Formula and preparation method of novel propofol fat emulsion preparation causing no pain and low injection stimulation

A technology of propofol fat and propofol, which can be used in oil/fat/wax inactive ingredients, anesthetics, emulsion delivery, etc., and can solve problems such as in-depth research on prostaglandins

Active Publication Date: 2011-06-08
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

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  • Formula and preparation method of novel propofol fat emulsion preparation causing no pain and low injection stimulation
  • Formula and preparation method of novel propofol fat emulsion preparation causing no pain and low injection stimulation
  • Formula and preparation method of novel propofol fat emulsion preparation causing no pain and low injection stimulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Example 1: Investigation of the applicability of ultrafiltration to ordinary propofol fat emulsion

[0085] Get 1000mL of propofol fat emulsion (such as the sample prepared according to Example 2) prepared by any embodiment, and take a small amount of sample to analyze the free propofol concentration in its water phase. according to figure 2 Assemble the "ultrafiltration production equipment" and select the ultrafiltration cartridge with suitable pore size. The main factor in the selection is that the aqueous solution, especially the free propofol in the water phase, can pass freely, while the fat emulsion cannot pass through as the selection parameter. First, equilibrate the ultrafiltration column with isotonic buffer solution, then slowly input the propofol fat emulsion into the ultrafiltration column to adjust the column pressure. The aqueous solution containing free propofol passes through the ultrafiltration column and is effectively separated from the propofol f...

Embodiment 2

[0086] Example 2: Investigation of the applicability of ultrafiltration to polyethylene glycol propofol fat emulsion

[0087] Get the polyethylene glycol propofol fat emulsion sample 1000mL prepared according to Example 10, take a small amount and analyze the free propofol concentration in its water phase. according to figure 2 Assemble the "ultrafiltration production equipment", select the ultrafiltration cartridge with the appropriate pore size, and use the water solution to pass through freely, but the fat emulsion cannot pass through as the selection parameter. First, equilibrate the ultrafiltration column with isotonic buffer solution, then slowly input the propofol fat emulsion into the ultrafiltration column to adjust the column pressure. The aqueous solution containing free propofol passes through the ultrafiltration column and is effectively separated from the propofol fat emulsion. The missing solution is replenished by buffer solution. Generally, the free propof...

Embodiment 3

[0092] Example 3: Highest propofol to diluent oil ratio (propofol: soybean oil weight ratio is 0.07)

[0093] prescription:

[0094] Propofol 10.0g

[0095] Soybean oil (for injection) 143.0g

[0096] Lecithin (for injection) 12.5g

[0097] Vitamin E 3.0g

[0098] Glycerin 22.0g

[0099] Add water for injection to 1000ml

[0100] Take 10.0g of propofol, 3.0g of vitamin E, 143.0g of refined soybean oil, add 12.5g of lecithin, heat and stir for about 10-20min to mix well. Another 700ml of water for injection was taken, and 22.0g of glycerin was added. Under nitrogen protection and stirring conditions, the propofol phospholipid oil solution was added to the aqueous glycerin solution, and the total amount was adjusted to 1000ml. Homogenize 7-8 times with a high-pressure homogenizer, the homogenization pressure is 100MPa, until the particle size is less than 300nm, adjust the pH to 6.0-8.0, filter, subpackage, inject nitrogen, and seal. Sterilize at 115°C for 15 minutes, an...

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Abstract

The invention discloses a formula and preparation method of a novel propofol fat emulsion preparation which causes no pain or can be used for obviously lowering injection stimulation and pain. The novel preparation comprises the main constituents of propofol, an emulsifier, refined soybean oil or other refined oil as an oil-soluble diluent, oleic acid or oleate with the effect of assisting emulsification, vitamin E or derivatives thereof with an antioxidation effect, an ionic complexing agent, and glycerol or micro molecular sugar as an isoosmotic adjusting agent.

Description

[0001] 1. Field [0002] The invention belongs to the series of medical drugs, and relates to the formulation and preparation of a new drug preparation, in particular to the formulation and preparation of a new type of propofol fat emulsion preparation with no pain and low injection stimulation. 2. Technical Background [0003] The anesthetic drug propofol (also known as dipofol, or propofol, or 2,6-diisopropylphenol, see structure figure 1 ) is a hindered phenol with strong lipophilicity, and is mostly used in the form of fat emulsion preparations for clinical induction and maintenance of anesthesia[1]. Propofol, as a commonly used clinical intravenous anesthetic, has been widely used for its fast onset, short duration of action, fast metabolism and high safety. However, propofol injection administration can cause injection pain with a high incidence (30-70%) at the injection site, which seriously affects the patient's body and spirit [2, 3, 4], thus limiting its further cli...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/05A61K47/44A61P23/00
Inventor 陈涛王汝涛惠民权马玉樊王惟娇
Owner XIAN LIBANG PHARMA
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