WO1994010977A1 - Compose pharmaceutique anti-microbien et induisant des interferons - Google Patents
Compose pharmaceutique anti-microbien et induisant des interferons Download PDFInfo
- Publication number
- WO1994010977A1 WO1994010977A1 PCT/RU1993/000209 RU9300209W WO9410977A1 WO 1994010977 A1 WO1994010977 A1 WO 1994010977A1 RU 9300209 W RU9300209 W RU 9300209W WO 9410977 A1 WO9410977 A1 WO 9410977A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- πaρa
- drug
- hours
- injections
- chτο
- Prior art date
Links
- 230000000845 anti-microbial effect Effects 0.000 title abstract description 5
- 239000004599 antimicrobial Substances 0.000 title abstract description 3
- 150000001875 compounds Chemical class 0.000 title abstract description 3
- 230000001939 inductive effect Effects 0.000 title abstract description 3
- 102000014150 Interferons Human genes 0.000 title abstract 2
- 108010050904 Interferons Proteins 0.000 title abstract 2
- 230000001064 anti-interferon Effects 0.000 title abstract 2
- 229940079322 interferon Drugs 0.000 title abstract 2
- 239000013543 active substance Substances 0.000 claims abstract description 14
- 238000002347 injection Methods 0.000 claims description 10
- 239000007924 injection Substances 0.000 claims description 10
- 229940126601 medicinal product Drugs 0.000 claims description 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 7
- 239000008024 pharmaceutical diluent Substances 0.000 claims description 4
- 239000011149 active material Substances 0.000 claims description 2
- 238000012986 modification Methods 0.000 abstract description 9
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 abstract description 3
- 229940124530 sulfonamide Drugs 0.000 abstract description 3
- 239000003085 diluting agent Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 33
- 239000003814 drug Substances 0.000 description 33
- 238000002360 preparation method Methods 0.000 description 21
- 230000000694 effects Effects 0.000 description 12
- 238000000034 method Methods 0.000 description 10
- 238000012360 testing method Methods 0.000 description 10
- 238000004458 analytical method Methods 0.000 description 9
- 241000699670 Mus sp. Species 0.000 description 8
- 208000025865 Ulcer Diseases 0.000 description 8
- 210000003205 muscle Anatomy 0.000 description 8
- 231100000397 ulcer Toxicity 0.000 description 8
- 238000002474 experimental method Methods 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- 239000000203 mixture Substances 0.000 description 6
- 239000008215 water for injection Substances 0.000 description 6
- 241000699666 Mus <mouse, genus> Species 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 5
- 239000000725 suspension Substances 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 238000005303 weighing Methods 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 4
- 241000700605 Viruses Species 0.000 description 4
- 208000027418 Wounds and injury Diseases 0.000 description 4
- 239000002674 ointment Substances 0.000 description 4
- 238000011160 research Methods 0.000 description 4
- 206010052428 Wound Diseases 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 230000035876 healing Effects 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 231100000331 toxic Toxicity 0.000 description 3
- 230000002588 toxic effect Effects 0.000 description 3
- 210000003462 vein Anatomy 0.000 description 3
- WZUVPPKBWHMQCE-UHFFFAOYSA-N Haematoxylin Chemical compound C12=CC(O)=C(O)C=C2CC2(O)C1C1=CC=C(O)C(O)=C1OC2 WZUVPPKBWHMQCE-UHFFFAOYSA-N 0.000 description 2
- 206010062065 Perforated ulcer Diseases 0.000 description 2
- 240000007651 Rubus glaucus Species 0.000 description 2
- 235000011034 Rubus glaucus Nutrition 0.000 description 2
- 235000009122 Rubus idaeus Nutrition 0.000 description 2
- 230000005856 abnormality Effects 0.000 description 2
- 206010003246 arthritis Diseases 0.000 description 2
- 230000006378 damage Effects 0.000 description 2
- 230000008021 deposition Effects 0.000 description 2
- 210000000883 ear external Anatomy 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 230000002452 interceptive effect Effects 0.000 description 2
- 238000007918 intramuscular administration Methods 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 210000004400 mucous membrane Anatomy 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
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- 229940127557 pharmaceutical product Drugs 0.000 description 2
- 229920003023 plastic Polymers 0.000 description 2
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- 238000012545 processing Methods 0.000 description 2
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- 241000792859 Enema Species 0.000 description 1
- 206010021703 Indifference Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical class [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 208000000558 Varicose Ulcer Diseases 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
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- 230000002411 adverse Effects 0.000 description 1
- 230000001166 anti-perspirative effect Effects 0.000 description 1
- 239000003213 antiperspirant Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000003385 bacteriostatic effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 235000013339 cereals Nutrition 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 235000019693 cherries Nutrition 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
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- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 229940126534 drug product Drugs 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 206010014599 encephalitis Diseases 0.000 description 1
- 206010014801 endophthalmitis Diseases 0.000 description 1
- 239000007920 enema Substances 0.000 description 1
- 229940095399 enema Drugs 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 239000010685 fatty oil Substances 0.000 description 1
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- 230000037406 food intake Effects 0.000 description 1
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- 230000009931 harmful effect Effects 0.000 description 1
- 231100000086 high toxicity Toxicity 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 235000013372 meat Nutrition 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 230000003387 muscular Effects 0.000 description 1
- 210000004165 myocardium Anatomy 0.000 description 1
- 230000001338 necrotic effect Effects 0.000 description 1
- 230000009972 noncorrosive effect Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 102000040430 polynucleotide Human genes 0.000 description 1
- 108091033319 polynucleotide Proteins 0.000 description 1
- 239000002157 polynucleotide Substances 0.000 description 1
- 229920006316 polyvinylpyrrolidine Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 244000144977 poultry Species 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
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- 238000013207 serial dilution Methods 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000009331 sowing Methods 0.000 description 1
- 210000000952 spleen Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-L sulfite Chemical compound [O-]S([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-L 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000007306 turnover Effects 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
-
- 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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
Definitions
- the claimed preparation for injections is predominantly water for injections.
