Flurbiprofen acetaminophen resin lipid microsphere injection, freeze-drying lipid microsphere injection and preparation methods

A technology of acetaminophen ester lipid and acetaminophen ester, applied in flurbiprofen acetaminophen ester lipid microsphere injection, non-steroidal anti-inflammatory analgesic drug injection, freeze-dried lipid microsphere In the field of injections and preparations, it can solve the problems of small dosage, long-term stability, venous irritation, etc.

Active Publication Date: 2013-04-24
WUXI ERYUN TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] If flurbiprofen paracetamol can be made into lipid microsphere injection, it will certainly provide a new type of non-steroidal anti-inflammatory drug for inje

Method used

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  • Flurbiprofen acetaminophen resin lipid microsphere injection, freeze-drying lipid microsphere injection and preparation methods
  • Flurbiprofen acetaminophen resin lipid microsphere injection, freeze-drying lipid microsphere injection and preparation methods
  • Flurbiprofen acetaminophen resin lipid microsphere injection, freeze-drying lipid microsphere injection and preparation methods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Prepare flurbiprofen acetaminophen lipid microsphere injection according to the following method:

[0096] (1) Preparation of medicated oil phase: Mix 1 g of flurbiprofen acetaminophen, 10 g of soybean oil for injection, 2.6 g of soybean lecithin and 0.5 g of oleic acid, heat to 65°C, and stir evenly to obtain a clear Medicinal oil phase;

[0097] (2) Prepare the water phase: mix 1.4g of soybean lecithin with 7ml of water for injection, heat to 65°C, stir evenly to obtain a clear water phase;

[0098] (3) Preparation of colostrum: under 10000rpm high-speed stirring, add the water phase obtained in step (2) to the oil phase obtained in step (1), stir evenly and adjust the pH value to 6 to obtain colostrum;

[0099] (4) Dilution: dilute the colostrum obtained in step (3) with 78ml of water for injection, the concentration of flurbiprofen acetaminophen in the diluted colostrum is 11.8mg / ml;

[0100] (5) Preparation of lipid microsphere injection: transfer the diluted col...

Embodiment 2

[0102] Prepare flurbiprofen acetaminophen lipid microsphere injection according to the following method:

[0103] (1) Preparation of medicated oil phase: Mix 2g of flurbiprofen acetaminophen, 15g of medium-chain fatty acid glycerides, 4.5g of egg yolk lecithin and 1.5g of sodium oleate, heat to 75°C, stir evenly to obtain clarified medicated oil phase;

[0104] (2) Prepare the water phase: mix 1.5g of egg yolk lecithin with 9ml of water for injection, heat to 75°C, stir evenly to obtain a clear water phase;

[0105] (3) Preparation of colostrum: under high-speed stirring at 10000rpm, add the water phase obtained in step (2) to the oil phase obtained in step (1), stir evenly and adjust the pH value to 7 to obtain colostrum;

[0106] (4) Dilution: dilute the colostrum obtained in step (3) with 67ml of water for injection, the concentration of flurbiprofen acetaminophen in the diluted colostrum is 26.3mg / ml;

[0107] (5) Preparation of lipid microsphere injection: transfer the ...

Embodiment 3

[0109] Prepare flurbiprofen acetaminophen lipid microsphere injection according to the following method:

[0110] (1) Preparation of medicated oil phase: Mix 0.1g of flurbiprofen acetaminophen, 1g of peanut oil and 0.9g of cholesterol in the total weight of the emulsifier, heat to 30°C, and stir well to obtain a clear medicated oil phase ;

[0111] (2) Preparation of water phase: Mix 0.1g of cholesterol with 1ml of water for injection, heat to 30°C, stir well to obtain a clear water phase;

[0112] (3) Preparation of colostrum: under 8000rpm high-speed stirring, add the water phase obtained in step (2) to the oil phase obtained in step (1), stir evenly and adjust the pH value to 5 to obtain colostrum;

[0113](4) Dilution: dilute the colostrum obtained in step (3) with 97ml of water for injection, and the concentration of flurbiprofen acetaminophen in the diluted colostrum is 1mg / ml;

[0114] (5) Preparation of lipid microsphere injection: transfer the diluted colostrum in s...

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Abstract

The invention relates to a flurbiprofen acetaminophen resin lipid microsphere injection, a freeze-drying lipid microsphere injection and a preparation method. Through a reasonable composition proportion and a preparation process with controllable parameters, good stability and strong operability, the flurbiprofen acetaminophen resin which is an indissolvable drug is wrapped in an oil phase and an interfacial film of a lipid microsphere, so that not only is the solubility of the drug remarkably strengthened, but also precipitation and oxidation do not occur easily, the physical and chemical stabilities of the drug are greatly improved, the devitrification phenomenon is avoided in the use and storage processes, a slow release effect is exerted and the action time of the drug in the blood plasma is prolonged, meanwhile, as the lipid microsphere targets to an inflammation part, the toxicity and the vessel stimulation during injection are remarkably reduced, the clinical application of the injections is safer, the treatment effect is more remarkable, and the injections and the methods are suitable for industrialized production and clinical application.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to non-steroidal anti-inflammatory and analgesic drug injections, in particular to a flurbiprofen acetaminophen ester lipid microsphere injection, a freeze-dried lipid microsphere injection and a preparation method. Background technique [0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of drugs with antipyretic and analgesic effects, and most of them also have anti-inflammatory and anti-rheumatic effects. Can be divided into antipyretic analgesics and anti-inflammatory analgesics. Non-steroidal anti-inflammatory drugs all inhibit the activity of cyclooxygenase (Cyclooxygenase, COX), thereby inhibiting the production of prostacyclin (PGI1), prostaglandin (PGE1, PGE2) and thromboxane A2 (TXA2) from arachidonic acid , and ultimately play an anti-inflammatory and analgesic role. The therapeutic effects of most NSAIDs are due to their inhibition of COX-2, but their adverse effec...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/216A61P29/00
Inventor 杨凌葛广波洪沫宁静邹超
Owner WUXI ERYUN TECH CO LTD
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