Long-cycled lipid emulsion profofol preparation
A lactofol, long-circulation technology, applied in the directions of oil/fat/wax inactive ingredients, anesthetics, emulsion delivery, etc., can solve the problems of increasing the passive targeting function of drugs, poor stability, etc., and improve the half-life of blood drugs. , inhibit clearance, improve the effect of treatment
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example 1
[0034] Example 1: Formulation of low-content propofol long-circulating fat emulsion (0.05% propofol)
[0035] Propofol
[0036] Take 99.5g of soybean oil, add 10.0g of lecithin, 0.4g of sodium oleate, and 3.0g of polyethylene glycol-phospholipid (PEG-DSPE), heat to 75°C under nitrogen protection, and stir for about 10min to make the added Various lipid compounds are fully dissolved, then add 0.5g propofol and 10ml vitamin E, dissolve and mix well. Another 800ml of water for injection was taken, and 22g of glycerol was added. Under the condition of nitrogen protection, the oil solution containing propofol was added into the aqueous glycerin solution under the condition of shearing and stirring to prepare colostrum, and the total amount was adjusted to 1000ml. Homogenize 5-8 times with a high-pressure homogenizer, the homogenization pressure is about 100MPa, until the particle size ranges from 150nm to 300nm, adjust the pH to 7.0-8.0, filter, subpackage, inject nitro...
example 2
[0037] Example 2: Formulation of high-content propofol long-circulating fat emulsion (10% propofol)
[0038] Propofol
10.0g
soybean oil (for injection)
90.0g
Lecithin (for injection)
10.0g
sodium oleate
0.4g
polyethylene glycol-phospholipid
3.0g
Vitamin E (for injection)
10ml
Glycerin
22g
Water for Injection
Add to 1000ml
[0039] Take 90g of soybean oil, add 10.0g of lecithin, 0.4g of sodium oleate, and 3.0g of polyethylene glycol-phospholipid (PEG-DSPE), heat to 75°C under nitrogen protection, and stir for about 10min so that the added Lipid compounds are fully dissolved, then add 10.0g propofol and 10ml vitamin E, dissolve and mix well. Another 800ml of water for injection was taken, and 22g of glycerol was added. Under the condition of nitrogen protection, the oil solution containing propofol was added into the aqueous glycerin solution under the condition of s...
example 3
[0041] Example 3: Long-circulating fat milk propofol formulation with low polyethylene glycol-phospholipid content
[0042] Propofol
[0043] Get soybean oil 99.0g, add 12.0g lecithin, 0.4g sodium oleate, 0.2g polyethylene glycol-phospholipid (PEG 2000 -DSPE), under the condition of nitrogen protection, heated to 75°C, stirred for about 10min to fully dissolve the various lipid compounds added, then added 1.0g propofol and 10ml vitamin E, dissolved and mixed. Another 800ml of water for injection was taken, and 22g of glycerol was added. Under the condition of nitrogen protection, the oil solution containing the drug was added into the glycerol aqueous solution under the condition of shearing and stirring to prepare colostrum, and the total amount was adjusted to 1000ml. Homogenize 5-8 times with a high-pressure homogenizer, the homogenization pressure is about 100MPa, until the particle size ranges from 150nm to 300nm, adjust the pH to 7.0-8.0, filter, subpackage, ...
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