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Tetracycline complexes with sustained activity

A technology of tetracyclines and complexes, applied in the field of treatment and/or prevention of bacterial infections, can solve the problems of difficult and unreliable handling and placing in periodontal pockets, and achieve easy formation and handling, delayed and sustained release, The effect of increased stability

Pending Publication Date: 2021-10-26
FRAUNHOFER GESELLSCHAFT ZUR FOERDERUNG DER ANGEWANDTEN FORSCHUNG EV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The consistency of the material (microspheres) requires special cartridges for application and makes handling and placement in periodontal pockets difficult and less reliable

Method used

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  • Tetracycline complexes with sustained activity
  • Tetracycline complexes with sustained activity
  • Tetracycline complexes with sustained activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Example 1: Formation of a 1:2 complex of minocycline (free base) and magnesium stearate

[0134] Minocycline (free base) was weighed together with magnesium stearate in a molar ratio of 1:2 in a round bottom flask. Specifically, minocycline (10 mg, M=457.48 g / mol, 218.8 μmol) was combined with magnesium stearate (25.848 mg, M=591.24 g / mol, 43.717 μmol). The two components were mixed briefly in a hand shaker. The mixture was suspended in undenatured ethanol (96% v / v, 2 mL) to obtain a pale yellow opaque suspension. Place the closed flask in a water bath with gentle vortexing. From about 50°C, complexes start to form and dissolve. At about 60-70°C, a clear orange solution formed which remained clear upon cooling to room temperature. Solvent was removed on a tempered shaker. figure 1 A vial with dried product is shown.

Embodiment 2

[0135] Example 2: Formation of a 1:1 complex of minocycline (free base) and magnesium stearate

[0136] The complex was prepared in a molar ratio of 1:1 in a similar manner as described in Example 1 by using appropriately adjusted amounts of minocycline (free base).

Embodiment 3

[0137] Example 3: Formation of a 1:2 complex of minocycline hydrochloride and magnesium stearate

[0138] A complex of minocycline hydrochloride and magnesium stearate in a molar ratio of 1:2 was prepared in a similar manner as described above in Example 1, using an appropriate amount of minocycline hydrochloride, The molar ratio of minocycline and magnesium stearate is 1:2.

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Abstract

The present invention generally relates to controlled release of tetracycline antibiotics. Specifically, The invention relates to a complex comprising a tetracycline compound (TC) or a pharmaceutically acceptable salt, hydrate or solvate thereof and a divalent metal carboxylate; a pharmaceutical preparation comprising the complex, methods for manufacturing the complex and the pharmaceutical preparation, and a complex or a pharmaceutical preparation for use in a method for treatment of the human or animal body, in particular for therapy and / or prophylaxis of a bacterial infection; and / or wherein antibiotic activity is maintained over a prolonged period of time; and / or for the therapy and / or prophylaxis of an acute, chronic or recurrent periodontal disease.

Description

[0001] field of invention [0002] The present invention generally relates to the controlled release of tetracycline antibiotics. Specifically, it relates to a complex comprising a tetracycline compound (TC) or a pharmaceutically acceptable salt, hydrate or solvate thereof and a divalent metal carboxylate; a pharmaceutical preparation comprising said complex, used for the preparation of said complexes and said pharmaceutical formulations, and methods for the treatment of the human or animal body, in particular for the treatment and / or prevention of bacterial infections; and / or wherein the antibiotic activity is maintained for a prolonged period of time; and / or with Complexes or pharmaceutical preparations for methods of treatment and / or prevention of acute, chronic or recurrent periodontal diseases. Background technique [0003] Tetracyclines are a class of antibiotics that inhibit protein synthesis by preventing the attachment of aminoacyl-tRNAs to ribosomal receptor (A) sit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/14A61K31/65C07C237/26A61P31/04
CPCA61K31/65A61P31/04C07C2603/46C07C237/24A61K9/0063A61K47/34Y02A50/30C07C237/26A61K9/0014A61P1/02C07C231/22C07C2603/40A61K47/593A61K47/69
Inventor 安德烈亚斯·基佐米尔科·布赫霍尔兹桑德拉·萨雷米尔卡斯滕·梅德马丁·基希贝格西格伦·艾克
Owner FRAUNHOFER GESELLSCHAFT ZUR FOERDERUNG DER ANGEWANDTEN FORSCHUNG EV