布比卡因多囊脂质体的包封率及粒径测定研究  

Determination of Encapsulation Efficiency and Particle Size of Bupivacaine Polycystic Liposomes

作　　者：彭玉帅 郭文娣 孙长迎 陈华[1] 尹利辉[1] PENG Yushuai;GUO Wendi;SUN Changying;CHEN Hua;YIN Lihui(National Institutes for Food and Drug Control,Beijing 102629,China;Yantai University,Shandong Yantai 264000,China)

机构地区：[1]中国食品药品检定研究院,北京102629 [2]烟台大学,山东烟台264000

出　　处：《中国医药导刊》2025年第1期41-46,共6页Chinese Journal of Medicinal Guide

基　　金：中国食品药品检定研究院中青年发展研究基金(2023A5)。

摘　　要：目的:测定两种不同工艺的布比卡因多囊脂质体仿制药和原研药的包封率及粒径分布,评估两种不同工艺的仿制产品和原研产品的区别,为后续该产品的一致性评价提供参考依据。方法:采用直接离心法加超滤离心法测定3种产品的包封率,直接离心法离心转速为6000 rpm,离心时间为10 min,而后再取直接离心法的上清液进行超滤离心,离心转速为6000 rpm,离心时间为20 min,使用HPLC法对布比卡因进行检测,以Waters XBridge C18为色谱柱,以0.02 mol·L^(-1)磷酸二氢钠缓冲溶液(pH=5.0)-乙腈(75∶25)为流动相,检测波长为240 nm,流速为1.5 mL·min^(-1);柱温为35℃;进样量为20μL。采用激光衍射法进行粒径大小和分布的测定,样品溶液的遮光率为15%,搅拌速率为80 rpm,样品池尺寸2 mm,分散介质为水,测试时间为10 s,样品平行测试3次。结果:HPLC检测包封率样品的方法中,布比卡因的质量浓度线性范围为4.58~45.81μg·mL^(-1)(r=0.9999),日内精密度RSD为0.27%(n=6),日间精密度为0.16%(n=3),重复性为0.60%(n=6),回收率为100.88%,RSD为2.67%(n=6)。样品1、样品2和原研产品包封率结果分别为86.52%、89.74%和86.91%。样品1、样品2和原研产品的中值粒径(X50)分别为25.35、22.65、25.79μm,RSD分别为0.36%、0.37%、0.51%(n=3)。结论:样品1的包封率和粒径大小与原研相似,而样品2的包封率和粒径与原研样品存在显著性差别,所建方法简单快捷,可以区分不同工艺的布比卡因多囊脂质体的包封率及粒径分布。Objective:To determine the encapsulation efficiency and particle size distribution of bupivacaine polycystic liposome generic with different processes and original.Evaluate the difference between the two different processes of the generic products and the original product,in order to provide reference for the consistency evaluation of the products in the future.Methods:The encapsulation efficiency of the three products was determined by direct centrifugal and ultrafiltration centrifugal method.The centrifugal speed of the direct centrifugal was 6000 rpm and the centrifugal time was 10 min.Then the supernatant of the direct centrifugal method was taken for ultrafiltration centrifugation,the centrifugal speed was 6000 rpm and the centrifugal time was 20 min.The determination was performed on HPLC with the column of Waters XBridge C18 and 0.02 mol·L^(-1) sodium dihydrogen phosphate buffer solution(pH=5.0)-acetonitrile(75∶25)as mobile phase.The detection wavelength was 240 nm and the flow rate was 1.5 mL·min^(-1).The column temperature was 35℃and the injection volume was 20μL.The particle size and its distribution of the three products were determined by laser diffraction method.The shading rate of the sample solution was 15%and the stirring rate was 80 rpm.The sample pool size was 2 mm and the dis-persion medium was water.The samples were tested continuously for 10 s and in parallel for 3 times.Results:The linear range of the con-centration of bupivacaine was 4.58~45.81μg·mL^(-1)(r=0.9999).The RSD of intra-day and inter-day precision were 0.27%(n=6)and 0.16%(n=3),respectively.The RSD of repeatability was 0.60%(n=6)and the recovery was 100.88%,and the RSD was 2.67%(n=6).The encapsulation efficiency of batch 1,batch 2 and the original product were 86.52%,89.74%and 86.91%,respectively.The median particle size(X50)of batch 1,batch 2 and the original product were 25.35,22.65,25.79μm,and the RSD were 0.36%,0.37%,0.51%(n=3),respectively.Conclusion:The encapsulation efficiency and particle size of batch 1 were sim

关 键 词：布比卡因多囊脂质体 包封率 粒径分布 离心 激光衍射 

分 类 号：R917[医药卫生—药物分析学]