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Solid cefprozi lipid nanoparticle preparation

A technology of propylene lipid and cefprozil is applied in the field of medicine and achieves the effects of simple preparation method, reduced toxic and side effects, and improved quality

Inactive Publication Date: 2012-01-25
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 in 750ml volume ratio and be 5: 1 in the mixed solvent of chloroform and methyl alcohol, 50 ℃ of constant temperature water bath heatings, stir and make it dissolve completely, then add 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;

[0142]...

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 Applications(China)
IPC IPC(8): A61K9/14A61K9/127A61K31/545A61K47/34A61P31/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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