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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

Active Publication Date: 2007-09-12
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a long-circulation fat milk propofol preparation, the long-circulation fat milk propofol preparation solves the problem of the poor stability of common fat milk by modifying the surface of fat milk with polyethylene glycol, and is easy to circulate from the body. The disadvantage of being quickly cleared by liver and spleen macrophages can keep fat emulsion in the blood for a long time, which increases the passive targeting function of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The present invention relates to propofol carrying fat emulsion preparation with long circulating time and its preparation process. The propofol carrying fat emulsion preparation consists of: propofol or liposoluble propofol derivative, vegetable oil as medicine solvent, lecithin as the surfactant of the emulsion, polyethylene glycol phospholipid derivative as the emulsion stabilizer and emulsifier to increase the half life of the fat emulsion in blood, oleic acid or oleate as the emulsion stabilizer and emulsifier, vitamin E as the antioxidant, and complexing agent for controlling metal ion. The propofol carrying fat emulsion preparation of the present invention has long retention period in blood, increased passive medicine targeting function, high stability, raised anesthetic action of propofol.

Description

technical field [0001] The invention relates to a drug-loaded preparation, in particular to a long-circulation fat milk propofol preparation. Background technique [0002] Propofol is a new type of intravenous anesthetic mainly used for induction and maintenance of general anesthesia. In recent years, it is also widely used in painless treatment such as short outpatient surgery, gastrointestinal endoscopy, and induced abortion. Its advantages are fast, short-acting, rapid and complete recovery, and no accumulation after continuous infusion. Propofol is insoluble in water, so the formulations used clinically include fat emulsion, cyclodextrin and water-soluble derivatives. Propofol fat emulsion preparation is a stable oil-in-water type (O / W) emulsion, available for intravenous injection. Phospholipid fat emulsion propofol has good safety performance and no stimulation, and is one of the main drugs widely used in clinical treatment for general anes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/05A61K47/44A61K47/24A61K47/34A61K47/12A61P23/00
Inventor 陈涛王汝涛惠民权傅经国
Owner XIAN LIBANG PHARMA
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