Superregulated long-cycled lipid emulsion carrying medicine reagent for mainline

A technology of fat emulsion and long circulation, which is applied in the direction of medical preparations with non-active ingredients, oil/fat/wax non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of increasing the passive targeting function of drugs and poor stability and other issues to achieve the effect of enhancing bioavailability and clinical therapeutic effect and improving stability

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

[0007] The object of the present invention is to provide a drug-loaded preparation of high-stable and long-circulating fat emulsion for intravenous injection, which solves the problem of poor stability of ordinary fat emulsion and is easily absorbed by the liver from the circulation in the body through the modification of the surface of the fat emulsion with polyethylene glycol. , The shortcoming of rapid removal of splenic macrophages can keep the fat emulsion in the blood for a long time, which increases the passive targeting function of the drug

Method used

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  • Superregulated long-cycled lipid emulsion carrying medicine reagent for mainline
  • Superregulated long-cycled lipid emulsion carrying medicine reagent for mainline
  • Superregulated long-cycled lipid emulsion carrying medicine reagent for mainline

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0044] Example 1: Long Circulating Lipid Emulsion Pharmaceutical Formulation with Minimal PEG-phospholipid Content

[0045] soybean oil (for injection)

[0046] Take 100.0 g of soybean oil, add 12.0 g of lecithin, 0.4 g of sodium oleate, and 0.2 g of polyethylene glycol-phospholipid (PEG-DSPE), and heat to 75°C under nitrogen protection, and stir for about 10 minutes to make the added Various lipid compounds are fully dissolved, then add 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 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. The high-pressure homogenizer homogenizes 5-8 times, the homogenization pressure is about 100MPa, and the particle size ranges from 150nm to 300nm, adjust the pH to 7.0-8.0, filter, ...

example 2

[0047] Example 2: Long Circulating Lipid Emulsion Pharmaceutical Formulation with Highest PEG-Phospholipid Content

[0048] soybean oil (for injection)

100.0g

Lecithin (for injection)

10.0g

sodium oleate

0.4g

polyethylene glycol-phospholipid

8.0g

Vitamin E (for injection)

10ml

Glycerin

22g

Water for Injection

Add to 1000ml

[0049] Take 100.0 g of soybean oil, add 10.0 g of lecithin, 0.4 g of sodium oleate, and 8.0 g of polyethylene glycol-phospholipid (PEG-DSPE), heat to 75°C under nitrogen protection, and stir for about 10 minutes to make the added Various lipid compounds are fully dissolved, then add 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 the drug was added into the glycerol aqueous solution under the condition of shearing and ...

example 3

[0051] Example 3: The long-circulation fat emulsion drug preparation prepared by the minimum content of animal and vegetable oil, liquid oily drug or oil solution as drug solvent (only using soybean oil as an example)

[0052] soybean oil (for injection)

[0053] Take 50.0g of soybean oil, add 10.0g of lecithin, 0.4g of sodium oleate, 4.0g of polyethylene glycol-phospholipid (PEG-DSPE), and heat to 75°C under nitrogen protection, and stir for about 10min to make the added Various lipid compounds are fully dissolved, then add 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 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. The high-pressure homogenizer homogenizes 5-8 times, the homogenization pressure is about 100...

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Abstract

The present invention relates to high stability medicine carrying fat emulsion preparation for intravenous injection and its preparation process. The high stability medicine carrying fat emulsion preparation consists of: clinically effective liposoluble medicine, oil with medicinal effect or 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 fat emulsion preparation of the present invention has long retention period in blood, increased passive medicine targeting function, high stability, raised bioavailability of the liposoluble medicine and raised clinical therapeutic effect.

Description

technical field [0001] The invention relates to a drug-carrying preparation, in particular to a drug-carrying preparation of highly stable and long-circulating fat emulsion (fat emulsion) for intravenous injection. Background technique [0002] Fat emulsion lipid emulsion or other advanced drug delivery technology is a new drug dosage form that has developed rapidly in recent years, and has high clinical and economic value. Fat emulsion is a stable oil-in-water (O / W) emulsion made of vegetable oil (the main component is fatty acid triglyceride), phospholipid emulsifier, isotonic agent and water for injection, which can be used for intravenous injection and can be completely absorbed by the body. metabolism and utilization. Fat emulsion has good safety performance and no irritation to veins, and is a parenteral nutrition widely used in clinical treatment. It can not only quickly provide patients with high energy, but also has good compatibility with...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/44A61K47/12A61K47/34A61K47/24A61K45/00A61K47/10A61K47/14A61K47/18A61K47/28
Inventor 陈涛王汝涛惠民权傅经国
Owner XIAN LIBANG PHARMA
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