EA021874B1 - Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same - Google Patents
Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same Download PDFInfo
- Publication number
- EA021874B1 EA021874B1 EA201001449A EA201001449A EA021874B1 EA 021874 B1 EA021874 B1 EA 021874B1 EA 201001449 A EA201001449 A EA 201001449A EA 201001449 A EA201001449 A EA 201001449A EA 021874 B1 EA021874 B1 EA 021874B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- silicon dioxide
- beta
- weight
- pharmaceutical composition
- preparing
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 7
- 230000000845 anti-microbial effect Effects 0.000 title claims abstract description 6
- 238000004519 manufacturing process Methods 0.000 title abstract description 4
- 238000007911 parenteral administration Methods 0.000 title abstract 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 24
- 239000000377 silicon dioxide Substances 0.000 claims abstract description 12
- 235000012239 silicon dioxide Nutrition 0.000 claims abstract description 10
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims abstract description 9
- 239000002132 β-lactam antibiotic Substances 0.000 claims abstract description 9
- 229940124586 β-lactam antibiotics Drugs 0.000 claims abstract description 9
- 239000000203 mixture Substances 0.000 claims abstract description 8
- 239000002245 particle Substances 0.000 claims abstract description 5
- 239000000126 substance Substances 0.000 claims abstract description 5
- 238000005299 abrasion Methods 0.000 claims abstract description 3
- 238000002347 injection Methods 0.000 claims abstract description 3
- 239000007924 injection Substances 0.000 claims abstract description 3
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 3
- 238000000034 method Methods 0.000 claims description 2
- 239000000843 powder Substances 0.000 claims 3
- 239000002086 nanomaterial Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 4
- 238000002360 preparation method Methods 0.000 abstract description 4
- 230000003115 biocidal effect Effects 0.000 abstract description 3
- 208000035473 Communicable disease Diseases 0.000 abstract description 2
- 206010061218 Inflammation Diseases 0.000 abstract description 2
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 239000002131 composite material Substances 0.000 abstract description 2
- 230000002458 infectious effect Effects 0.000 abstract description 2
- 208000027866 inflammatory disease Diseases 0.000 abstract description 2
- 230000004054 inflammatory process Effects 0.000 abstract description 2
- 244000005700 microbiome Species 0.000 abstract description 2
- 210000001539 phagocyte Anatomy 0.000 abstract description 2
- 239000000243 solution Substances 0.000 abstract description 2
- 239000003242 anti bacterial agent Substances 0.000 abstract 1
- 229940088710 antibiotic agent Drugs 0.000 abstract 1
- 239000004599 antimicrobial Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 an active ingredient, beta-lactam antibiotics and fine 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 μm) is increased to at least 25 %. The obtained mixture is used for preparing injection solutions.
Description
(57) Изобретение относится к фармакологии, медицине, ветеринарии и к фармацевтической промышленности, в частности к способу получения оригинальных композитных антимикробных препаратов для парентерального применения, которые обладают повышенной терапевтической эффективностью при лечении тяжёлых форм инфекционно-воспалительных заболеваний. Предложенные фармацевтические композиции содержат в качестве действующего вещества бета-лактамные антибиотики и высокодисперсный наноструктурированный диоксид кремния в соотношениях от 10:1 до 75:1 по весу соответственно. Присутствующие в композиции частицы диоксида кремния являются средствами доставки молекул антибиотиков в фагоциты, что позволяет целенаправленно повышать концентрацию антимикробных препаратов в зонах воспаления и существенно нивелировать феномен антибиотикорезистентности микроорганизмов. Заявляемый способ получения фармацевтической композиции заключается в смешивании субстанции беталактамного антибиотика с высокодисперсным наноструктурированным диоксидом кремния, отличающийся тем, что смесь вышеуказанных веществ в соотношениях от 10:1 до 75:1 по весу соответственно подвергают механической обработке путем ударно-истирающих воздействий до увеличения весовой доли мелкодисперсной фракции (< 5 мкм) не менее чем до 25%. Полученную смесь используют для приготовления инъекционных растворов.(57) The invention relates to pharmacology, medicine, veterinary medicine and the pharmaceutical industry, in particular to a method for producing original composite antimicrobial preparations for parenteral use, which have increased therapeutic efficacy in the treatment of severe forms of infectious and inflammatory diseases. The proposed pharmaceutical compositions contain beta-lactam antibiotics and highly dispersed nanostructured silicon dioxide as active ingredient in ratios of 10: 1 to 75: 1 by weight, respectively. The particles of silicon dioxide present in the composition are means of delivering antibiotic molecules to phagocytes, which makes it possible to purposefully increase the concentration of antimicrobial agents in areas of inflammation and significantly level the phenomenon of antibiotic resistance of microorganisms. The inventive method of obtaining a pharmaceutical composition consists in mixing the substance of a betalactam antibiotic with highly dispersed nanostructured silicon dioxide, characterized in that the mixture of the above substances in ratios from 10: 1 to 75: 1 by weight, respectively, is subjected to mechanical treatment by impact-abrasion to increase the weight fraction of finely divided fractions (<5 microns) not less than 25%. The resulting mixture is used for the preparation of injection solutions.
