1. Technology of Yellow River institute， Zhengzhou 450063，China；2.Henan University College of Pharmacy， Kaifeng 475004， China；3.China Pharmaceutical University， Nanjing 210009，China
OBJECTIVE To prepare oleanolic acid intravenous emulsions and study its pharmacokinetics in rats. METHODS Oleanolic acid intravenous emulsion was prepared by two-step emulsification using high speed stirring-ultrasonic wave. The pharmaceutical properties including appearance，content，Ke，particle size，and Zeta potential were determined. Rats were i.v. injected with oleanolic acid intravenous emulsion or oleanolic acid solution via tail veins. The concentrations in rat plasma were assayed by high-performance liquid chromatography （HPLC）. The pharmacokinetic parameters were computed by 3P97 program package. RESULTS The droplets of oleanolic acid intravenous emulsion were almost spherical，The mean diameter was （176.0±3.8） nm，and Zeta potential was （-17.5±4.1） mV. The content of oleanolic acid intravenous emulsions was （87.8±1.8）%. The plasma pharmacokinetic process of the oleanolic acid intravenous emulsions obeyed a two-compartment model. t1/2β of oleanolic acid intravenous emulsions was （308.1±22.8） min，and AUC was （208.6±15.6） μg·min·mL-1， obviously higher than control preparation. CONCLUSION The intravenous emulsion has high content and even diameter. Its pharmacokinetic property has significant change with improved bioavailability.
CHEN Hong-xun;HE Ping;XU Zhi-jie;YOU Guo-ye;LIU Wn-lu;XIO Yn-yu.
Preparation of Oleanolic Acid Intravenous Emulsions and Its Pharmacokinetics in Rats[J]. Chinese Pharmaceutical Journal, 2011, 46(13): 1023-1026
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