Slow release antibiotics preparation of bioactive substance

A technology of antibiotics and preparations, which is applied in the field of antibiotics preparations, and can solve the problems of release reaction impact, insignificance, etc.

Inactive Publication Date: 2009-05-13
HERAEUS KULZER GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the preparation method of this antimicrobial storage system has a non-trivial effect on the release response
Systems containing salts of poorly soluble antibiotics have the disadvantage that a specific form of salt must be synthesized for each antibiotic used prior to the manufacture of long-acting formulations

Method used

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  • Slow release antibiotics preparation of bioactive substance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Prepare a kind of by 51mg gentamicin sulfate (700U / mg, Fluka company produces), 51mg sodium lauryl sulfate (Aldrich company produces), 280mg poly L-lactide (molecular weight~10,000gmol -1 ) and 1118mg of dibasic calcium phosphate (produced by Fluka). Each 200 mg of this mixture was pressed into a disc-shaped molding having a diameter of 13 mm with a press within 2 minutes under a pressure of 5 tons.

[0055] Wherein, the molar ratio of the amphoteric component and the antibiotic is >SDS:Genta=177:0.72=2.458333333:1

Embodiment 2

[0057] Prepare a kind of by 51mg gentamicin sulfate (700U / mg, Fluka company produces), 51mg sodium lauryl sulfate (Aldrich company produces), 280mg poly L-lactide (molecular weight~10,000gmol -1 ) and 1118mg of dibasic calcium phosphate dihydrate (produced by Fluka). Each 200 mg of this mixture was pressed into a disc-shaped molding having a diameter of 13 mm with a press within 2 minutes under a pressure of 5 tons.

[0058] Wherein, the molar ratio of the amphoteric component and the antibiotic is >SDS:Genta=177:0.72=2.458333333:1

Embodiment 3

[0060] Prepare a kind of by 51mg gentamicin sulfate (700U / mg, Fluka company produces), 51mg sodium lauryl sulfate (Aldrich company produces), 280mg poly L-lactide (molecular weight~10,000gmol -1 ) and 1118mg of calcium sulfate dihydrate (Fluka) mixture. Each 200 mg of this mixture was pressed into a disc-shaped molding having a diameter of 13 mm with a press within 2 minutes under a pressure of 5 tons.

[0061] Wherein, the molar ratio of the amphoteric component and the antibiotic is >SDS:Genta=177:0.72=2.458333333:1

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Abstract

An amphiphilic organic sulfate, sulfamate, sulfonate, disulfate, disulfonate or trisulfonate is included in an aminoglycoside, lincosamide, 4-quinolone or tetracycline antibiotic preparation to retard the release of the antibiotic from the preparation. An antibiotic preparation comprises a mixture of an amphiphilic component consisting of one or more alkyl, aryl, alkylaryl, cycloalkyl or alkylcycloalkyl sulfates, sulfamates or sulfonates, fatty acid-2-sulfonates, alkyl or cycloalkyl disulfates, alkyl, cycloalkyl, aryl or alkylaryl disulfonates or aryl or alkylaryl trisulfonates and one or more aminoglycoside, lincosamide, 4-quinolone or tetracycline antibiotics.

Description

technical field [0001] The present invention relates to an antibiotic preparation and multiple uses thereof. Background technique [0002] In human and veterinary medicine, the treatment of local microbial infections of soft and hard tissues requires high concentrations of local antibiotics in the area of ​​infected tissue. It has long been known that the continuous use of antibiotics has its own set of problems. When continuous medication is used, it is often necessary to use a very high dose of antibiotics in order to achieve an effective antibacterial concentration of antibiotics in the infected tissue. Thus, especially in the case of aminoglycoside antibiotics and tetracycline antibiotics, their kidney and ear toxicity can seriously damage the body. Therefore, it is easy for people to think of locally adopting the delivery method of antibiotics, or converting them into suitable long-acting dosage forms. [0003] Antibiotic slow-release depot systems for the treatment ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/726A61K31/7048A61K31/7036A61K31/66A61K31/63A61K31/545A61K31/4704A61K31/43A61K31/65A61K9/00A61P31/04A61K9/10A61K9/14A61K9/20A61K9/22A61K9/70A61K31/00A61K31/70A61K45/06A61K45/08A61K47/02A61K47/14A61K47/16A61K47/20A61K47/24A61L27/54A61L31/16
CPCA61L2300/802A61L2300/406A61K9/2013A61K31/00A61L2300/602A61K9/0024A61K31/7036A61L27/54A61P31/00A61P31/04
Inventor S·福哥特M·斯纳波劳KL-D·科恩
Owner HERAEUS KULZER GMBH
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