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

Abstract:

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 6 000 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 6 000 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 20 μL. 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 dispersion medium was water. The samples were tested continuously for 10 s and in parallel for 3 times.Results： The linear range of the concentration of bupivacaine was 4.58 ~ 45.81 μg·mL^-1 （r=0.999 9）. 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， 25.79 μm， and the RSD were 0.36%， 0.37%， 0.51% （n=3）， respectively.Conclusion： The encapsulation efficiency and particle size of batch 1 were similar to that of the original， while the encapsulation efficiency and particle size of batch 2 were significantly different from that of the original. The method is easy to operate， and it can distinguish the encapsulation efficiency and particle size distribution of bupivacaine polycystic liposomes with different processes.

Key words:  , Bupivacaine polycystic liposomes； , Encapsulation efficiency； , Particle size distribution； , Centrifuge； , Laser diffraction