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Flurbiprofen paracetamol lipid microsphere injection, freeze-dried lipid microsphere injection and preparation method

A technology of acetaminophen ester lipid and acetaminophen ester, which can be used in freeze-dried delivery, anti-inflammatory agents, pharmaceutical formulations, etc., and can solve the problems of small dosage, long-term stability, venous irritation, etc.

Active Publication Date: 2016-08-03
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 injection with small dosage, high safety, good long-term stability and small vein irritation medicine, benefiting the majority of patients, but there is no related report

Method used

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  • Flurbiprofen paracetamol lipid microsphere injection, freeze-dried lipid microsphere injection and preparation method
  • Flurbiprofen paracetamol lipid microsphere injection, freeze-dried lipid microsphere injection and preparation method
  • Flurbiprofen paracetamol lipid microsphere injection, freeze-dried lipid microsphere injection and preparation method

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 high-speed stirring at 8000rpm, 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 i...

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Abstract

The invention relates to a flurbiprofen acetaminophen ester lipid microsphere injection, a freeze-dried lipid microsphere injection and a preparation method. The present invention wraps the insoluble drug flurbiprofen acetaminophen ester in the oil phase and interfacial membrane of lipid microspheres through a preparation process with reasonable composition ratio and controllable parameters, good stability and strong operability It not only significantly enhances the solubility of the drug, but also is not easy to precipitate and oxidize, greatly improving the physical and chemical stability of the drug, avoiding the crystallization phenomenon in the process of use and storage; it also has a sustained release effect, prolonging the drug The action time in plasma; at the same time, because the lipid microspheres are targeted to the inflammatory site, it can significantly reduce the toxicity and vascular irritation during injection, and the clinical application is safer and the curative effect is more significant, which is suitable for industrial production and clinical practice. 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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Patent Type & Authority Patents(China)
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