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Propofol-containing fat emulsion preparation

A fat emulsion, propofol technology, applied in non-active medical preparations, oil/fat/wax non-active ingredients, anesthetics, etc., to achieve the effect of reducing side effects

Inactive Publication Date: 2007-02-07
OTSUKA PHARM FAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Therefore, a propofol-containing fat emulsion that prevents or relieves the occurrence of severe pain, etc. during administration without compromising the stability and safety of the emulsion has not yet been developed.

Method used

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  • Propofol-containing fat emulsion preparation
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Examples

Experimental program
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Effect test

Embodiment 1-4

[0086] (1) The fat emulsions of the present invention (total volumes of 100 ml each) composed of the components shown in Table 2 were prepared as follows.

[0087] components

Volume / 100ml

Control (1%

Diprivan TM

injection)

Example 1

Example 2

Example 3

Example 4

HP-β-CyD

-

0.02g

0.05g

0.1g

0.2g

Propofol

1g

1g

1g

1g

1g

soybean oil

10g

10g

10g

10g

10g

egg yolk lecithin

1.2g

1.2g

1.2g

1.2g

1.2g

Glycerin

2.21g

2.21g

2.21g

2.21g

2.21g

Water for Injection

Appropriate amount

Appropriate amount

Appropriate amount

Appropriate amount

Appropriate amount

[0088] The components shown in Table 2 are the following products.

[0089] Propofol: ALBEMARLE product

[0090] Soybean oil: Purified soybean oil...

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Abstract

The present invention provides a propofol-containing fat emulsion that can be administered with reduced vascular pain without incorporating a local anesthetic such as lidocaine; and a process for producing the same. The fat emulsion comprises 0.1 to 5 w / v% of propofol, 2 to 20 w / v% of an oily component, 0.4 to 10 w / v% of an emulsifier and 0.02 to 0.3 w / v% of at least one compound selected from the group consisting of cyclodextrins, cyclodextrin derivatives and pharmacologically acceptable salts thereof, and is in the form of a fat emulsion.

Description

technical field [0001] The present invention relates to fat emulsions containing propofol (PROPOFOL), the administration of which reduces vascular pain. Background technique [0002] Propofol (2,6-diisopropylphenol) is a lipophilic substance that induces hypnosis. Due to its poor water solubility, propofol is usually prepared as an oil-in-water fat emulsion using oily components and emulsifiers, which can be administered directly into the bloodstream by intravenous injection or infusion. Such a fat emulsion containing propofol is widely used as a general anesthetic, a sedative, etc. (see, for example, U.S. Patent No. 5,714,520). Its known commercially available products include, for example, 1% Diprivan TM injection (AstraZeneca). [0003] However, it has been reported that during the administration of such preparations by intravenous injection or infusion, side effects of severe pain (vascular pain) generally occur (see, for example, W. Klemment, J.O. Arndt, British Jour...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61K9/10A61K47/24A61K47/40A61K47/44A61P25/20A61K9/107
CPCA61K47/40A61K9/107A61K31/05A61P23/00A61P25/20A61P29/00A61K31/045
Inventor 武田光市松田宪治寺尾敏光井上忠昭今川昂倍味繁
Owner OTSUKA PHARM FAB INC
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