Preparation Of Cetiour-Allicin Liposomes And Study Of Its Pharmacokinetics In Rats

This paper aims to present the Preparation of Ceftiofur-Allicin Liposomes.To select the preparative method of Liposomes and take the envelopment rate as the index.According to orthogonal design,the optimum technological condition of A₂B₃C₂D is obtained:which was established as follows:the proportion of cholesterol and lecithin in weight was l:2,the proportion of Ceftiofur and Allicin in weight was l:2,and that medicine and liqids in weight was l:10,the ratio to volume of organic phase and water phase was l:3.To select the assay method of the envelopment rate.An RP-HPLC method was established The mobile phase consisted of methanol-water-acetic acid （80:20:0.2） with the flow rate of 1.0 ml-min^-1,the detector at 283 nm and the sample size in 10μL. The retention time of Ceftiofur （5.7±0.2min） > The retention time of Allicin （12.6±0.2min） and other impurity peak was separated fully under the chromatographic condition..Meanwhile on these grounds of this chromatographic condition it determined colour spectrum numerical value of the sample solution, which calculated density though propotional standard curve equation,and then calculated entrapment efficiency of liposomes by the followe quation.entrapment efficiency=（?）×100%The liposome is milk and not impurity in our eyes.The average rate of entrapment of Ceftiofurwas 37% and that Allicin was 86%.This paper is to study the pharmacokinetics of Liposomes of Ceftiofur and Allicin in the singleness,compatibility and their making medicines compatible for. An HPLC method was established.The mobile phase consisted of acetonitrile-water-tetrahydrofuran （70:27:3） （detecting Allicin） ,acetonitrile-water-trifluoroacetic acid （30:70:0.1） （detecting Ceftiofur） with the flow rate of 1.0ml·min^-1 and the detector at 242 nm and the sample size in 20μL. The retention time of Ceftiofur （8.9±0.2min） , The retention time of Allicin （11.8±0.2min） and other impurity peak was separated fully under the chromatographic condition. Then determination of pharmacokinetics parameters has been carried out by HPLC.BAPP2.0 analysis software is used to analyse these measured data,so we get the following pharmacokinetics results:Ceftiofur solution,Allicin solution,Ceftiofur and Allicin solution, Ceftiofur-Allicin liposomes.Half-life of the drug in Liposomes are bigger than singleness.Ka of the drug in Liposomes is obviously greater than Ke (Ka _ceftiofur=6.29 h^-1> Ke_ceftiofur =1.03 h^-1;Ka_Allicin=1.12 h^-1>Ke_Allicin=0.11 h^-1) ,and it is explained that drug sorption is prompt,and the absorption rate is greater than elimination rate in liposomes,making medicine reaching effective blood medicine promptly in the body and maintaining longer effective time.The result shows a evident sustained release property in Ceftiofur and Allicin liposomes.