- the claimed medication can be used in the form of rectal candles, and this is useful, so that the content of the active substance is 12.5-17.5%.
- any pharmaceutical base for candles can be used as a base.
- the claimed medicinal product may be used for external use only, in combination with - 4 -
- the claimed step-5 takes advantage of a high-potency-modifying activity (a pharmaceutical-aminobenzulfanilamide).
- the claimed medical device does not have any annoying effect on its own.
- the claimed preparation induces an infection in the serum of mice after 5 hours after administration (previous infection) with an activity of 40-80 units / ml, which takes up to 40-80 units / ml. ⁇ 72 hours ago, there was a decrease in rates in the world.
- the inventive method is the following composition in wt /%: ⁇ -modification of para-aminobenzene sulfanes-amide - 2, 0; ⁇ polivinyl ⁇ i ⁇ - lidon - 3, 0; water for injection - other 12.61 + 3.1 13, 46 + 4, 14, 59 + 3, 9, 04 + 0, 81 , 84 + 0,
- ⁇ ⁇ same v ⁇ emya is ⁇ lz ⁇ vanie zayavlyaem ⁇ g ⁇ ⁇ e ⁇ a ⁇ a in eg ⁇ ⁇ e ⁇ a ⁇ ev ⁇ iches ⁇ y d ⁇ ze, blag ⁇ - da ⁇ ya vys ⁇ y bi ⁇ d ⁇ s ⁇ u ⁇ n ⁇ s ⁇ i, m ⁇ zhe ⁇ usiliva ⁇ ba ⁇ e ⁇ i ⁇ s- ⁇ a ⁇ iches ⁇ e deys ⁇ vie ⁇ e ⁇ a ⁇ a ⁇ a and ⁇ em thus eg ⁇ ⁇ e ⁇ a ⁇ ev- 0 ⁇ iches ⁇ uyu e ⁇ e ⁇ ivn ⁇ s ⁇ .
- the inventive product is found in the quality of an antimicrobial and internally induced drug.
- the inventive preparation may be used in any pharmaceutical preparation.
- the content of the active substance is 1.5–2.5 wt%.
- the above studies on the selection of the optimal concentration of the active substance were shown in the declared range - eleven -
- the claimed ⁇ e ⁇ a ⁇ a ⁇ for ine ⁇ tsy m ⁇ zhe ⁇ d ⁇ lni ⁇ el- n ⁇ s ⁇ de ⁇ zha ⁇ ⁇ livinil ⁇ i ⁇ lid ⁇ n niz ⁇ m ⁇ le ⁇ ulya ⁇ ny ⁇ i s ⁇ n ⁇ shenii ⁇ m ⁇ nen ⁇ v follows, in wt%: ⁇ is ⁇ alliches ⁇ aya ⁇ -m ⁇ di ⁇ i ⁇ atsiya ⁇ a ⁇ a amin ⁇ benz ⁇ lsul ⁇ anilamida-1, 5-2, 5 ⁇ livinil ⁇ i ⁇ lid ⁇ n niz ⁇ m ⁇ le ⁇ ulya ⁇ ny 2, 0-4, 0 ⁇ a ⁇ matsev ⁇ iches ⁇ y ⁇ azbavi ⁇ el ⁇ s ⁇ aln ⁇ e ⁇ vedenie ⁇ livinil ⁇ i ⁇ lid ⁇ na in s ⁇ s ⁇ av
- the device is based on its indifference and ensuring the necessary sedimentary stability and absorbability
- the inventive product can be used in the form of rectal candles, and, thus, the preferred content of the active material is 12.5–17.5 wt%.
- the analysis of the above studies showed that the use of candles containing 12.5-17.5% of the active substance is secured by a 2.0 percent (2.0 percent).
- any pharmaceutically acceptable base fat base, oil and other may be used. - 12 -
- the inventive product can be used for other applications, and, as a result, it is a component that is in the form of a medium-mediated , 4-tetrahydroimidine and their mass ratio of 1: 1.
