乙酰氨基阿维菌素注射用缓释剂质量标准与药学等效研究

doi:10.16431/j.cnki.1671-7236.2021.03.030

摘要/Abstract

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，1.8 μm）；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：2 μL。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/cm³，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。

关键词: 乙酰氨基阿维菌素(EPR); 质量标准; 药物释放; 药学等效

Abstract: 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,1.8 μm),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:2 μL.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/cm³,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.

Key words: eprinomectin (EPR); quality standard; drug release; pharmaceutical equivalence

中图分类号:

S859.7

耿响, 刘希望, 杨亚军, 李剑勇. 乙酰氨基阿维菌素注射用缓释剂质量标准与药学等效研究[J]. 中国畜牧兽医, 2021, 48(3): 1054-1063.

GENG Xiang, LIU Xiwang, YANG Yajun, LI Jianyong. Study on Quality Standard and Pharmaceutical Equivalence of Eprinomectin Sustain-release Injections[J]. China Animal Husbandry and Veterinary Medicine, 2021, 48(3): 1054-1063.

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