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Propofol medium-long-chain fatty emulsion

A fat emulsion and propofol technology, which is applied in the direction of oil/fat/wax non-active ingredients, anesthetics, emulsion delivery, etc., can solve the problems that limit the stability and safety of propofol emulsion, and achieve good safety, The effect of good stability

Active Publication Date: 2012-03-07
四川国瑞药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These all limit the stability and safety of propofol emulsion

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: a kind of propofol medium / long-chain fat emulsion, full amount 1000ml, is made of following components:

[0021] Propofol: 10g

[0022] Soybean oil: 55g

[0023] Medium Chain Triglycerides 55g

[0024] Glycerin 23g

[0025] Lecithin 6g

[0026] Sodium hydroxide 0.02g

[0027] Oleic acid 0.3g

[0028] Appropriate amount of water for injection.

[0029] The preparation method is as follows:

[0030] 1. Under the protection of nitrogen, add the prescription amount of soybean oil and medium chain triglyceride to the container and heat up to 80-90°C, add egg yolk lecithin and oleic acid under high-speed stirring (1500-3000rpm) to disperse; then Add the prescribed amount of propofol to prepare the oil phase.

[0031] 2. Put an appropriate amount of water for injection (above 70°C) in a container, add the prescribed amount of glycerin, stir and mix well, and filter through a 0.22 μm filter membrane to prepare an aqueous phase.

[0032] 3. Under the prote...

Embodiment 2

[0036] Embodiment 2: a kind of propofol medium / long-chain fat emulsion, full amount 1000ml, is made of following components:

[0037] Propofol: 15g

[0038] soybean oil: 70g

[0039] Medium Chain Triglycerides 70g

[0040] Glycerin 20g

[0041] Lecithin 8g

[0042] Sodium hydroxide 0.03g

[0043] Oleic acid 0.4g

[0044] Appropriate amount of water for injection.

[0045] The preparation method is the same as in Example 1.

Embodiment 3

[0046] Embodiment 3: a kind of propofol medium / long-chain fat emulsion, full amount 1000ml, is made of following components:

[0047] Propofol: 20g

[0048] Soybean oil: 100g

[0049] Medium Chain Triglycerides 100g

[0050] Glycerin 25g

[0051] Lecithin 12g

[0052] Sodium hydroxide 0.05g

[0053] Oleic acid 0.6g

[0054] Appropriate amount of water for injection.

[0055] The preparation method is the same as in Example 1.

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PUM

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Abstract

The invention discloses a propofol medium-long-chain fatty emulsion, which is made from the following components of: by weight, 10-20 parts of propofol, 50-100 parts of soybean oil, 50-100 parts of medium-chain triglyceride, 20-25 parts of glycerin, 6-12 parts of phosphatidylcholine bilayer, 0.02-0.05 part of sodium hydroxide, 0.3-0.6 part of oleic acid and injection water.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy and relates to a medium / long-chain fat emulsion of propofol. Background technique [0002] Propofol (chemical name: 2,6-diisopropylphenol) is a new type of rapid and short-acting intravenous anesthetic commonly used clinically for induction of anesthesia, maintenance of anesthesia, and sedation of critically ill ICU patients. It has the advantages of rapid onset of anesthesia induction, rapid recovery and complete functional recovery, and low incidence of postoperative nausea and vomiting. [0003] Although propofol is an effective anesthetic, it is a water-insoluble drug that is difficult to formulate directly into solution for intravenous administration. To solve the problem of propofol dosing, pharmacists have conducted a lot of research. Initially, Cremophor EL, an injectable non-ionic surfactant, was used to solubilize it to prepare a 1% aqueous solution of propofol. However, Crem...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/05A61K47/44A61P23/00
Inventor 朱义王一茜沈文龙
Owner 四川国瑞药业有限责任公司
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