Preparation of Oleanolic Acid Intravenous Emulsions and Its Pharmacokinetics in Rats

CHEN Hong-xun;HE Ping;XU Zhi-jie;YOU Guo-ye;LIU Wn-lu;XIO Yn-yu

Chinese Pharmaceutical Journal ›› 2011, Vol. 46 ›› Issue (13) : 1023-1026.

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PDF(792 KB)
Chinese Pharmaceutical Journal ›› 2011, Vol. 46 ›› Issue (13) : 1023-1026.

Preparation of Oleanolic Acid Intravenous Emulsions and Its Pharmacokinetics in Rats

  • CHEN Hong-xuan1,3,HE Ping2,XU Zhi-jie2,YOU Guo-ye2,LIU Wan-lu2,XIAO Yan-yu3
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Abstract

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.

Key words

oleanolic acid / intravenous emulsions / pharmacokinetics

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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

References


[1] HUANG D,DING Y,LI Y,et al. Anti-tumor activity of a 3-oxo derivative of oleanolic acid[J].Cancer Lett,2006,23(3):289-229.
[2] RAPHAEL T J,KUTTAN G. Effect of naturally occurring triterpenoids glycyrrhizic acid,ursolic acid,oleanolic acid and nomilin on the immune system[J]. Pharm Pharmacol,2003,10(8): 483-489.
[3] YOSHIMI N. Modifying effects of fungal and herb metabolites on azoxymethane-induced intestinal and herb metabolites on azoxymethaneinduced intestinal carcinogenesis in rats[J]. Jap Cancer Res,1992,8(3):1273-1278.
[4] SOMOVAL L I,SHODE F O,MIPANDO M,et al.Cardiotonic and antidysrhythmic effects of oleanolic and ursolic acids,methyl maslinate and uvaol[J]. Pharm Pharmacol,2004,11(10): 121-129.
[5] SOMOVA L O,NADAR A,RAMMANAN P. Cardiovascular antihyperlipidemic and antioxidant effects of oleanolic and ursolic acids in experimental hypertension[J]. Pharm Pharmacol,2003,10(5):115-121.
[6] FLAVIA A R, DE ANDRADE BARCALA C A M, DA SILVA FARIA M C,et al. Antimutagenicity of ursolic acid and oleanolic acid against doxorubicin-induced clastogenesis in Balb/c mice[J].Life Sci,2006,79(13):1268-1273.
[7] WANG D R. New research of oleanolic acid [J]. Tianjin Pharm(天津药学),2003,15(3):57-59.
[8] WANG L X,HAN G J,LIU W Y,et al. Chemical and pharmacological research of oleanolic acid [J]. J Pharm Practice(药学实践杂志),2001,19(2):104-107.
[9] TIAN L T,MA H,DU N S,et al. Pharmacological research of oleanolic acid[J]. China J Chin Mater Med(中国中药杂志),2002,27(12):882-884.
[10] WANG L X,HAN G J. Chemical and biological research of oleanolic acid[J]. J Pharm Practice(药学实践杂志),2001,19(2):104-107.
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