Date Abhijit A, Nagarsenker Mangal S
Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E.), Mumbai 400098, India.
AAPS PharmSciTech. 2008;9(1):138-45. doi: 10.1208/s12249-007-9023-7. Epub 2008 Jan 19.
The objective of this investigation was to evaluate the potential of the microemulsions to improve the parenteral delivery of propofol. Pseudo-ternary phase diagrams were plotted to identify microemulsification region of propofol. The propofol microemulsions were evaluated for globule size, physical and chemical stability, osmolarity, in vitro hemolysis, pain caused by injection using rat paw-lick test and in vivo anesthetic activity. The microemulsions exhibited globule size less than 25 nm and demonstrated good physical and chemical stability. Propofol microemulsions were slightly hypertonic and resulted in less than 1% hemolysis after 2 h of storage with human blood at 37 degrees C. Rat paw-lick test indicated that propofol microemulsions were significantly less painful as compared to the marketed propofol formulation. The anesthetic activity of the microemulsions was similar to the marketed propofol formulation indicating that they do not compromise the pharmacological action of propofol. The stability studies indicated that the microemulsions were stable for 3 months when stored at 5 +/- 3 degrees C. Thus, microemulsions appeared to be an interesting alternative to the current propofol formulations.
本研究的目的是评估微乳剂改善丙泊酚肠胃外给药的潜力。绘制了伪三元相图以确定丙泊酚的微乳化区域。对丙泊酚微乳剂进行了粒径、物理和化学稳定性、渗透压、体外溶血、采用大鼠舔爪试验评估的注射引起的疼痛以及体内麻醉活性等方面的评估。微乳剂的粒径小于25nm，并且表现出良好的物理和化学稳定性。丙泊酚微乳剂呈轻度高渗，在37℃与人血储存2小时后溶血率低于1%。大鼠舔爪试验表明，与市售丙泊酚制剂相比，丙泊酚微乳剂引起的疼痛明显减轻。微乳剂的麻醉活性与市售丙泊酚制剂相似，表明它们不会损害丙泊酚的药理作用。稳定性研究表明，微乳剂在5±3℃储存时3个月内稳定。因此，微乳剂似乎是当前丙泊酚制剂的一个有趣替代物。
