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Preparation and Evaluation of Propofol Microemulsion for Parenteral Use

Propofol(2,6-diisopropyl phenol) is a phenol derivative that is chemically distinct from other intravenous serdative 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 2.6-95.1 and 91.3∼94.2%, respective17: 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 mPa ·sec and 4.4∼5.3 mPa ·sec, 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 1.v injection showed 2-compartment model. Pharmacokinetics of A-5 was similar to that of commercial emulsion(POFOL).