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Pharmaceutical composition containing polymyxin and application thereof

A technology of polymyxin and composition, applied in the field of pharmaceutical compositions including polymyxin and its synergist, can solve the problem of difficulty in meeting demand, low success rate, long development cycle of new antibiotic drugs, etc. problem, to achieve good therapeutic effect, increase bioavailability, and reduce the effect of drug dosage

Pending Publication Date: 2020-12-18
ARTIVILA BIOPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Difficult to meet demand due to long development cycle and low success rate of new antibiotic drugs

Method used

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  • Pharmaceutical composition containing polymyxin and application thereof
  • Pharmaceutical composition containing polymyxin and application thereof
  • Pharmaceutical composition containing polymyxin and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The present invention provides a pharmaceutical composition containing polymyxin, said pharmaceutical composition comprising C507-0440 and polymyxin, wherein the chemical name of C507-0440 is N-[3-(methylthio)phenyl] -2,3-Dihydro-1H-cyclopenta[b]quinolin-9-amine, the PubChem SID number is 328424803, the specific structural formula is as follows:

[0043]

[0044] The pharmaceutical composition is the combination of C507-0440 or its pharmaceutically acceptable salt and polymyxin, or the mixed preparation of C507-0440 or its pharmaceutically acceptable salt and polymyxin.

[0045] Wherein, the polymyxin is polymyxin A, polymyxin B, polymyxin C, polymyxin D or polymyxin E.

[0046] Among them, polymyxin B is preferred in the pharmaceutical composition, and the concentration of polymyxin B is 0.023-64 ug / mL.

[0047] Wherein, the mass ratio of C507-0440 or its pharmaceutically acceptable salt to polymyxin B is 0.22-5300:1.

[0048] Wherein, in the pharmaceutically acce...

Embodiment 2

[0051] In this example, Klebsiella pneumoniae standard strain ATCC13883, Klebsiella pneumoniae clinical drug-resistant strain SZ021, Klebsiella pneumoniae clinical drug-resistant strain SZ206, Klebsiella pneumoniae clinical drug-resistant strain SZ301, Bao Acinetobacter mannequin ATCC19606 standard strain, Acinetobacter baumannii clinical drug-resistant strain SZ362, Pseudomonas aeruginosa model strain PA14 and Escherichia coli standard strain ATCC25922 were shaken at 37°C and 220 rpm until OD 600 =0.6~0.8, the combined effect of C507-0440 and polymyxin B was determined by checkerboard experiment, so as to further illustrate the present invention. The specific steps of the checkerboard experiment are as follows:

[0052] A. OD 600 = 0.6 ~ 0.8 of the bacterial culture density adjusted to OD 600 =0.001;

[0053] B. Polymyxin B was serially diluted 2 times along the abscissa, and C507-0440 was serially diluted 2 times along the ordinate;

[0054] C. Set up a blank group (a...

Embodiment 3

[0058] In this example, the mechanism by which C507-0440 enhances the activity of polymyxin B in Klebsiella pneumoniae is explored through proteome experiments, so as to further illustrate the present invention.

[0059] Control group: Klebsiella pneumoniae standard strain (ATCC13883) was inoculated into fresh LB broth medium supplemented with dimethyl sulfoxide at a volume ratio of 1:100, and cultured with shaking at 37°C and 220 rpm until OD 600 =0.6~0.8, 10000rpm, 3min centrifuge to collect the bacteria, then wash twice with pre-cooled PBS; resuspend the bacteria pellet, resuspend with four times the volume of lysis buffer, and sonicate on ice, at 15000rpm, 4℃ Centrifuge for 10 minutes, collect the supernatant, trypsinize, HPLC fractionation, and perform mass spectrometry analysis;

[0060] Single-drug group: inoculate the Klebsiella pneumoniae standard strain (ATCC13883) at a volume ratio of 1:100 into fresh LB broth medium supplemented with 3.175ug / mL C507-0440, at 37°C, ...

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Abstract

The invention discloses a pharmaceutical composition containing polymyxin and application thereof, and belongs to the field of biological medicine. The pharmaceutical composition comprises C507-0440 and polymyxin, the C507-0440 and the polymyxin are combined for use so that the activity of the polymyxin in gram-negative bacteria can be effectively improved, and the drug resistance of the polymyxinis inhibited; and meanwhile, the C507-0440 can significantly reduce the use dosage of the polymyxin, and is conductive to reducing side effects caused by drug use.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing polymyxin and its application, in particular to a pharmaceutical composition comprising polymyxin and its synergist, which is applied to resist Gram-negative bacteria and belongs to the field of biomedicine. Background technique [0002] According to the statistics of the World Health Organization, about 700,000 people die from bacterial infections every year in the world. In the treatment of various bacterial infections or diseases caused by pathogenic microorganisms, antibiotics are the main drugs used, but with the use of antibiotics, bacteria can strengthen their drug resistance through various ways, including secreting a variety of antibiotic hydrolytic enzymes (super Broad-spectrum β-lactamase, carbapenemase, etc.), gene mutations of drug targets, loss or translocation of membrane porins, active efflux pump system, etc., the above pathways have caused bacterial antibiotic resistance...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61P31/04A61K31/473
CPCA61K38/12A61K31/473A61P31/04A61K2300/00Y02A50/30
Inventor 黄维胡春霞章金勇邹全明崔瑞勤柳施一
Owner ARTIVILA BIOPHARMA
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