摘要
依据《中华人民共和国兽药典》与《兽药研究技术指导原则汇编》等相关指导要求,对乙酰氨基阿维菌素(EPR)注射用缓释剂进行外观、黏度、pH、水分、密度、内毒素、含量及有关物质检测,建立EPR注射用缓释剂的质量标准并比较与参比制剂的药学等效性。含量与有关物质检测方法为使用ZORBAX Eclipse Plus C18柱(2.1 mm×50 mm,1.8μm);流动相:甲酸∶水∶乙腈(0.04 mL∶40 mL∶60 mL);流速:0.4 mL/min;检测波长:245 nm;柱温:35℃;进样量:2μL。在37℃,转速为50 r/min,0.5%SDS的PBS缓冲液条件下,比较自研与原研EPR注射用缓释剂的药学等效性。EPR注射用缓释剂外观澄清透明,平均相对黏度为46.45 mPa·s,平均pH为6.88,制剂中不含水分,密度为1.13 g/cm^(3),内毒素满足<0.1 EU/mL限度,含量>5%的标示值,有关物质的量<5%,检测结果均符合注射剂制剂要求;在同一条件下释放31 d后,自研与原研EPR注射用缓释剂累积释放量均超过80%,且自研与原研的相似因子(f2)值>50。自研EPR注射用缓释剂的检测结果均符合注射剂标准,自研与原研EPR注射用缓释剂具有药学等效。
Following the Veterinary Pharmacopoeia of the People’s Republic of China and The Compendium of Technical Guidelines for Research on Veterinary Drugs,the appearance,viscosity,pH,moisture,density,endotoxin,content and releated-substances tests were carried out on eprinomectin(EPR)extended-release injection agent to establish the quality standard and compare the pharmacological equivalence with the reference formulation.Content and related substances were determined on ZORBAX Eclipse Plus C18 column(2.1 mm×50 mm,1.8μm),mobile phase:formic acid∶water∶acetonitrile(0.04 mL∶40 mL∶60 mL);Flow rate:0.4 mL/min;Detection wavelength:245 nm;Column temperature:35℃;Injection volume:2μL.The pharmacological equivalence of the agent(f2 value)was calculated by comparing the release degree under the conditions of PBS buffer of 0.5%SDS at 37℃and the rotation speed of 50 r/min.After testing,the appearance of EPR sustained-release injection agent was clear and transparent,the average relative viscosity was 46.45 mPa·s,the average pH was 6.88,the preparation did not contain water,the density was 1.13 g/cm^(3),the endotoxin met the limit of less than 0.1 EU/mL,the content was greater than the labeled value of 5%,the amount of the substance was less than 5%,the test results were all in line with the injectable preparation requirements.After 31 d of release under the same conditions,both self-research and the original EPR sustained-release injection agent release were more than 80%,and the f2 value of self-research and the original was more than 50.The test results of self-researched EPR sustained-release injection agent were all in accordance with the standard for injectable agents,and the self-researched and original EPR sustained-release injection agent were pharmacologically equivalent.
作者
耿响
刘希望
杨亚军
李剑勇
GENG Xiang;LIU Xiwang;YANG Yajun;LI Jianyong(Key Laboratory of New Animal Drug Project of Gansu Province, Key Laboratory of Veterinary Pharmaceutical Development,Ministry of Agriculture and Rural Affairs of the People’s Republic of China,Lanzhou Institute of Husbandry and Pharmaceutical Science of CAAS,Lanzhou 730050,China)
出处
《中国畜牧兽医》
CAS
北大核心
2021年第3期1054-1063,共10页
China Animal Husbandry & Veterinary Medicine
基金
国家重点研发计划专项(2016YFD0501306)。
