Study On Preparation And Quality Standard Of Sustained Release Microsphere For Injection

This subject study on preparation and prescription of the Ivermectin(IVM) microspheres, and the research prepared the injection of the microspheres and established its quality control standards. provide reference and guidance for the production of the injection. Establish a method for determining the content of Ivermectin in the sustained-release microspheres. Optimization the preparation process of sustained-release microspheres by using response surface methodology, then used the orthogonal experiment to optimizing the suspension systemy, and research the in vitro release of the injection. According to the "China Veterinary Pharmacopoeia" method to study the quality of the injection, Preliminary study on toxicity of Ivermectin sustained-release microspheres injection, through the acute toxicity test and sub chronic toxicity test. Finally, make a quality standard for the injection.Established a method for determining the content of ivermectin sustained-release microspheres of HPLC ivermectin; The results suggested that the optimal microspheres preparation condition was 651r/min of stirring speed, 7 : 16 of the mass ratio and 1.47% of Poly(vinyl alcohol)(PVA) mass concentration, and under these conditions the drug loading rate was 29.4%, The optimal suspension system was that the particle diameter was d ≤ 80 μm, and the mass fractions of the microspheres, Tween 20 and sodium carboxymethyl cellulose(SCMC) were 2.5%, 1.5% and 1% respectively. The effective component stably releases in 20 d in vitro which achieves sustained releasing effect. The determination of ivermectin sustained-release microsphere injection on mice LD50 was 14.61 m L/kg·BW, and its 95% confidence limit is 11.58 m L/kg·BW ~ 18.75 m L/kg·BW, the Subchronic Toxicity test results showed that the in vivo injection on rats with cumulative toxicity. Finally, set up the quality standard for the injection.