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A sustained-release microsphere preparation contain flurbiprofen and its preparation method

A slow-release microsphere preparation, flurbiprofen technology, which is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, anti-inflammatory agents, etc., can solve the problems of easy crystallization and poor stability, etc. , to extend shelf life, improve storage stability, improve drug loading and encapsulation efficiency

Active Publication Date: 2019-01-18
GUANGDONG JIABO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to overcome the poor stability of the flurbiprofen sustained-release microsphere preparations in the prior art, the prior art deficiencies that crystallization is prone to occur during use and storage, the object of the present invention is to provide a kind of flurbiprofen containing flurbiprofen The slow-release microsphere preparation is prepared from the following raw materials in parts by weight: 10-100 parts of polyester, 2-5 parts of flurbiprofen

Method used

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  • A sustained-release microsphere preparation contain flurbiprofen and its preparation method
  • A sustained-release microsphere preparation contain flurbiprofen and its preparation method
  • A sustained-release microsphere preparation contain flurbiprofen and its preparation method

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Embodiment 1

[0025] Embodiment 1 The present invention comprises flurbiprofen sustained-release microsphere preparation and preparation method thereof

[0026] A preparation containing flurbiprofen sustained-release microspheres, which is prepared from the following raw materials in parts by weight: 10 g of polyester, 2 g of flurbiprofen, an emulsifier of 0.2% of the organic phase of the sustained-release microspheres, and a stabilizer It is 0.01% of the organic phase of sustained-release microspheres. The polyester is polylactic acid-polyethylene glycol with a molecular weight of 15000 and an intrinsic viscosity of 0.5dL / g, wherein the molar ratio of lactic acid to ethylene glycol in the polylactic acid-polyethylene glycol is 70:30. The emulsifier is poloxamer, and the stabilizer is disodium EDTA.

[0027] The preparation method of the described sustained-release microsphere preparation comprising flurbiprofen comprises:

[0028] (1) Prepare the drug-containing organic phase: mix flurbi...

Embodiment 2

[0032] Embodiment 2 The present invention comprises flurbiprofen sustained-release microsphere preparation and preparation method thereof

[0033] A preparation containing flurbiprofen sustained-release microspheres, which is prepared from the following raw materials in parts by weight: 100 g of polyester, 5 g of flurbiprofen, an emulsifier of 0.6% of the organic phase of the sustained-release microspheres, and a stabilizer 0.05% of the organic phase of the slow-release microspheres. The polyester is polylactic acid-polyethylene glycol with a molecular weight of 12000 and an intrinsic viscosity of 0.45dL / g, wherein the molar ratio of lactic acid to ethylene glycol in the polylactic acid-polyethylene glycol is 50:50. The emulsifier is poloxamer, and the stabilizer is disodium EDTA.

[0034] The preparation method of the described sustained-release microsphere preparation comprising flurbiprofen comprises:

[0035] (1) Preparation of the drug-containing organic phase: mixing f...

Embodiment 3

[0039] Embodiment 3 The present invention comprises flurbiprofen sustained-release microsphere preparation and preparation method thereof

[0040] A preparation containing flurbiprofen sustained-release microspheres, which is prepared from the following raw materials in parts by weight: 55 g of polyester, 3.5 g of flurbiprofen, and the emulsifier is 0.4% of the organic phase of the sustained-release microspheres, stable The agent is 0.03% of the organic phase of the slow-release microspheres. The polyester is polylactic acid-polyethylene glycol with a molecular weight of 13500 and an intrinsic viscosity of 0.5dL / g, wherein the molar ratio of lactic acid to ethylene glycol in the polylactic acid-polyethylene glycol is 60:40. The emulsifier is poloxamer, and the stabilizer is disodium EDTA.

[0041] The preparation method of the described sustained-release microsphere preparation comprising flurbiprofen comprises:

[0042] (1) Preparation of the drug-containing organic phase: ...

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Abstract

The invention relates to a sustained-release microsphere preparation containing flurbiprofen and a preparation method thereof, belonging to the pharmaceutical preparation field. In order to overcome the shortcomings of the prior art that flurbiprofen sustained-release microsphere preparation has poor stability and is prone to crystallization during use and storage, it is an object of the present invention to provide a sustained-release microsphere preparation containing flurbiprofen, wherein the sustained-release microsphere preparation is prepared from the following raw materials in parts byweight: 10-100 parts of polyester and 2-5 parts of flurbiprofen, and that sustained-release microsphere preparation further comprises an emulsifying agent and a stabilizing agent. A sustain release microsphere preparation prepared by that solvent evaporation method has high encapsulation efficiency and drug load, stable property and no obvious change in encapsulation efficiency and drug load during long-term storage, thus effectively prolonging the storage time of medicament and improving the quality stability of medicament.

Description

technical field [0001] The invention relates to a sustained-release microsphere preparation containing flurbiprofen and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] The chemical name of flurbiprofen is (±)-2-(2-fluoro-4-biphenyl)-propionic acid, white or off-white crystalline powder. Soluble in methanol, ethanol, acetone or ether, soluble in acetonitrile, almost insoluble in water. The molecular formula is C15H13FO2, the molecular weight is 244.26100, the density is 1.279g / cm3 (25°C), the melting point is 110-112°C (lit.), and the boiling point is 376°C. Clinically, it is mainly suitable for rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, etc. It can also be used for symptomatic treatment of soft tissue diseases (such as sprains and strains) and mild to moderate pain (such as dysmenorrhea and postoperative pain, toothache, etc.). [0003] Flurbiprofen is a propionic acid non-steroidal anti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/192A61K47/34A61K47/36A61P19/02A61P19/08A61P29/00A61P19/04
CPCA61K9/1075A61K31/192A61K47/34A61K47/36A61P19/02A61P19/04A61P19/08A61P29/00
Inventor 李庆曾少群彭创业蔡文坚岳峰
Owner GUANGDONG JIABO PHARM CO LTD
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