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Cefaclor submicro-emulsion solid preparation and novel application thereof

A solid preparation, cefaclor technology, applied in the field of medicine, can solve the problems of low bioavailability, poor stability, etc., and achieve the effect of simple production process, low cost, and improved drug therapeutic index

Inactive Publication Date: 2010-05-26
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The object of the present invention is to provide a kind of cefaclor microemulsion solid preparation and new application thereof, specifically, the solid preparation and new application thereof of the cefaclor through microemulsification process, well solve the cephalosporin currently on the market Problems of poor stability and low bioavailability of Crow solid preparations, and it can also be used to prepare drugs for the treatment of bacterial peritonitis, and satisfactory technical results have been obtained

Method used

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  • Cefaclor submicro-emulsion solid preparation and novel application thereof
  • Cefaclor submicro-emulsion solid preparation and novel application thereof
  • Cefaclor submicro-emulsion solid preparation and novel application thereof

Examples

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Effect test

Embodiment 1

[0027] The preparation of embodiment 1 cefacloride microemulsion particles

[0028] Add 200g of soybean lecithin, 100g of poloxamer 188 and 150g of sodium glycocholate into 3000ml of water for injection, then add 100g of cefaclor and mix evenly, heat and stir in a water bath at 80°C until it melts, and cut it with a tissue masher Stir for 10 min at a speed of 15000 r / min to obtain the first emulsion, then circulate and emulsify through a high-pressure homogenizer for 5 times to obtain an emulsion, then freeze-dry in a large plate, and pulverize to obtain 522 g of submicron emulsion particles of cefaclor, with a yield of 94.9%.

Embodiment 2

[0029] The preparation of embodiment 2 cefacloride microemulsion particles

[0030] Add 1200g of soybean lecithin, 600g of poloxamer 188 and 1200g of sodium glycocholate into 20000ml of water for injection, then add 100g of cefaclor and mix evenly, heat and stir in a water bath at 90°C until it melts, and cut it with a tissue masher Stir for 20 minutes at a speed of 12000r / min to obtain the first emulsion, then circulate and emulsify it through a high-pressure homogenizer for 5 times to obtain an emulsion, and then spray dry to obtain 2868 g of submicron emulsion particles of cefaclor with a yield of 92.5%.

Embodiment 3

[0031] The preparation of embodiment 3 cefaclor tablets

[0032]The 68.7g cefaclor microemulsion granules, 45g starch, 57g microcrystalline cellulose and 12g carboxymethyl starch sodium prepared in Example 1 were passed through 80 mesh sieve respectively, then mixed homogeneously, and 5% povidone K was added 30 30ml of 80% ethanol solution was used to make soft materials, granulated with a 20-mesh sieve, dried at 60°C, granulated with a 20-mesh sieve, then added with 2.4g of magnesium stearate, mixed evenly, and compressed into tablets to obtain cefaclor tablets.

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Abstract

The invention aims at providing a cefaclor submicro-emulsion solid preparation and a novel application thereof, in particular to a solid preparation of cefaclor processed by micro-emulsification and a novel application thereof. The invention solves the problems of poor stability and low bioavailability of the on-sale cefaclor solid preparation at present very well, can also be used for preparing a medicine for treating bacterial peritonitis and obtains a satisfactory technical effect.

Description

technical field [0001] The invention relates to a cefaclor microemulsion solid preparation and its new application, in particular to a cefaclor microemulsified solid preparation and its new application, belonging to the technical field of medicine. Background technique [0002] Bacterial peritonitis refers to acute bacterial peritonitis caused by liver disease or kidney disease, ascites, and non-abdominal viscera. It may be related to the impairment of reticuloendothelial system function, decreased phagocyte activity, weakened conditioning function, and decreased peritoneal defense against bacteria. In liver cirrhosis with portal hypertension, bacteria are significantly reduced in the liver, and intestinal bacteria may enter the ascites through the intestinal wall and cause translocation infection. Most of the pathogenic bacteria are Escherichia coli, followed by pneumococcus and streptococcus. The widespread use of antibiotics in clinical practice has resulted in drug res...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K9/00A61K31/545A61K47/42A61K47/38A61K47/36A61K47/34A61K47/32A61P31/04A61K47/10A61K47/24A61K47/26A61K47/28
Inventor 陶灵刚
Owner HAINAN MEIDA PHARMA
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