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Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same

A technology for parenteral administration and antibacterial drugs, applied in the field of antibacterial drug preparations and its manufacturing, to achieve the effect of no waste price

Inactive Publication Date: 2013-05-08
维克托历沃维奇·利莫诺夫
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The present invention solves the problem of producing an antibacterial pharmaceutical composition for injection based on the use of β-lactam and silica nanoparticle antibiotics which are more effective for the treatment of infectious and inflammatory diseases High therapeutic efficacy (compared to standard beta-lactams considered as the basis of the present invention)

Method used

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  • Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same
  • Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same
  • Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same

Examples

Experimental program
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Effect test

example 1

[0036] Example 1. Manufacture of solid compositions: β-lactam antibiotics – finely dispersed nanostructured silica.

[0037] Processing of β-lactam antibiotics and ВНSiO in weight ratios of 10:1, 20:1, 30:1 and 40:1 in a circular rotary mill 2 mixture for 1, 2 and 4 hours. The data on the particle size composition of the aqueous suspension and the HPLC analysis of the antibiotic content (in % of starting material) are listed in Table 2.

[0038] Table 2

[0039] Particle size composition and antibiotic content of aqueous suspensions in different compositional variants

[0040]

[0041] * - Finely dispersed nanostructured silica** - mechanically activated

[0042] As can be seen from Table 2, the selected composition manufacturing conditions make the finely dispersed ВНSiO 2 The fraction of fractions (particle size less than 5 microns) is increased to a certain value (not less than 25%) and chemical degradation of antibiotics is avoided.

example 2

[0043] Example 2. Determination of therapeutic efficacy of antibacterial preparations and pharmaceutical compositions.

[0044] Therefore, beta-lactam antibiotics (cefazolin, cefuroxime, cefotaxime, ceftriaxone, cefoperazone, cefoperazone / sulbactam, ceftazidime, cefepime, cefoxitin, aztreonam) have been studied. , meropenem, carbenicillin) and its mechanization for 2 hours by weight ratio of 30:1 antibiotic / ВНSiO 2 Compositions of mixtures (cefazolin / ВНSiO 2 , Cefuroxime / ВНSiO 2 , Cefotaxime / ВНSiO 2 , Ceftriaxone / ВНSiO 2 , Cefoperazone / ВНSiO 2 , Cefoperazone / Sulbactam / ВНSiO 2 , Ceftazidime / ВНSiO 2 , Cefepime / ВНSiO 2 , Cefoxitin / ВНSiO 2 , Aztreonam / ВНSiO 2 , Meropenem / ВНSiO 2 , Carbenicillin / ВНSiO 2 ).

[0045] For the determination of β-lactams and their inclusion ВНSiO 2 The therapeutic efficacy of the pharmaceutical composition, according to [22, 23], using an experimental sepsis model and for the obtained data (χ 2 ) statistical processing metho...

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Abstract

The invention relates to pharmacology, medicine, veterinary medicine and to the pharmaceutical industry, in particular to a process for preparing original composite antimicrobial preparations for parenteral administration which have increased therapeutic effectiveness in the treatment of severe forms of infectious and inflammatory diseases. The proposed pharmaceutical compositions comprise, as active ingredient, beta-lactam antibiotics and highly disperse nanostructured silicon dioxide in ratios of from 10:1 to 75:1 by weight, respectively.; The silicon dioxide particles present in the composition are the means of supplying the molecules of the antibiotics to the phagocytes, which makes it possible to increase, in a targeted manner, the concentration of the antimicrobial preparations in the areas of inflammation and to substantially neutralize the phenomenon of antibiotic resistance of microorganisms. The claimed process for preparing a pharmaceutical composition consists in mixing a beta-lactam antibiotic substance with highly disperse nanostructured silicon dioxide and is characterized in that the mixture of the above-mentioned substances in ratios of from 10:1 to 75:1 by weight, respectively, is subjected to mechanical processing by means of impact abrasion until the proportion by weight of the finely disperse fraction (5 [mu]m) is increased to at least 25%. The resultant mixture is used for preparing injection solutions.

Description

technical field [0001] The invention belongs to antibacterial drug preparation and its manufacturing technology. It is used in medicine and veterinary medicine to treat infectious and inflammatory diseases, and in the pharmaceutical industry to manufacture medicinal products. Background technique [0002] Most current successful therapies for infectious and inflammatory diseases are based on the use of different anti-infective agents, including β-lactam antibiotics. [0003] β-lactams are agents having a β-lactam ring as a common segment of chemical structure (natural and semisynthetic penicillins, cephalosporins, cephamycins, carbapenems and monobactams), the β-lactam ring determines the antibacterial activity and a series of common properties of this group of pharmaceutical preparations [1]. [0004] All β-lactams have a broad antimicrobial spectrum and a high level of antimicrobial activity, but many of them are due to the production of a specific enzyme that hydrolyzes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/545A61K9/51A61K47/04A61P31/04
CPCA61K9/0019A61K47/02A61K31/545A61K9/141A61P31/04
Inventor 维克托历沃维奇·利莫诺夫康斯坦丁瓦连京诺维奇·盖杜尔亚历山大瓦莱雷维奇·杜什金
Owner 维克托历沃维奇·利莫诺夫
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