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Injection cefteram composition

A technology of cefdram and a composition, applied in the field of cefdram composition for injection, can solve the problems of high cost, waste, inability to be used as an injection and the like

Inactive Publication Date: 2005-12-21
黄文豪
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the medicine still has the following disadvantages: (1) currently marketed dosage forms are tablets and syrups, but due to the low solubility of the medicine in water, the bioavailability of these oral preparations is low, and the remainder is excreted, resulting in A lot of waste; in addition, due to its low solubility, it cannot be directly made into injections
(2) A series of adverse reactions after oral administration of the drug, including gastrointestinal dysfunction, especially diarrhea, accompanied by nausea and vomiting
(3) In the production process of cefditoren pivoxil, it is obtained by the esterification reaction of cefditoren axetil, and the cost is relatively high
But because the water solubility of the pharmaceutically acceptable salt of cefditoren or cefdozelen is also very poor, therefore the injectable antimicrobial drug of cefdozelen or its pharmaceutically acceptable salt also does not appear on the market

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0009] Under aseptic environment, 100 grams of cefditoren sterile powder and 35 grams of sodium carbonate sterile powder are fully dry and physically mixed with a mixer to obtain the cefditoren composition for injection, which is then subpackaged into bottles and sealed with rubber stoppers. Seal the bottle.

Embodiment 2

[0011] Put 100 grams of L-arginine into an aqueous solution reaction bottle containing 100 grams of cefditoren sodium salt, dissolve and mix, add 0.1mol / L sodium hydroxide aqueous solution to adjust the pH to 7.4, and sterilize and filter to obtain ceftiram for injection Lun composition, divided into bottles, sealed with rubber stoppers after drying.

Embodiment 3

[0014] (-) indicates that the sample was not completely dissolved and a precipitate remained.

[0015] (+) indicates that the sample can be completely dissolved without leaving any precipitate.

[0016] The experimental results show that the present invention can improve the solubility of cefditoren in water.

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PUM

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Abstract

The present invention discloses a cefteram composition for injection. It includes cefteram as active component or its medicinal salt and solubility promoter, and the described solubility promoter is basic amino acid or inorganic acid salt of alkali metal or organic acid salt of alkali metal or inorganic acid salt of alkali earth metal or organic acid salt of alkali earth metal. The weight portion ratio of cefteram or its medicinal salt and solubility promoter is 1:0.05-20. Said injection has good antibacterial action, and has good water solubility.

Description

(1) Technical field: [0001] The invention relates to the third-generation cephalosporin antibiotic cefditoren, in particular to a cefditoren composition for injection. (two) background technology: [0002] Cefditoren axetil is the third generation of oral cephalosporin antibiotic prodrugs. Its mechanism of action is mainly to form active cefditoren (which can be called cefditoren acid "Cefteram" after being taken orally into the gastrointestinal tract and hydrolyzed by intestinal wall esterase). Acid", also known as cefditoren free acid "Cefteram Free Acid") to play an antibacterial effect. Cefditoren axetil is used for acute bronchitis, pneumonia, gonorrhea urethritis; pharyngitis; tonsils, etc. caused by sensitive bacteria. It has the characteristics of broad spectrum, high efficiency, enzyme resistance and low toxicity, and is an anti-infection oral drug widely used in clinical practice. However, the medicine still has the following disadvantages: (1) currently marketed...

Claims

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Application Information

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IPC IPC(8): A61K31/545
Inventor 黄文豪
Owner 黄文豪
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