A novel, lipid-free nanodispersion formulation of propofol and its characterization
A novel, lipid-free nanodispersion formulation of propofol and its characterization
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DOI：
10.1007/s11095-004-1872-0
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发表时间：
2005-03-01
影响因子：
3.7
通讯作者：
Gardner, CR
中科院分区：
文献类型：
--
作者：
Chen, HM;Zhang, Z;Gardner, CR
目的。丙泊酚是一种广泛使用的麻醉剂，具有非常理想的快速“起效”和“失效”作用。它目前被配制成脂质乳剂，已知这种乳剂会促进微生物生长。在本研究中，对一种新型的无脂质丙泊酚纳米分散制剂进行了特性研究。
方法。对该制剂的物理和化学稳定性、与红细胞的体外相容性以及抗菌效果进行了评估。在大鼠体内对该制剂的药代动力学和药效学特性进行了评估。
结果。我们的数据表明，这种无脂质制剂在物理和化学上是稳定的。与商业乳剂制剂得普利麻相比，它对红细胞造成的溶血更少，并且具有更强的抗菌活性。此外，该无脂质制剂在大鼠体内显示出与得普利麻相似的药理作用。
结论。这种新型的无脂质制剂在体外性能上有所改善，同时不影响体内效果，因此是丙泊酚一种有前景的新替代物。
Purpose. Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized.Methods. The formulation was evaluated for its physical and chemical stability, in vitro compatibility with red blood cells, and its antimicrobial effectiveness. In vivo pharmacokinetic and pharmacodynamic properties of the formulation were evaluated in rats.Results. Our data suggest that this lipid-free formulation is physically and chemically stable. Compared to the commercial emulsion formulation Diprivan, it causes less hemolysis with red blood cells and has improved antimicrobial activity. In addition, the lipid-free formulation demonstrates similar pharmacological effects to Diprivan in rats.Conclusions. This novel, lipid-free formulation exhibits improved in vitro properties without compromising in vivo effects, therefore representing a promising new alternative for propofol.