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Stable flurbiprofen axetil micro-nano-emulsion and preparation method thereof

A technology of flurbiprofen axetil and micro-nano emulsion, which is applied in the fields of emulsion delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc. Pain and other problems, to achieve good thermodynamic stability, small and uniform particles, reduce the effect of injection pain

Active Publication Date: 2014-12-10
HEBEI YIPIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example: the risk of hypertriglyceridemia is greater, and the burden of liver fat metabolism is heavier, especially for patients with lipid metabolism disorders.
Therefore, in order to improve the safety of flurbiprofen axetil fat emulsion, patents CN101940549A and CN102552133A disclose a kind of medium / long-chain triglyceride flurbiprofen axetil injection and its preparation method, all adopting a certain proportion of easy human body absorption The fat emulsion prepared with digested medium-chain and long-chain triglycerides as auxiliary materials solves the safety hazards such as hyperlipidemia caused by using long-chain triglycerides alone
[0004] Yet the prescription of existing flurbiprofen axetil fat emulsion injection and preparation technology still have following shortcoming: the first, in the high-temperature sterilization of preparation technology or still may occur demulsification, delamination phenomenon, due to high temperature and Oxidation and degradation reactions of soybean oil and phospholipids still exist under high-speed shearing, which increases the degradation of the main flurbiprofen axetil, affects the stability of the preparation, and thus affects the clinical application of the preparation
Second, the particle size of the flurbiprofen axetil fat emulsion disclosed in the current literature is about 300nm, which is easy to break the emulsion and cause pain during injection
However, the stability of fat emulsion is poor, and the half-life in blood is short, so the drug tissue targeting of this existing preparation also needs to be enhanced
Fourth, flurbiprofen axetil is easily hydrolyzed into flurbiprofen and 1-hydroxyethyl acetate, and the latter is further degraded into acetic acid (impurity A) and formaldehyde impurities (impurity B), thereby affecting the safety of the preparation, need strict control

Method used

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  • Stable flurbiprofen axetil micro-nano-emulsion and preparation method thereof
  • Stable flurbiprofen axetil micro-nano-emulsion and preparation method thereof
  • Stable flurbiprofen axetil micro-nano-emulsion and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] prescription

[0040]

[0041] Process:

[0042] (1) Preparation of the oil phase: Take 3.0g egg yolk lecithin, 3g polyethylene glycol-tocopherol palmitate, add 150g soybean oil and 150g medium chain triglycerides, and stir at 30°C under nitrogen protection 20min to fully dissolve, then add 10g flurbiprofen axetil, dissolve and mix evenly, as the oil phase;

[0043] (2) Preparation of the water phase: under the conditions of nitrogen protection and a temperature of 30°C, take 500 ml of water for injection, add 30 g of glycerin, and stir to dissolve it as the water phase;

[0044] (3) Preparation of colostrum: under nitrogen protection and temperature 30℃, add step (1) oil phase to step (2) water phase, high-speed shear dispersion, shear speed 10000rpm, time 15 minutes to form Colostrum, and adjust the total amount to 1000ml with water for injection;

[0045] (4) High-pressure homogenization: Under nitrogen protection and a temperature of 30°C, the colostrum obtained in step (3)...

Embodiment 2

[0049] prescription

[0050]

[0051] Process:

[0052] (1) Preparation of the oil phase: take 20g egg yolk lecithin, 3.0g sodium oleate, 20g polyethylene glycol-tocopherol succinate and add 87.5g soybean oil and 87.5g medium chain triglycerides, in a nitrogen protected Under the conditions, stir at 40°C for 20 minutes to fully dissolve, then add 45g flurbiprofen axetil, dissolve and mix well, as the oil phase;

[0053] (2) Preparation of water phase: Take 500ml of water for injection under the condition of nitrogen protection and temperature of 40°C, add 10g of glycerin, stir to dissolve it, as the water phase;

[0054] (3) Preparation of colostrum: under nitrogen protection and temperature 40℃, add step (1) oil phase to step (2) water phase, high-speed shear dispersion, shear speed 8000rpm, time 35 minutes to form Colostrum, and adjust the total amount to 1000ml with water for injection;

[0055] (4) High-pressure homogenization: Under nitrogen protection and a temperature of 40°C, ...

Embodiment 3

[0058] prescription

[0059]

[0060] Process:

[0061] (1) Preparation of the oil phase: take 11g egg yolk lecithin, 6.0g sodium oleate, 40g polyethylene glycol-tocopherol palmitate and add 25g soybean oil and 25g medium chain triglycerides, under nitrogen protection , Stir at 20°C for 20min to fully dissolve, then add 80g flurbiprofen axetil, dissolve and mix well, as the oil phase;

[0062] (2) Preparation of the water phase: under the condition of nitrogen protection and temperature of 20°C, take 500ml of water for injection, add 50g of glycerin, stir to dissolve it, and serve as the water phase;

[0063] (3) Preparation of colostrum: under the condition of nitrogen protection and temperature of 20℃, add the oil phase of step (1) to the water phase of step (2), high-speed shear dispersion, shear speed 7000rpm, time 40 minutes, and form Colostrum, and adjust the total amount to 1000ml with water for injection;

[0064] (4) High-pressure homogenization: Under the conditions of nitro...

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Abstract

The invention relates to a stable flurbiprofen axetil micro-nano-emulsion and a preparation method thereof, and belongs to the technical field of medicine preparations. The stable flurbiprofen axetil micro-nano-emulsion is prepared from flurbiprofen axetil, plant oil serving as a solvent, lecithin serving as a surfactant, a polyethylene glycol derivative and the like, and has the characteristics of good stability, quick response, low toxic and side effect and the like.

Description

Technical field [0001] The invention relates to an emulsion and a preparation method thereof, in particular to a stable flurbiprofen axetil micro-nano emulsion and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] The chemical name of flurbiprofen axetil is (±)2-(2-fluoro-4-biphenyl)propionic acid-1-acetoxyethyl ester, which is a non-steroidal anti-inflammatory drug. Its mechanism of action is mainly to inhibit the activity of cyclooxygenase in the arachidonic acid cascade, thereby inhibiting the synthesis of prostaglandins that cause pain and inflammation, and play an analgesic effect. Its analgesic effect is stronger than that of aspirin, and even surpasses that of analgesia. Flurbiprofen axetil is a prodrug prepared by esterification of flurbiprofen and has lipophilicity. After intravenous injection, it can be quickly hydrolyzed into the active substance flurbiprofen. After 5-10 minutes, the plasma ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/216A61K47/34A61P29/00
Inventor 武玉洁周冉张晓彩可方远程瑶邱玉敏贾宗英
Owner HEBEI YIPIN PHARMA
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