Study On Preparation, Determination And Pharmacokinetics Of Ivermectins Sustained-release Injection

Object: Study on the long-acting and sustained-release preparation for preventing and curing parasitic diseases of livestock is the focus of world-wide research. With Ivermectins (IVM) being the raw materials, we plan to prepare IVM Sustained-release Injection with broad spectrum, high performance, safety and less effect on environment. And we hope to obtain a new type sustained-release IVM Injection, which has the advata-ges such as feasibility for producting, convenience for injecting, and can prevent and cure parasitic disease for three or four monthes only by taking it once. Method: 1) Preparing IVM sustained-release injection with IVM being the raw materials. 2) Determining the content of IVM in IVM sustained-release injection by HPLC-UV. 3) Determining IVM in plasma of sheep and researching pharmacokinetic in sheep body by HPLC after injecting in the lateral face of the neck at a dose of 10 mg/kg. Evaluating the sustained-release performance of the preparation. Results: 1) We obtained canary, clarify oily IVM sustained-release injection. 2) Sudan III as internal standard, establishing the method of determing IVM H2B1a in plasma of sheep by HPLC. The limited of determination of the method is 1.8 ng/ml. The outstanding characteristic of the method is that the cost of pretreatment is low and manipulation is simple. 3) Depending on C-T curves, the parameters of pharmacokinetic were estimated as follows: Tmax=8.0 d: Cmax=82.3 ng/ml; AUC=3642 ng/ml×d; MRT=45.9 d. Experimental result indicated that Ivermectins Sustained-release Injection has definite sustained -releasing effect no less than 4 months.