Preparation and Evaluation of Propofol Microemulsion for Parenteral Use

마이크로에멀젼을 이용한 프로포폴 주사제의 개발 및 평가

  • Published : 2002.10.01

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).

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References

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