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Medicine composition containing cefateram cyclodextrin capsule and its preparing method

A technology of cyclodextrin inclusion compound and cefditoren axetil, which is applied in the field of pharmaceutical composition containing cefditoren axetil cyclodextrin inclusion compound and its preparation, and can solve problems such as difficulty in the pharmaceutical adaptability of cefditoren axetil , to achieve the effect of improving oral bioavailability, high water solubility and enhancing drug stability

Inactive Publication Date: 2007-07-18
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

Therefore, the use of cyclodextrins to improve the pharmaceutical suitability of cefditoren pivoxil is difficult and unpredictable

Method used

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  • Medicine composition containing cefateram cyclodextrin capsule and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Mix 20g of β-cyclodextrin with 20ml of pure water, heat, add 10g of cefditoren axetil at 40°C, mix thoroughly for 3 hours, then add dilute NaHCO drop by drop 3 Solution to system pH 8.5-9.0, add dilute hydrochloric acid dropwise to pH 6.5-7.0 after 1 hour, then cool, keep at 5°C for 24 hours; cold filter, wash with cold water twice, and dry under reduced pressure at room temperature to obtain a yellow solid clathrate. The clathrate obtained can be used to prepare pharmaceutical compositions.

Embodiment 2

[0075] Basically the same as Example 1, but using 30g of β-cyclodextrin and 150ml of pure water. The obtained solid clathrate is directly packed into capsules, so that each capsule contains 50 mg of the main drug.

Embodiment 3

[0077] Basically the same as Example 1, but using 50g of β-cyclodextrin and 150ml of pure water. The clathrate obtained can be used to prepare pharmaceutical compositions.

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PUM

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Abstract

A composite medicine with high solubility, stability and activity and low hemolytic irritation contains cefteram ester and the pharmacologically acceptable dextrin chosen from beta-cyclodextrin and its derivatives. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing cephalosporin antibiotic cyclodextrin inclusion complex and a preparation method thereof. Background technique [0002] Cefdteren pivoxil, English name: Cefteram Pivoxil, synonym: Cefdteram neopentyl pivoxil, trade name: Tomiron, chemical name (+)-(6R, 7R)-7-[(z)- 2-(2-Amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-[(5-methyl-2H-tetrazol-2-yl)-methyl]-8-oxo pivaloyloxymethyl 5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate, molecular formula C 22 h 27 N 9 o 7 S 2 , molecular weight 593.63. This product is a solid insoluble in water, melting point: about 110°C, good photothermal stability in solid state, unstable in solution, and decomposes rapidly when encountering acid and alkali. [0003] This product is the third-generation oral cephalosporin, which is the prodrug of cefdteren modified by ester group structure. Its own activity is relatively weak. It has broad-spectrum antibact...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K47/40A61P31/04
Inventor 任勇高剑锋孙海松韩彬彬吴玲孙晓东
Owner 海南和德通医药科技信息咨询有限公司
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