Cefuroxime axetil lipid microsphere solid preparation

The technology of cefuroxime axetil and furoxacil axetil is applied in the field of medicine and can solve the problems of low cefuroxime axetil liposome encapsulation rate, unsatisfactory solubility of cefuroxime axetil, low bioavailability and the like, To achieve the effect of improving drug therapeutic index, increasing quality stability, and reducing drug side effects

Inactive Publication Date: 2011-06-15
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But the cefuroxime axetil liposome encapsulation rate that this patent method makes is not high, and leakage rate is high, and the solubility of cefuroxime axetil is not ideal simultaneously, causes bioavailability not high
[0010] Chinese patent CN1939305A discloses a kind of cefuroxime axetil liposome and preparation method thereof, is made up of cefuroxime axetil, soybean lecithin and cholesterol, and the three weight ratios are 1: 2: 2, and the liposome that makes improves improved the solubility of cefuroxime axetil, but the preparation method of this patent is relatively loaded down with trivial details, and the encapsulation efficiency of this liposome is low, and leakage rate is high, and stability is not good
[0012] However, the challenge in preparing lipospheres lies in the selection of appropriate components and preparation methods

Method used

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  • Cefuroxime axetil lipid microsphere solid preparation
  • Cefuroxime axetil lipid microsphere solid preparation
  • Cefuroxime axetil lipid microsphere solid preparation

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preparation example Construction

[0042] On the other hand, the present invention provides the preparation method of above-mentioned cefuroxime axetil lipid microsphere solid preparation, and this method comprises:

[0043] Add gum arabic, sodium deoxycholate and polysorbate 80 into purified water, then add cefuroxime axetil and mix evenly, heat and stir in a water bath at 70-90°C until it melts, use a tissue masher to shear and stir to obtain the primary emulsion , and then cyclically emulsified by a high-pressure homogenizer to obtain an emulsion, and then freeze-dried or spray-dried to obtain lipid microspheres.

[0044] In a preferred embodiment of the preparation method of the cefuroxime axetil lipid microsphere solid preparation of the present invention, the tissue masher used is a JJ-2B type high-speed tissue masher, and the rotating speed for shearing is 12000-15000r / min, The time for shearing and stirring is 10-20 minutes.

[0045] Among them, as a high-pressure milk homogenizer, the model NS1001L im...

Embodiment 1

[0070] The preparation of embodiment 1 cefuroxime axetil lipid microsphere tablet

[0071] The raw and auxiliary materials used are as follows:

[0072] Cefuroxime Axetil 125g

[0073] Gum Arabic 500g

[0074] Sodium deoxycholate 225g

[0075] Polysorbate 80 312.5g

[0076] Starch 800g

[0077] Microcrystalline Cellulose 200g

[0078] Croscarmellose Sodium 200g

[0079] Povidone K30 50g

[0080] Magnesium Stearate 50g

[0081] Preparation Process:

[0082] (1) Add 500g of gum arabic, 225g of sodium deoxycholate and 312.5g of polysorbate 80 into 2000ml of purified water, then add 125g of cefuroxime axetil and mix evenly, heat and stir in a water bath at 90°C until it melts, and use a tissue masher Shearing and stirring for 20 minutes at a rotational speed of 12000r / min to obtain the first emulsion, and then cyclically emulsifying it through a high-pressure homogenizer for 5 times to obtain an emulsion, and then freeze-drying to obtain lipid microspheres.

[0083] (2) ...

Embodiment 2

[0084] Example 2 Preparation of Cefuroxime Axetil Lipid Microsphere Capsules

[0085] The raw and auxiliary materials used are as follows:

[0086] Cefuroxime Axetil 125g

[0087] Gum Arabic 875g

[0088] Sodium deoxycholate 625g

[0089] Polysorbate 80 375g

[0090] Microcrystalline Cellulose 1000g

[0091] Carboxymethyl Starch Sodium 500g

[0092] Povidone K30 20g

[0093] Talc powder 100g

[0094] Preparation Process:

[0095](1) Add 875g of gum arabic, 625g of sodium deoxycholate and 375g of polysorbate 80 into 9000ml of purified water, then add 125g of cefuroxime axetil and mix evenly, heat and stir in a water bath at 70°C until it melts, and cut it with a tissue masher. Cut and stir for 10 minutes at a rotational speed of 15000r / min to obtain the primary emulsion, and then circulate and emulsify it through a high-pressure homogenizer for 5 times to obtain an emulsion, which is then spray-dried to obtain lipid microspheres.

[0096] (2) Mix the prepared lipid mic...

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Abstract

The invention provides a cefuroxime axetil lipid microsphere solid preparation which is prepared from the following raw and auxiliary materials in parts by weight: 1 part of cefuroxime axetil, 3-11 parts of arabic gum, 0.4-8 parts of deoxysodium cholate and 1.5-10 parts of polysorbate 80. The cefuroxime axetil lipid microsphere solid preparation provided by the invention has the advantages of improved dissolution rate, improved bioavailability, high stability and increased quality stability, is suitable for being degraded in vivo, and does not have toxicity and immunogenicity. Especially, a large amount of test data proves that the preparation provided by the invention can be used as a medicament carrier to improve the medication index, improve the product quality of the preparation, reduce toxic side effects, reduce medicament doses and the like.

Description

technical field [0001] The invention relates to a lipid microsphere preparation, in particular to a cefuroxime axetil lipid microsphere solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefuroxime axetil (Ceftin), chemical name (6R, 7R)-7-[2-furyl (methoxyimino) acetamido]-3-carbamoyloxymethyl-8-oxo -5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 1-acetoxyethyl ester, molecular formula: C 20 h 22 N 4 o 10 S, the molecular weight is 510.48, the structural formula is as follows: [0003] [0004] Cefuroxime axetil is a semi-synthetic second-generation cephalosporin drug. It is a prodrug of cefuroxime with broad-spectrum antibacterial activity. It was launched by Glaxo-Wellcome in 1988. CEFTIN), the trade name of domestic generic drugs is Xinjunling. Cefuroxime axetil shows antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and anaerobic bacteria, has broad-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/36A61P31/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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