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A kind of stable flurbiprofen axetil micro-nano emulsion and preparation method thereof

A technology of flurbiprofen axetil and micro-nano emulsion, which is applied in the direction of emulsion delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of easy demulsification, pain, and liver fat metabolism To avoid problems such as heavy burden, achieve good thermodynamic stability, reduce injection pain, and reduce vascular stimulation

Active Publication Date: 2016-08-24
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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  • A kind of stable flurbiprofen axetil micro-nano emulsion and preparation method thereof
  • A kind of stable flurbiprofen axetil micro-nano emulsion and preparation method thereof
  • A kind of 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 of egg yolk lecithin and 3g of polyethylene glycol-tocopherol palmitate, add them to 150g of soybean oil and 150g of medium-chain triglycerides, and stir at 30°C under the condition of nitrogen protection 20min to fully dissolve, then add 10g flurbiprofen axetil, dissolve and mix well, as the oil phase;

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

[0044] (3) Preparation of colostrum: under nitrogen protection and a temperature of 30°C, add the oil phase of step (1) into the water phase of step (2), 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 the condition of ...

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-vitamin E succinate and add them to 87.5g soybean oil and 87.5g medium-chain triglycerides. Under the conditions, stir at 40°C for 20 minutes to fully dissolve, then add 45g of flurbiprofen axetil, dissolve and mix well, as the oil phase;

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

[0054] (3) Preparation of colostrum: under nitrogen protection and a temperature of 40°C, add the oil phase of step (1) into the water phase of step (2), 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 a...

Embodiment 3

[0058] prescription

[0059]

[0060] Process:

[0061] (1) Preparation of oil phase: Take 11g egg yolk lecithin, 6.0g sodium oleate, 40g polyethylene glycol-vitamin E palmitate, add 25g soybean oil and 25g medium chain triglyceride, under the condition of nitrogen protection , stirred at 20°C for 20 minutes to fully dissolve, then added 80 g of flurbiprofen axetil, dissolved and mixed evenly, as the oil phase;

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

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

[0064] (4) High-pressure homogenization: Under the con...

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Abstract

The invention relates to a stable flurbiprofen axetil micro-nano emulsion and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. A stable flurbiprofen axetil micro-nano emulsion of the present invention contains flurbiprofen axetil, vegetable oil as a solvent, lecithin as a surfactant, polyethylene glycol derivatives, etc., has good stability, Quick effect, low toxicity and side effects.

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, belonging to the technical field of pharmaceutical preparations. Background technique [0002] The chemical name of flurbiprofen axetil is (±) 2-(2-fluoro-4-biphenyl) propionate-1-acetoxyethyl ester, which belongs to non-steroidal anti-inflammatory drugs. Its mechanism of action is mainly to inhibit the activity of cyclooxygenase in the cascade cascade of arachidonic acid, thereby inhibiting the synthesis of prostaglandins that cause pain and inflammation, and play an analgesic role. Its analgesic effect is stronger than that of aspirin, and even surpasses the new analgesic. Flurbiprofen axetil is a prodrug prepared by esterification of flurbiprofen, which is lipophilic. After intravenous injection, it can be rapidly hydrolyzed into the active substance flurbiprofen, and the plasma ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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