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Liposomal formulations of amidine substituted beta-lactam compounds for use in the treatment of bacterial infections

A technology of liposomes and compounds, applied in the field of liposome β-lactam preparations

Inactive Publication Date: 2019-07-05
AICURIS ANTI INFECTIVE CURES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, neither strong acidic pH nor acetonitrile is required for drug product formulation

Method used

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  • Liposomal formulations of amidine substituted beta-lactam compounds for use in the treatment of bacterial infections
  • Liposomal formulations of amidine substituted beta-lactam compounds for use in the treatment of bacterial infections
  • Liposomal formulations of amidine substituted beta-lactam compounds for use in the treatment of bacterial infections

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Experimental program
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Embodiment Construction

[0084] 1. Preparation of Liposomes

[0085]All liposomal formulations were prepared by the thin film hydration method. Briefly, an accurately weighed amount of 55 / 45 (mol) DSPC / Chol was dissolved in a round bottom flask with chloroform, and a film was produced at 40°C under reduced pressure. After complete removal of the organic solvent, the membrane was hydrated with one of the following buffers: 300 mM ammonium sulfate; 150 mM sodium acetate; 120 mM calcium acetate, or 0.9% NaCl (used as a negative control) and HEPES / saline buffer at pH 7.4 (HBS) (used as a negative control) at a final concentration of 60 mM lipid.

[0086] After one hour of hydration at 65°C (the membrane was completely removed from the flask wall), a Lipexthermobarrel extruder equipped with polycarbonate membranes of various pore sizes (400, 200 and 100 nm) was used The liposomes were extruded so as to reach a final size of 130-150 nm with PdI<0.100. In this size range, maximum theoretical encapsulation...

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Abstract

The present invention provides new and effective liposomal fomiulations for the administration of beta-lactams.

Description

technical field [0001] The present invention relates to liposomal β-lactam formulations, encapsulation of such β-lactams within liposomes for drug delivery purposes and the use of such formulations in the treatment and prophylaxis of bacterial infections. Background technique [0002] The present invention relates to novel β-lactam formulations, their preparation and use. In particular, the present invention relates to novel β-lactam compounds, which are amidine-substituted monocyclic compounds useful as antimicrobial agents, and their encapsulation in liposomes as drug delivery systems. β-lactam derivatives. [0003] Public health experts and officials consider the emergence and spread of antibiotic resistant bacteria to be one of the major public health problems of the 21st century. While not a new phenomenon in itself, the spread of antibiotic-resistant bacteria has reached unprecedented levels. Although the majority of drug-resistant isolates continue to emerge in the...

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Application Information

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IPC IPC(8): A61K31/427A61K9/127A61P31/04
CPCA61K9/127A61K31/427A61P31/04Y02A50/30
Inventor 约戈什瓦尔·巴克哈夫
Owner AICURIS ANTI INFECTIVE CURES
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