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Propofol-containing fat emulsion

A technology of fat emulsion and propofol, which is applied in the direction of non-active ingredients of oil/fat/wax, anesthetics, anti-inflammatory agents, etc., can solve problems that have not been developed yet, achieve excellent filter permeability, prevent fungal contamination, and reduce The effect of destruction

Inactive Publication Date: 2008-04-02
OTSUKA PHARM FAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Thus, a propofol-containing fat emulsion formulation that can maintain emulsion stability during its administration and can prevent and / or reduce the occurrence of vascular pain without the introduction of local anesthetics such as lidocaine has not yet been developed.

Method used

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Examples

Experimental program
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Effect test

Embodiment 1-3

[0079] A fat emulsion formulation (total volume 100 mL) of the present invention comprising the components given in Table 1 described below was prepared as follows. The values ​​in Table 1 represent the weight-to-volume (w / v%) percentage concentration of each component based on the total volume of the fat emulsion formulation obtained.

[0080] The following components were used.

[0081] (1) Propofol (manufactured by ALBEMARLE)

[0082] (2) Soybean oil (refined soybean oil; manufactured by Nisshin Oil Mills, Ltd.)

[0083] (3) Yolk lecithin (purified egg yolk lecithin; produced by Kewpie)

[0084] (4) MCT (C8-10 triglyceride, trade name "Myglyol", produced by SASOL)

[0085] First, propofol given in Table 1, soybean oil and MCT as an oily component were mixed. Add egg yolk lecithin to the resulting mixture. Then, a solution in which glycerol was dissolved in water for injection to obtain a final glycerol concentration of 2.21 w / v% was added thereto, using a Polytron high...

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Abstract

The invention provides a propofol-containing fat emulsion preparation and a method for preparing the same. The propofol-containing fat emulsion preparation comprises: 0.1-2w / v% propofol, 10-20w / v % oily component, and 2-5w / v% emulsifier, the weight of the oily component is about 5-about 200 times that of propofol, and the weight of the emulsifier is about 0.9-200 times that of propofol about 50 times, and the average particle size of the emulsion particles is 180nm or less. The propofol-containing fat emulsion formulation of the present invention can relieve vascular pain occurring during its administration without introducing a local anesthetic such as lidocaine or the like thereinto.

Description

technical field [0001] The present invention relates to fat emulsion formulations containing propofol for the substantial reduction of vascular pain when such formulations are administered by intravenous injection or infusion. Background technique [0002] Propofol (2,6-diisopropylphenol) is a lipophilic substance that induces a hypnotic state. Since propofol is practically insoluble in water, it is usually formulated as an oil-in-water fat emulsion formulation using an oily component and an emulsifier in such a way that propofol can be administered intravenously or infused Can be administered directly into the bloodstream. Propofol in the form of a fat emulsion formulation is widely used as a general anesthetic, sedative, etc. (eg US Pat. No. 5,714,520). For example, there is known a commercially available propofol-containing fat emulsion preparation (trade name: "1% Diprivan Injection", comprising 1 g of propofol, 10 g of soybean oil, and 1.2 g of egg yolk lecithin, Pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61K9/10A61K47/14A61K47/24A61K47/44A61P23/00A61P25/20
CPCA61K9/0019A61K31/05A61K9/1075A61K9/107A61P23/00A61P25/00A61P25/04A61P25/20A61P29/02A61K47/14
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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