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Compound isopropyl phenol injection containing local anesthetic and preparation method therefor

A technology of compound propofol microemulsion and compound propofol fat emulsion, which is applied in the field of medicine, can solve the problems of difficult control of drug concentration and increased drug contamination, and achieve the effects of reducing the incidence of pain, safe medication, and definite curative effect

Inactive Publication Date: 2012-05-30
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to clinical drug screening, local anesthetics such as lidocaine are ideal drugs for mixing with propofol, but preclinical mixing and other operations increase the probability of drug contamination, and the drug concentration is difficult to control

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 (compound propofol fat emulsion): (1) Take 20 g of egg yolk lecithin, 150 g of refined soybean oil, and 10 g of propofol, preheat to 80° C., stir, and mix well. (2) Take 50g of polyethylene glycol, 20g of glycerin, 2g of lidocaine hydrochloride and an appropriate amount of water for injection, preheat to 80°C, stir, and mix well. (3) Add (2) into (1), stir while adding, and disperse through a tissue masher, 20,000 revolutions per minute, three minutes, repeat three times. (4) Add an appropriate amount of water for injection preheated to 80°C to a full volume of 1000ml, pass through a high-pressure homogenizer, repeat three times, take samples, observe the particle size under a microscope, and stop when the particle size of the emulsion meets the requirements. (5) Filtration, filling, filling with N 2 , seal, sterilize, number, and obtain the product.

Embodiment 2

[0029] Example 2 (compound propofol submicron emulsion): (1) Take 15 g of egg yolk lecithin and 10 g of propofol, preheat to 80° C., stir, and mix well. (2) Take 100g of 1,2-propanediol, 20g of poloxamer, 25g of glycerin, 1g of lidocaine hydrochloride and an appropriate amount of water for injection, preheat to 80°C, stir, and mix well. (3) Add (2) into (1), stir while adding, and disperse through a tissue masher, 20,000 revolutions per minute, three minutes, repeat three times. (4) Add an appropriate amount of water for injection preheated to 80°C to a full volume of 1000ml, pass through a high-pressure homogenizer, repeat three times, take samples, observe the particle size under a microscope, and stop when the particle size of the emulsion meets the requirements. (5) Filtration, filling, filling with N 2 , seal, sterilize, number, and obtain the product.

Embodiment 3

[0030] Embodiment 3 (compound propofol microemulsion): (1) get propofol 10g, V E 2g, preheat to 80°C, stir and mix well. (2) Take 500g of 1,2-propanediol, 30g of poloxamer, 15g of glycerin, 5g of lidocaine hydrochloride and an appropriate amount of water for injection, preheat to 80°C, stir, and mix well. (3) Add (2) into (1), stir while adding, and disperse through a tissue masher, 20,000 revolutions per minute, three minutes, repeat three times. (4) Add an appropriate amount of water for injection preheated to 80°C to a full volume of 1000ml, pass through a high-pressure homogenizer, repeat three times, take samples, observe the particle size under a microscope, and stop when the particle size of the emulsion meets the requirements. (5) Filtration, filling, filling with N 2 , seal, sterilize, number, and obtain the product.

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PUM

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Abstract

A compound isopropylphenol injection containing local anesthetic contains proportionally isopropylphenol, the local anesthetic chosen from procaine, lidocaine, etc, the refined plant oil for injection, emulsifier, isotonic regulator, antioxidant, pH regulator and the water for injection. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound propofol injection containing a local anesthetic and a preparation process thereof. Background technique [0002] Propofol, namely 2,6-diisopropylphenol, is a new systemic intravenous anesthetic. It has excellent characteristics such as rapid onset of action, short action time, rapid and complete recovery, few adverse reactions, no sequelae, wide application range (can be used for anesthesia induction, maintenance and auxiliary epidural anesthesia, etc.), and easy-to-control dosage. [0003] Since its anesthetic activity was discovered in 1977, many researches have been carried out on the formulation, and clinical application has been more and more extensive. Pharmacodynamic studies of propofol have shown that propofol is inactive when administered orally, possibly due to disruption of the gastrointestinal tract. At present, the dosage form of clinical application a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/05A61K9/08A61P23/00
Inventor 王思玲苏德森罗瑞昌
Owner SHENYANG PHARMA UNIVERSITY
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