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Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method

A technology of cyclodextrin inclusion compound and cefuroxime axetil, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, and pharmaceutical formulas, which can solve the problems of increasing costs and increasing safety risks in clinical application of drugs , increase the environmental protection work of producers and other issues, and achieve the effect of easy dissolution, strong activity and good stability

Inactive Publication Date: 2007-07-25
海南和德通医药科技信息咨询有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the conventional preparation methods of clathrates in the prior art, organic solvents are usually used, or a large amount of organic solvents are used, which not only increases the cost of preparation, but also increases the safety hazards of clinical application of drugs, and also increases the environmental protection of producers. Work

Method used

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  • Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method
  • Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method
  • Medicine composition containing ceftin cyclodextrin clathrate, and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Mix 300.0g β-cyclodextrin with 300ml pure water, heat, add 60.0g cefuroxime axetil at 50°C, mix well, then add dilute NaHCO drop by drop 3 Solution to pH = 8.0, cooled to room temperature, mixed and ground for 3 hours, then adjusted to pH = 7.0 with dilute HCl acid solution, cooled at 5°C for 24 hours; filtered, washed once with water, and dried under reduced pressure at room temperature to obtain yellow Solid clathrate.

[0079] Mix 360g of solid clathrate (containing 60g of cefuroxime axetil) with 100g of pregelatinized starch, 30g of microcrystalline cellulose, and 10g of croscarmellose sodium, grind them uniformly through a 100-mesh sieve, dry granulate, and prepare The obtained granules are mixed with 2.0g talcum powder and 1.0g magnesium stearate, granulated through a 16-mesh sieve, and compressed to obtain 1000 cefuroxime axetil inclusion tablets, each containing cefuroxime axetil 60mg.

Embodiment 2

[0081] It is basically the same as Example 1, but using 240g β-cyclodextrin and 60g hydroxypropyl-β-cyclodextrin, and after adjusting the dilute HCl acid solution to pH=7.0, remove water under reduced pressure at a temperature of 50°C, after Dry under reduced pressure at room temperature to obtain a yellow solid clathrate.

Embodiment 3

[0083] It is basically the same as Example 1, but using 240g of β-cyclodextrin and 60g of sulfobutyl-β-cyclodextrin, in addition, after the dilute HCl acid solution is adjusted to pH = 7.0, water is removed under reduced pressure at a temperature of 50°C, after Dry under reduced pressure at room temperature to obtain a yellow solid clathrate.

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PUM

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Abstract

An inclusion compound of cefuroxime axetil with high solubility, stability and activity contains cefuroxime axetil and the pharmacologically acceptable cyclodextrin chosen from alpha-cyclodextrin, beta-cyclodextrin, gamma-cyclodextrin and their derivatives. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a pharmaceutical composition of a cephalosporin antibiotic cyclodextrin inclusion compound containing an ester prodrug structure and a preparation method thereof. Background technique [0002] Cefuroxime axetil (cefuroxime axetil), is the prodrug of cephalosporin antibiotic cefuroxime, chemical name: (6R, 7R)-7-[2-furyl (methoxyimino) acetamido]-3-amino Formyloxymethyl-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, molecular weight: 510.48. Cefuroxime axetil is an ester prodrug screened from various derivatives of cefuroxime C4 carboxyl modified by different ester groups. The in vitro test of cefuroxime axetil has very low activity relative to cefuroxime, while in animals Tests have shown that cefuroxime axetil is well absorbed and can be efficiently activated by enzymes to take effect as the prototype drug cefuroxime (GB1571683). In clinical pra...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K47/48A61P31/04A61K47/69
Inventor 任勇高剑锋韩彬彬马学琴吴玲孙晓东
Owner 海南和德通医药科技信息咨询有限公司
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