021874 В1021874 B1
Claims (2)
Priority Applications (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EA201001449A EA021874B1 (en) | 2010-09-13 | 2010-09-13 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
| JP2013528146A JP2013537190A (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition having antibacterial action for parenteral administration and method for producing the same |
| AU2011302724A AU2011302724C1 (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
| PCT/RU2011/000320 WO2012036585A1 (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
| BR112012023964A BR112012023964A2 (en) | 2010-09-13 | 2011-05-11 | antimicrobial pharmaceutical composition for parenteral administration and production process |
| CN2011800044095A CN103096896A (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
| MX2012010535A MX2012010535A (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same. |
| NZ598831A NZ598831A (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
| CA2785228A CA2785228A1 (en) | 2010-09-13 | 2011-05-11 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EA201001449A EA021874B1 (en) | 2010-09-13 | 2010-09-13 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201001449A1 EA201001449A1 (en) | 2012-02-28 |
| EA021874B1 true EA021874B1 (en) | 2015-09-30 |
Family
ID=45908207
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201001449A EA021874B1 (en) | 2010-09-13 | 2010-09-13 | Pharmaceutical composition with antimicrobial activity for parenteral administration and process for preparing same |
Country Status (9)
| Country | Link |
|---|---|
| JP (1) | JP2013537190A (en) |
| CN (1) | CN103096896A (en) |
| AU (1) | AU2011302724C1 (en) |
| BR (1) | BR112012023964A2 (en) |
| CA (1) | CA2785228A1 (en) |
| EA (1) | EA021874B1 (en) |
| MX (1) | MX2012010535A (en) |
| NZ (1) | NZ598831A (en) |
| WO (1) | WO2012036585A1 (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP9901877A1 (en) * | 1996-02-29 | 1999-12-28 | Fujisawa Pharmaceutical Co., Ltd. | Tablets containing béta-lactam antibiotic and process for producing the same |
| WO2008062429A2 (en) * | 2006-08-11 | 2008-05-29 | Panacea Biotec Limited | Particles for delivery of active ingredients, process of making and compositions thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2377985C2 (en) | 2006-12-25 | 2010-01-10 | Сергей Михайлович Юдин | Preparation for treating infectious diseases caused by multiresistant bacteria |
-
2010
- 2010-09-13 EA EA201001449A patent/EA021874B1/en not_active IP Right Cessation
-
2011
- 2011-05-11 WO PCT/RU2011/000320 patent/WO2012036585A1/en active Application Filing
- 2011-05-11 CN CN2011800044095A patent/CN103096896A/en active Pending
- 2011-05-11 AU AU2011302724A patent/AU2011302724C1/en not_active Ceased
- 2011-05-11 JP JP2013528146A patent/JP2013537190A/en not_active Withdrawn
- 2011-05-11 NZ NZ598831A patent/NZ598831A/en not_active IP Right Cessation
- 2011-05-11 BR BR112012023964A patent/BR112012023964A2/en not_active IP Right Cessation
- 2011-05-11 MX MX2012010535A patent/MX2012010535A/en not_active Application Discontinuation
- 2011-05-11 CA CA2785228A patent/CA2785228A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP9901877A1 (en) * | 1996-02-29 | 1999-12-28 | Fujisawa Pharmaceutical Co., Ltd. | Tablets containing béta-lactam antibiotic and process for producing the same |
| WO2008062429A2 (en) * | 2006-08-11 | 2008-05-29 | Panacea Biotec Limited | Particles for delivery of active ingredients, process of making and compositions thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2011302724B2 (en) | 2012-06-28 |
| BR112012023964A2 (en) | 2016-08-02 |
| JP2013537190A (en) | 2013-09-30 |
| CN103096896A (en) | 2013-05-08 |
| NZ598831A (en) | 2013-11-29 |
| EA201001449A1 (en) | 2012-02-28 |
| WO2012036585A1 (en) | 2012-03-22 |
| AU2011302724C1 (en) | 2012-11-29 |
| AU2011302724A1 (en) | 2012-05-03 |
| CA2785228A1 (en) | 2012-03-22 |
| MX2012010535A (en) | 2012-11-16 |
| WO2012036585A8 (en) | 2012-10-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |