Acta Chim Slov. 2020 Mar;67(1):179-188.
Despite of the clinical, scientific, and commercial development, many patients complain about pain on the intravenous injection of propofol. Present work was undertaken to develop a stable multi-dose propofol nano-emulsion using 32 full factorial design which is supposed to be associated with less anticipated pain during intravenous administration. Propofol was incorporated in the mixture of disodium edetate, sodium oleate, thioglycerol, glycerol, egg lecithin, soyabean oil and medium chain triglyceride oil, and homogenization was continued at controlled temperature of 20 °C. The product did not show any significant change in visible extraneous particulate matter, pH, osmolality, bacterial endo-toxin, sterility, high performance liquid chromatography (HPLC) their stability and impurities after exposing at 40 °C for 3 and 6 months. Homogenization at 850 bar pressure of 30 min duration produced 174 nm particles with -53.6 mV zeta potential indicating its stability.
尽管在临床、科学和商业方面都取得了发展，但仍有许多患者在静脉注射丙泊酚时会感到疼痛。本研究采用 32 个全因子设计，开发了一种稳定的多剂量丙泊酚纳米乳剂，据称这种乳剂在静脉给药时疼痛的发生率较低。丙泊酚被加入到乙二胺四乙酸二钠、油酸钠、硫代甘油、甘油、蛋黄卵磷脂、豆油和中链甘油三酯油的混合物中，并在 20°C 的控制温度下继续进行均质化处理。该产品在 40°C 下暴露 3 个月和 6 个月后，在可见异物、pH 值、渗透压、细菌内毒素、无菌、高效液相色谱（HPLC）及其稳定性和杂质方面均未显示出任何显著变化。在 850 巴压力下均质 30 分钟可产生 174nm 的颗粒，其 Zeta 电位为-53.6mV，表明其稳定性。
