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

A method for preparing a biphenol lipid microsphere preparation comprising the steps of:

• 1) Dissolving an emulsifier completely with injection-grade oil under a nitrogen atmosphere and in a 70° C. water bath;
• adding antioxidants, with stirring for dissolution, before adding 2,2′,6,6′-tetraisopropyl-4,4′-biphenol, with heat and stirring for dissolution, to obtain an oil phase;
• 2) Dissolving a tonicity adjusting agent and a complexing agent in injection-grade water to obtain an aqueous phase;
• 3) Adding the oil phase slowly to the aqueous phase while shearing under nitrogen for 5 minutes to obtain a preliminary emulsion;
• 4) Homogenizing the preliminary emulsion with a high-pressure homogenizer and filtering with a microporous membrane filter before flushing with nitrogen, sealing and autoclaving at 115° C. to form the final product.

A method for preparing a biphenol lipid microsphere preparation, comprising the steps of:

• 1) Weighing the raw materials:
• 1 g˜30 g of 2,2′,6,6′-tetraisopropyl-4,4′-biphenol, 100 ml˜300 ml of injection-grade oil, 25 g of glycerin, 10 g˜15 g of emulsifier, 5 g˜10 g antioxidants, with the remaining being injection-grade water;
• 2) Dissolving the emulsifier and antioxidant (Vitamin E) completely with injection-grade oil under a nitrogen atmosphere and in a 70° C. water bath, before adding the biphenol, with heat and stirring for dissolution, to obtain an oil phase;
• 3) Dissolving the glycerin and the complexing agent in the injection-grade water, with stirring, to obtain an aqueous phase;
• 4) Adding the oil phase slowly to the aqueous phase while shearing under nitrogen (10000 r, 5 min) to obtain a preliminary emulsion, and adjusting pH to around 8.0 with NaOH;
• and
• 5) Homogenizing the preliminary emulsion 5˜8 times with a high-pressure homogenizer at 800˜900 bar and filtering with a microporous membrane filter before flushing with nitrogen, sealing and autoclaving at 115° C. to obtain the final product (1000 ml).

A method for preparing biphenol lipid microsphere preparation comprising the steps of:

• 1) Weighing the raw materials:
• 1 g˜30 g of 2,2′,6,6′-tetraisopropyl-4,4′-biphenol, 100 ml˜300 ml of injection-grade oil, 25 g of glycerin, 10 g˜15 g of emulsifier, 5 g˜10 g antioxidants, with the remaining being injection-grade water;
• 2) Dissolving the emulsifier and antioxidant (Vitamin E) completely with the injection-grade oil under a nitrogen atmosphere and in a 70° C. water bath before adding the biphenol, with heat and stirring for dissolution, to obtain an oil phase;
• 3) Dissolving the glycerin, antioxidant (ascorbic acid or sodium bisulfite) and complexing agent in the injection-grade water, with stirring, to obtain an aqueous phase;
• 4) Adding the oil phase slowly to the aqueous phase while shearing under nitrogen (10000 r, 5 min) to obtain a preliminary emulsion, and adjusting pH to around 8.0 with NaOH;
• 5) Homogenizing the preliminary emulsion 5˜8 times with a high-pressure homogenizer at 800˜900 bar, filtering with a microporous membrane filter, filling with nitrogen, sealing and autoclaving at 115° C. to obtain the final product (1000 ml).