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MICRO-EMULSION PREPARATION WITH HIGH CONCENTRATION OF PROPHOPOL FOR ANESTHESIC APPLICATIONS

机译:高浓度异丙酚微乳液制备的麻醉应用

摘要

The invention provides a method and composition for increasing the dissolution and bioavailability of propofol (2,6-diisopropylphenol) for use as an intravenously administered anesthetic in mammals. According to this method, a base composition of a self-emulsifying emulsion is prepared, which is used to make a water-based microemulsion preparation. In a preferred two-component (2) base composition, it consists of a surfactant containing polyethylene glycol and liquid propofol. A microemulsion is prepared by mixing this base composition with a carrier fluid, which leads to the formation of a microemulsion containing propofol concentrations up to about 4 wt.% Propofol to the volume of the microemulsion. In a four-component (4) base composition, it consists of a surfactant containing polyethylene glycol; liquid propofol; water-immiscible solvent and ethanol. A microemulsion is prepared by mixing this base composition with a carrier fluid, which leads to the formation of a microemulsion containing propofol concentrations up to about 10 wt.% Propofol to the volume of the microemulsion.
机译:本发明提供了用于提高异丙酚(2,6-二异丙基苯酚)的溶解度和生物利用度的方法和组合物,所述丙泊酚(2,6-二异丙基苯酚)在哺乳动物中用作静脉内施用的麻醉剂。根据该方法,制备自乳化乳液的基础组合物,其用于制备水基微乳液制剂。在优选的两组分(2)基础组合物中,它由含有聚乙二醇和液态丙泊酚的表面活性剂组成。通过将该基础组合物与载液混合来制备微乳液,这导致形成的微乳液包含相对于该微乳液的体积最多约4重量%的异丙酚的丙泊酚浓度。在四组分(4)基础组合物中,它由包含聚乙二醇的表面活性剂组成;液体异丙酚与水不混溶的溶剂和乙醇。通过将该基础组合物与载体流体混合来制备微乳液,这导致形成的微乳液包含相对于该微乳液的体积最多约10重量%的异丙酚的丙泊酚浓度。

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