Peng Jie, Dong Wu-Jun, Li Ling, Xu Jia-Ming, Jin Du-Jia, Xia Xue-Jun, Liu Yu-Ling
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing City Key Laboratory of Drug Delivery Technology and Novel Formulations, Beijing 100050, China.
J Food Drug Anal. 2015 Dec;23(4):828-835. doi: 10.1016/j.jfda.2015.04.004. Epub 2015 May 19.
The effect of different high pressure homogenization energy input parameters on mean diameter droplet size (MDS) and droplets with > 5 μm of lipid injectable emulsions were evaluated. All emulsions were prepared at different water bath temperatures or at different rotation speeds and rotor-stator system times, and using different homogenization pressures and numbers of high-pressure system recirculations. The MDS and polydispersity index (PI) value of the emulsions were determined using the dynamic light scattering (DLS) method, and large-diameter tail assessments were performed using the light-obscuration/single particle optical sensing (LO/SPOS) method. Using 1000 bar homogenization pressure and seven recirculations, the energy input parameters related to the rotor-stator system will not have an effect on the final particle size results. When rotor-stator system energy input parameters are fixed, homogenization pressure and recirculation will affect mean particle size and large diameter droplet. Particle size will decrease with increasing homogenization pressure from 400 bar to 1300 bar when homogenization recirculation is fixed; when the homogenization pressure is fixed at 1000 bar, the particle size of both MDS and percent of fat droplets exceeding 5 μm (PFAT) will decrease with increasing homogenization recirculations, MDS dropped to 173 nm after five cycles and maintained this level, volume-weighted PFAT will drop to 0.038% after three cycles, so the "plateau" of MDS will come up later than that of PFAT, and the optimal particle size is produced when both of them remained at plateau. Excess homogenization recirculation such as nine times under the 1000 bar may lead to PFAT increase to 0.060% rather than a decrease; therefore, the high-pressure homogenization procedure is the key factor affecting the particle size distribution of emulsions. Varying storage conditions (4-25°C) also influenced particle size, especially the PFAT.
评估了不同高压均质能量输入参数对脂质注射乳剂的平均液滴直径（MDS）和直径大于5μm的液滴的影响。所有乳剂均在不同的水浴温度、不同的转速和转子-定子系统时间下制备，并使用不同的均质压力和高压系统再循环次数。使用动态光散射（DLS）方法测定乳剂的MDS和多分散指数（PI）值，并使用光阻/单颗粒光学传感（LO/SPOS）方法进行大直径尾部评估。使用1000巴的均质压力和七次再循环时，与转子-定子系统相关的能量输入参数不会对最终粒径结果产生影响。当转子-定子系统能量输入参数固定时，均质压力和再循环会影响平均粒径和大直径液滴。当均质再循环固定时，粒径将随着均质压力从400巴增加到1300巴而减小；当均质压力固定在1000巴时，MDS和超过5μm的脂肪滴百分比（PFAT）的粒径都会随着均质再循环次数的增加而减小，MDS在五个循环后降至173nm并保持该水平，体积加权PFAT在三个循环后将降至0.038%，因此MDS的“平台期”比PFAT出现得晚，当两者都处于平台期时产生最佳粒径。在1000巴下进行九次等过多的均质再循环可能导致PFAT增加到0.060%而不是减小；因此，高压均质程序是影响乳剂粒径分布的关键因素。不同的储存条件（4-25°C）也会影响粒径，尤其是PFAT。
