一种新型的、无脂质的丙泊酚纳米分散制剂及其特性。
A novel, lipid-free nanodispersion formulation of propofol and its characterization.
作者信息
Chen Hongming, Zhang Zhong, Almarsson Orn, Marier Jean-Francois, Berkovitz Dina, Gardner Colin R
机构信息
TransForm Pharmaceuticals, Inc., 29 Hartwell Avenue, Lexington, Massachusetts 02421, USA.
出版信息
Pharm Res. 2005 Mar;22(3):356-61. doi: 10.1007/s11095-004-1872-0.
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.
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消退作用。它目前被制成脂质乳剂，而脂质乳剂已知会支持微生物生长。在本研究中，对一种新型的无脂质纳米分散体制剂的丙泊酚进行了表征。
方法
评估了该制剂的物理和化学稳定性、与红细胞的体外相容性以及其抗菌效果。在大鼠中评估了该制剂的体内药代动力学和药效学特性。
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。与市售乳剂配方得普利麻相比，它对红细胞的溶血作用较小，并且具有改善的抗菌活性。此外，无脂质制剂在大鼠中表现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不影响体内效果的情况下表现出改善的体外特性，因此代表了丙泊酚一种有前景的新替代品。
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