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Solid cefprozi lipid nanoparticle preparation

A cefprozil, solid lipid nanotechnology, applied in the field of medicine, to achieve the effects of increasing concentration, improving solubility, and improving controlled release effect

Inactive Publication Date: 2012-12-19
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, the challenge in preparing solid lipid nanoparticles lies in the selection of appropriate ingredients and preparation methods

Method used

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preparation example Construction

[0074] On the other hand, the present invention provides the preparation method of cefprozil solid lipid nanoparticle, the method comprises the following steps:

[0075] (a) adding palmitic acid and glyceryl tristearate into an organic solvent, heating in a constant temperature water bath at 50° C., stirring to dissolve it completely, then adding cefprozil, fully stirring to dissolve it, and forming an organic phase;

[0076] (b) dissolving polyoxyethylene 40 stearate in water, heating in a constant temperature water bath at 50°C, and stirring to dissolve it to form a water phase;

[0077] (c) Slowly add the organic phase into the stirring water phase, keep the temperature at 50° C., and continue stirring for 1 h;

[0078] (d) removing the organic solvent under reduced pressure to obtain translucent colostrum;

[0079] (e) the colostrum in the above steps is quickly added to an appropriate amount of cold water under the stirring condition of 2000 rpm, and the high-pressure ho...

Embodiment 1

[0134] The preparation of embodiment 1 cefprozil solid lipid nanoparticle sheet

[0135] The raw materials used are as follows:

[0136]

[0137] Adopt following production process to prepare cefprozil solid lipid nanoparticle sheet:

[0138] (1) 150g of palmitic acid and 75g of glyceryl tristearate are added into 750ml volume ratio in the mixed solvent of chloroform and methyl alcohol of 5: 1, 50 ℃ of constant temperature water baths are heated, and stirring makes it dissolve completely, then adds 125g cefprozil, Thoroughly stir to make it dissolve and form the organic phase;

[0139] (2) Dissolve 100g of polyoxyethylene 40 stearate in 2000ml of water, heat in a constant temperature water bath at 50°C, stir to dissolve, and form a water phase;

[0140] (3) Slowly add the organic phase into the stirring water phase, keep the temperature at 50° C., and continue stirring for 1 h;

[0141] (4) remove organic solvent under reduced pressure, obtain translucent colostrum;

...

Embodiment 2

[0147] The preparation of embodiment 2 cefprozil solid lipid nanoparticle capsules

[0148] The raw materials used are as follows:

[0149]

[0150] Adopt following production process to prepare cefprozil solid lipid nanoparticle capsules:

[0151] (1) 200g of palmitic acid and 100g of glyceryl tristearate are added into 1000ml of a volume ratio of 5: 1 in the mixed solvent of chloroform and methanol, heated in a constant temperature water bath at 50°C, stirred to make it dissolve completely, then add 250g of cefprozil, Thoroughly stir to make it dissolve and form the organic phase;

[0152] (2) Dissolve 80g of polyoxyethylene 40 stearate in 400ml of water, heat in a constant temperature water bath at 50°C, stir to dissolve, and form a water phase;

[0153](3) Slowly add the organic phase into the stirring water phase, keep the temperature at 50° C., and continue stirring for 1 h;

[0154] (4) remove organic solvent under reduced pressure, obtain translucent colostrum;...

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Abstract

The invention discloses a solid cefprozi lipid nanoparticle preparation and a preparation method thereof. Cefprozi, palmitic acid and glycerol tristearate are dissolved in an organic solvent to form an oil phase; and with a water solution of polyoxyethylene 40 stearate as water phase, the cefprozi is entrapped in a solid lipid nanoparticle to obtain the solid cefprozi lipid nanoparticle preparation by adopting a mixed emulsifying and high-pressure uniformly-emulsifying combined method. The solid lipid nanoparticle preparation provided by the invention has the advantages of high drug loading amount, uniformity in grain size, long reservation time of a medicament in blood circulation and better slowly-releasing and controlled-release effects; and the quality of a preparation product is improved and toxic or side effects are reduced. In addition, equipment used by a preparation method is simple, easy for operation and suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a lipid nanoparticle solid preparation, in particular to a cefprozil lipid nanoparticle preparation and a solid preparation method thereof, belonging to the technical field of medicine. . Background technique [0002] Cefprozil, chemical name is (6R,7R)-3-propenyl-7-[(R)-2-amino-2-(4-hydroxyphenyl)acetamido]-8-oxo-5-thia -1-Azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate, molecular formula C 18 h 19 N 3 o 5 S·H 2 O, molecular weight 407.44, structural formula as follows: [0003] [0004] Cefprozil is a non-ester cephalosporin developed by the Bristol-Myers Tokyo Research Institute in 1983. It is an antibiotic that is effective orally, and has a wider and higher antibacterial spectrum and activity than the first-generation cephalexin and cefadroxil. The antibacterial spectrum of cefprozil includes the main Gram-positive and negative bacteria of common respiratory tract infections and urinary tract infections....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/127A61K31/545A61K47/34A61P31/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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