37 (1998)