A kind of pharmaceutical composition of flurbiprofen axetil

A flurbiprofen axetil and composition technology, which is applied in the field of flurbiprofen axetil pharmaceutical compositions, can solve the problems of difficult storage, easy oxidation, particle size increase, etc., and achieve non-degradable, good stability, The effect of uniform particle size

Active Publication Date: 2016-03-02
桂林澳林制药有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] But the particle diameter of the flurbiprofen axetil fat emulsion injection that adopts above-mentioned prescription or preparation method to make is all about 200nm, is easy to demulsification
In addition, ordinary fat emulsion injection is a heterogeneous liquid preparation, which is a thermodynamically and kinetically unstable system. During long-term storage, the emulsion droplet particles are easy to merge, resulting in the phenomenon of particle size increase and emulsion droplet agglomeration. It is not easy to store, which limits the Stability and safety of flurbiprofen axetil fat emulsion injection
Moreover, both oil and phospholipids are prone to oxidation, hydrolysis occurs during preparation and storage, and the reduction of oil emulsification will also make the drug unable to be completely encapsulated, thereby increasing the degradation of the main drug flurbiprofen axetil, while the ratio of flurbiprofen to Profen ester degrades to generate flurbiprofen (A) and 1-hydroxyethyl acetate (B), and 1-hydroxyethyl acetate is further degraded into acetic acid (C) and formaldehyde (D), wherein flurbiprofen Fen is an active metabolite, while impurities C and D are impurities that cause safety hazards and need to be strictly controlled

Method used

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  • A kind of pharmaceutical composition of flurbiprofen axetil
  • A kind of pharmaceutical composition of flurbiprofen axetil
  • A kind of pharmaceutical composition of flurbiprofen axetil

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Experimental program
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Effect test

Embodiment 1

[0039] prescription:

[0040]

[0041] Preparation Process:

[0042] 1) Under nitrogen protection, soybean oil and lecithin are heated to 70°C, and while stirring, flurbiprofen axetil and vitamin E are added to dissolve to obtain an oil phase;

[0043] 2) Under nitrogen protection, add glycerol to part of the water for injection, dissolve, and obtain an aqueous phase;

[0044] 3) Under nitrogen protection, add the oil phase of step 1) into the water phase of step 2), disperse by high-speed shearing for 20 minutes, the shearing speed is 6000rpm, then adjust pH=4.5 with a pH adjuster, and add water for injection Dilute to 1000ml, stir to get colostrum;

[0045] 4) Under the protection of nitrogen, add the colostrum into the high-pressure homogenizer, set the high-pressure homogenization pressure to 800bar, and perform high-pressure homogenization 3 times. During the high-pressure homogenization process, adjust the flow of condensed water and control the temperature of the e...

Embodiment 2

[0049] prescription:

[0050]

[0051] Preparation Process:

[0052] 1) Under nitrogen protection, soybean oil and lecithin were heated to 75°C, and while stirring, flurbiprofen axetil and vitamin E were added to dissolve to obtain an oil phase;

[0053] 2) Under nitrogen protection, add glycerol to part of the water for injection, dissolve, and obtain an aqueous phase;

[0054] 3) Under nitrogen protection, add the oil phase of step 1) to the water phase of step 2), disperse by high-speed shearing for 30 minutes, the shearing speed is 8000rpm, then adjust pH=6.5 with a pH adjuster, and add water for injection Dilute the volume to 1000ml and stir to obtain colostrum; the pH adjusting agent is disodium hydrogen phosphate and citric acid buffer, and the dosage is to make the injection pH=6.5, wherein disodium hydrogen phosphate and citric acid The molar ratio is 4:1;

[0055] 4) Under nitrogen protection, add colostrum into the high-pressure homogenizer, set the high-pressur...

Embodiment 3

[0059] prescription:

[0060]

[0061] Preparation Process:

[0062] 1) Under nitrogen protection, soybean oil and lecithin are heated to 72°C, and while stirring, flurbiprofen axetil and vitamin E are added to dissolve to obtain an oil phase;

[0063] 2) Under nitrogen protection, add glycerol to part of the water for injection, dissolve, and obtain an aqueous phase;

[0064] 3) Under nitrogen protection, add the oil phase of step 1) to the water phase of step 2), disperse by high-speed shearing for 25 minutes, the shearing speed is 7000rpm, then adjust pH=5.5 with a pH regulator, and add water for injection Dilute to 1000ml, stir to get colostrum;

[0065] 4) Under nitrogen protection, add colostrum into the high-pressure homogenizer, set the high-pressure homogenization pressure to 800bar, and perform high-pressure homogenization 4 times. During the high-pressure homogenization process, adjust the flow of condensed water and control the temperature of the emulsion to n...

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Abstract

The invention belongs to the technical field of medicines and in particular relates to a pharmaceutical composition of flurbiprofen axetil. The pharmaceutical composition of the flurbiprofen axetil is a fat emulsion injection and is prepared from the following components in parts by weight: 0.005-0.015g / ml flurbiprofen axetil, 0.1-0.12g / ml soybean oil, 0.01-0.02g / ml lecithin, 0.001-0.002g / ml vitamin E, 0.01-0.03g / ml glycerol and a proper amount of pH regulator. The fat emulsion injection is uniform in particle size, is good in stability, is capable of greatly relieving degradation of the flurbiprofen axetil so as to reduce generation of other impurities and lower safety hidden dangers and is good in dilution stability of compatibility.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition of flurbiprofen axetil. Background technique [0002] Flurbiprofen axetil is a non-steroidal anti-inflammatory drug, and 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 relieve pain. effect. Its analgesic effect is stronger than aspirin, even more than analgesic new. [0003] Flurbiprofen axetil, its chemical name is: (±) 2-(2-fluoro-4-biphenyl) propionate-1-acetoxyethyl ester, molecular formula: C 19 H 19 FO 4 , molecular weight: 330.36, its structural formula is: [0004] [0005] Flurbiprofen axetil is insoluble in water and needs to be made into a liquid emulsion suitable for intravenous injection. Flurbiprofen axetil fat emulsion injection (trade name Kaifen) is a preparation based on the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/216A61K9/107A61K47/22A61P29/00
CPCA61K9/0019A61K9/107A61K31/216A61K47/10A61K47/22A61K47/24A61K47/44
Inventor 黄文豪
Owner 桂林澳林制药有限责任公司
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