2,2',6,6'-tetraisopropyl-4,4'-biphenol lipid microsphere preparations and preparation methods therefor

Abstract

This invention relates to a 2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparation having 2,2′,6,6′-tetraisopropyl-4,4′-biphenol as its active ingredient and formed into said lipid microsphere preparation with common medically used injection-grade oil, emulsifier, and injection-grade water.

1 - 10 . (canceled) 
     
     
         11 . A 2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparation for use in intravenous injections, wherein every 100 ml of said preparation comprises 0.1 to 0.3 weight % of 2,2′,6,6′-tetraisopropyl-4,4′-biphenol, 10 to 30 weight % of soybean oil, 1 to 1.5 weight % of injection-grade egg lecithin, 0.5 to 1 weight % of vitamin E, 0.01 to 1 weight % of sodium hydroxide, 0.1 to 2.5 weight % of glycerin, 0.01 to 1 weight % of EDTA, and the remaining being injection-grade water; and wherein the average particle size is 150 nm to 300 nm. 
     
     
         12 . A method for preparing the 2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparation of claim  1  for use in intravenous injections, comprising the steps of:
 1) Dissolving appropriate amounts of injection-grade egg lecithin and vitamin E completely in injection-grade soybean oil under a nitrogen atmosphere in a 70° C. water bath before adding 2,2′,6,6′-tetraisopropyl-4,4′-biphenol, with heat and stirring for dissolution, to obtain an oil phase; 
 2) Dissolving appropriate amounts of glycerin and EDTA in injection-grade water, with stirring, to obtain an aqueous phase; 
 3) Adding said oil phase slowly to said aqueous phase while shearing under nitrogen at 10000 r for 5 minutes to obtain a preliminary emulsion, and adjusting the pH to around 8.0 with NaOH; and 
 4) Homogenizing said preliminary emulsion 5 to 8 times under a pressure of 800 to 900 bar before filtering with a microporous membrane filter, flushing with nitrogen, sealing and autoclaving at 115° C. to obtain said lipid microsphere preparation.