Propofol fat emulsion injection and preparation method thereof

A technology for propofol fat and injection, applied in the field of medicine, can solve the problems of unstable thermodynamics and kinetics, increase in particle size, and large particle size of fat emulsion, so as to improve drug delivery and enhance particle size uniformity. , the effect of reducing particle size

Active Publication Date: 2013-12-04
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This technology solves the problem of poor stability of ordinary fat emulsions by introducing polyethylene glycol phospholipid derivatives into the formulation to modify the surface of the fat emulsion. However, the formulation ingredients are complex, the particle size of the fat emulsion is large, and the preparation cost is high.
[0004] To sum up, the particle size of the propofol lipid emulsion disclosed in the current literature is about 300nm, which is easy to break the emulsion, and at the same time, it is easy to cause pain during injection
In addition, ordinary fat emulsions are heterogeneous liquid preparations, which are thermodynamically and kinetically unstable systems. During long-term storage, emulsion droplet particles are easy to merge and increase in particle size, which limits the stability and stability of propofol fat emulsions. safety

Method used

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  • Propofol fat emulsion injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Prescription: Propofol 500g, soybean oil 3500g, soybean lecithin 900g, glycerin 2000g, Tween-80220g, phosphoric acid 40g, appropriate amount of pH regulator, the balance is water for injection, the total volume is 50L.

[0027] Preparation Process:

[0028] (1) Heat soybean oil and soybean lecithin to 78-80°C under nitrogen protection, add propofol while stirring to dissolve, then add Tween-80 and mix well to obtain the oil phase;

[0029] (2) Add glycerol and phosphoric acid in sequence to 40L water for injection to dissolve to obtain an aqueous phase;

[0030] (3) Under the protection of nitrogen, while stirring at a high speed of 1800rpm, add the oil phase of step (1) into the water phase of step (2), keep stirring for 3-5min, and adjust the pH=7.5 with 0.1mol / L sodium hydroxide solution -8.0, add water for injection to make up the volume, stir to get more uniform colostrum;

[0031] (4) Under the protection of nitrogen, add colostrum into a high-pressure homogeniz...

Embodiment 2

[0035] Prescription: Propofol 500g, soybean oil 4000g, soybean lecithin 800g, glycerin 2000g, Tween-80200g, phosphoric acid 40g, appropriate amount of pH regulator, the balance is water for injection, the total volume is 50L.

[0036] Preparation process: with embodiment 1.

[0037] The prepared propofol fat emulsion injection was centrifuged in a DT5-3 centrifuge for 30 minutes, and the fat emulsion was still clear and transparent without precipitation, stratification and turbidity. This shows that its physical stability is good, which can indirectly explain that it can still maintain good stability after standing for a long time naturally. Another appropriate amount of propofol fat emulsion injection was taken, and its particle size and particle size distribution were measured with a laser particle size analyzer. The results showed that the average particle size of propofol fat emulsion injection was 135nm, and the polydispersity coefficient was 0.142; it can be seen that t...

Embodiment 3

[0039] Prescription: 200g of propofol, 1200g of soybean oil, 400g of soybean lecithin, 1000g of glycerin, 100g of Tween-80, 20g of phosphoric acid, an appropriate amount of pH regulator, the balance is water for injection, the total volume is 20L.

[0040] (1) Heat soybean oil and soybean lecithin to 78-80°C under nitrogen protection, add propofol while stirring to dissolve, then add Tween-80 and mix well to obtain the oil phase;

[0041] (2) Add glycerol and phosphoric acid in sequence to 16L water for injection to dissolve to obtain the aqueous phase;

[0042] (3) Under the protection of nitrogen, while stirring at a high speed of 1800rpm, add the oil phase of step (1) into the water phase of step (2), keep stirring for 3-5min, and use 0.1mol / L sodium hydroxide solution and 0.1mol / L sodium hydroxide solution L hydrochloric acid solution to adjust pH=7.5-8.0, add water for injection to constant volume, stir to obtain more uniform colostrum;

[0043] (4) Under the protection ...

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Abstract

The invention discloses propofol fat emulsion injection and a preparation method thereof. The propofol fat emulsion injection comprises, by weight percent, 1% of propofol, 6-8% of soybean oil, 1.5-2.0% of soybean lecithin, 3-5% of glycerol, 0.1-0.8% of tween-80, 0.05-0.1% of phosphoric acid, appropriate amount of pH regulator and the balance of water for injection, wherein the amount of the pH regulator is enough to regulate pH of the water for injection to 7.5-8.0. The propofol fat emulsion injection improves drug delivery, decreases particle size, and improves uniformity of particle size, and accordingly stability of the injection is improved, pain during injection is lowered, and drug dependency of patients is increased.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a fat emulsion preparation. Specifically, the present invention relates to a propofol fat emulsion injection and a preparation method thereof. Background technique [0002] Propofol is a new 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 fast onset of anesthesia induction, rapid recovery and complete functional recovery, and low incidence of postoperative nausea and vomiting. [0003] The chemical name of propofol is 2,6-diisopropylphenol, which is extremely insoluble in water. Therefore, the current dosage form of propofol is fat emulsion. CN102366404A discloses a propofol medium / long-chain fat emulsion, which consists of the following components in parts by weight: 10-20 parts of propofol, 50-100 parts of soybean oil, and 50-100 parts of m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/05A61K47/44A61K47/24A61K47/26A61P23/00A61P25/20
Inventor 张振乾冯艳
Owner NANJING CHIA TAI TIANQING PHARMA
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