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Flurbiprofen axetil microsphere preparation

A technology of flurbiprofen axetil and lipid microspheres, which is applied in anti-inflammatory agents, non-central analgesics, medical preparations with non-active ingredients, etc., and can solve problems such as demulsification, affecting clinical use of preparations, and stratification

Active Publication Date: 2013-07-17
WUHAN DOCAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the existing flurbiprofen axetil liposphere injection will be affected by factors such as raw materials, preparation conditions and storage conditions during preparation and storage, and there are stability problems. Demulsification and delamination may occur during high temperature sterilization or storage, which will affect the clinical use of the preparation
In addition, the drug tissue targeting of this existing preparation also needs to be enhanced

Method used

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  • Flurbiprofen axetil microsphere preparation
  • Flurbiprofen axetil microsphere preparation
  • Flurbiprofen axetil microsphere preparation

Examples

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preparation example Construction

[0067] The preparation method described above may further comprise the step of removing water from the aqueous preparation using prior art methods to obtain the preparation in dry form, for example, the water-containing liquid preparation may be dehydrated by lyophilization to obtain freeze-drying. preparation.

[0068] The lipid microsphere formulation of the present invention has anti-inflammatory and / or analgesic effects. Therefore, the present invention provides the use of the lipid microsphere preparation for preparing analgesic or anti-inflammatory drugs. In one embodiment, the lipid microspheres of the present invention can be used for postoperative analgesia or cancer analgesia. In another embodiment, the lipid microspheres of the present invention can be used for the prevention and treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis and the like.

[0069] Chitosan is the only macromolecular polysaccharide with cations in nature. It has excellen...

Embodiment 1

[0072] Preheat 100g soybean oil for injection (purchased from Tieling Beiya Medicinal Oil Co., Ltd.) to 70-80°C, add 15g egg yolk lecithin (purchased from Japan Q.P.Corporation, FCPlant), stir to form a uniform oil phase, and slowly add 10g of flurbiprofen axetil crude drug (according to US 5196567 or Guo Daliang et al., the synthesis of flurbiprofen axetil, Qilu Pharmaceutical Affairs, 2007 Volume 26 the method described in the 9th phase is prepared), stir with the speed of 4000rpm to make it Uniformly dissolved in the oil phase; add 25 g of glycerol for injection (purchased from Hunan Erkang Pharmaceutical Co., Ltd.) into an appropriate amount of water for injection preheated to 70-80 ° C, stir to form a homogeneous aqueous phase, and slowly add 5 g of chitosan (purchased from the product). From Zhejiang Golden Shell Biochemical Co., Ltd., the weight average molecular weight is 3.5×10 5 , deacetylation degree 98%), stir for 5min under the condition of 5000rpm to make it even...

Embodiment 2

[0075] Preheat 100g soybean oil for injection to 70~80℃, add 12.5g egg yolk lecithin, stir to form a uniform oil phase, slowly add 10g flurbiprofen axetil API, stir at 5000rpm to make it evenly dissolved in the oil Add 22.5g of glycerin for injection into water for injection preheated to 70-80℃, stir to form a homogeneous water phase, slowly add 10g of chitosan, and stir at 3000rpm for 8min to make it evenly dissolved in the water phase; Under the condition of 10000rpm, the oil phase was slowly dropped into the water phase, stirred for 10min, and the milky white colostrum was formed after uniform dispersion; the pH value of the colostrum was adjusted to 6.3 with disodium hydrogen phosphate and citric acid as pH adjusters, and the diluted The volume was 1L, transferred to a high-pressure homogenizer, and homogenized to an average particle size below 300nm under the conditions of 600bar and 50°C; after filtration with a 1.0 μm microporous membrane, the obtained lipid microsphere ...

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Abstract

The invention provides a flurbiprofen axetil microsphere preparation, a preparation method and an application thereof. The plurbiprofen axetil microsphere preparation comprises flurbiprofen axetil, an oil phase solvent and chitosan and / or derivatives thereof and an emulsifying agent. The method for preparing the flurbiprofen axetil microsphere preparation comprises the following steps of: (1) mixing oil phase mixture containing the flurbiprofen axetil, the oil phase solvent and the emulsifying agent so as to produce a uniform oil phase; (2) mixing aqueous phase mixture containing chitosan and / or the derivatives thereof and water so as to form a uniform aqueous phase; (3) adding the oil phase into the aqueous phase so as to form initial emulsion; and (4) homogenizing the initial emulsion. The invention further provides an application of the flurbiprofen axetil microsphere preparation to be used for preparing analgesic or anti-inflammatory drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a flurbiprofen axetil lipid microsphere preparation comprising chitosan or a derivative thereof. Background technique [0002] Flurbiprofen axetil, whose chemical name is (±) 2-(2-fluoro-4-biphenyl) propionate-1-acetoxyethyl ester, is a non-steroidal analgesic prodrug. The active product of the prodrug, flurbiprofen, is a cyclooxygenase (COX) inhibitor. As a non-steroidal anti-inflammatory drug (NSAID), flurbiprofen has anti-inflammatory and analgesic effects and is clinically used for the treatment of pain or inflammatory diseases. [0003] Most of the commercially available preparations of flurbiprofen are oral preparations, such as flurbiprofen tablets, flurbiprofen sustained-release tablets and the like. Since it has been found that oral flurbiprofen can easily cause adverse reactions such as gastrointestinal disorders, and most patients cannot take oral drugs whe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/192A61K47/36A61K47/44A61P29/00
Inventor 黄岭张文军
Owner WUHAN DOCAN PHARMA
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