- the claimed ⁇ e ⁇ a ⁇ a ⁇ in an ointment ⁇ isy ⁇ i for HA ⁇ uzhn ⁇ g ⁇ ⁇ imeneniya was is ⁇ y ⁇ an in ⁇ liniches ⁇ i ⁇ usl ⁇ viya ⁇ in naib ⁇ lee ⁇ yazhely ⁇ sluchaya ⁇ ⁇ udn ⁇ zazhivlyaemy ⁇ gn ⁇ yny ⁇ ⁇ an ⁇ azlichny ⁇ n ⁇ z ⁇ l ⁇ giches ⁇ i ⁇ ⁇ m ( ⁇ iches ⁇ i ⁇ ulcers ven ⁇ zn ⁇ g ⁇ ⁇ is ⁇ zhdeniya maly ⁇ d ⁇ 5 cm 2 and b ⁇ lshi ⁇ than 5 cm 2 and ⁇ az- me ⁇ v ⁇ sle ⁇ e ⁇ atsi ⁇ nny ⁇ gn ⁇ yny ⁇ ⁇ an).
- Urological form of treatment Duration of treatment (days) and application of the known known ointment preparation
- the manufacturing process of the product is carried out under aseptic conditions.
- the resulting drug product for injections provides a special suspension with an optical density of 2, 3, after 5 minutes of failure, the value of an optical pressure of 2 is 2, 2
- the Gynthological Control did not detect any changes in the domestic organizations. For example, 2.
- the manufacturing process of the claimed product is carried out under aseptic conditions.
- the Gynthological Control did not detect any changes in the domestic organizations.
- mice were administered the claimed preparation in a dose of 50 mcg / 0.2 ml (1st group) and 5 mice in a dose of 150 mcg / 0, 2 ml (2nd group) were given an internal dose. Abandonment of arthritis after 5, 24 and 72 hours after the introduction of the drug. Connecting an appliance to the computer by removing the pressure from the circuit breaker is connected to the microphone.
- mice The first group of mice was already 5 hours later at an average level of 40-80 units / ml, after 24 hours it was 160 units / ml and decreased to 20 units / ml for 72 hours.
- the 2nd group was lively, after 5 hours after the introduction of the preparation, the level of the mixture was 80 units / ml, after 24 hours, it went up to 72 ml / d for 20 ml and increased to 20 ml.
- Utilities are prepared by pouring. Each candle contains 0.3 g of the active substance and 1.7 g of the fat pharmaceutical product.
- Obstruction from the ear vein takes place after 0.5, 1, 2, 4, 6 hours.
- the concentration of the drug in the region is determined by the method of Prabssting-Gavrilov. Parallel tests are carried out with a pharmaceutical preparation for p-pa-aminobenzenesulfanilamide.
- the maximum concentration is already after 0.5-1 hours after introduction and maintenance of the therapeutic concentration (in the range of 2-20 ⁇ g / ml) for 6 hours.
- Ezinom has shown that there are no essential deviations from the normal normal structure.
- the inventive drug possesses antimicrobial and interfering activity and is used in medical practice.
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/256,494 US5510387A (en) | 1992-11-16 | 1993-08-31 | Antimicrobial interferon-inducing medicament |
EP93922097A EP0630644A4 (fr) | 1992-11-16 | 1993-08-31 | Compose pharmaceutique anti-microbien et induisant des interferons. |
AU51212/93A AU665127C (en) | 1992-11-16 | 1993-08-31 | Anti-microbial and interferon-inducing pharmaceutical compound |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
RU92671814 | 1992-11-16 | ||
RU92-006718/14 | 1992-11-16 | ||
RU93401514 | 1993-01-20 | ||
RU93-004015/14 | 1993-01-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1994010977A1 true WO1994010977A1 (fr) | 1994-05-26 |
Family
ID=26653733
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/RU1993/000209 WO1994010977A1 (fr) | 1992-11-16 | 1993-08-31 | Compose pharmaceutique anti-microbien et induisant des interferons |
Country Status (1)
Country | Link |
---|---|
WO (1) | WO1994010977A1 (fr) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0630644A4 (fr) * | 1992-11-16 | 1996-02-28 | Leonidov Nikolai B | Compose pharmaceutique anti-microbien et induisant des interferons. |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2321283A1 (fr) * | 1975-05-14 | 1977-03-18 | Parcor | Medicament nouveau a activite antibacterienne |
FR2361103A1 (fr) * | 1976-07-15 | 1978-03-10 | Basf Ag | Solutions de sulfonamide-trimethoprime |
US4401663A (en) * | 1981-06-30 | 1983-08-30 | The Procter & Gamble Company | Novel sulfonamide derivatives |
DE3800256A1 (de) * | 1987-01-08 | 1988-07-21 | Squibb & Sons Inc | Bioadhaesive suppositorienmassen |
US5151265A (en) * | 1987-11-03 | 1992-09-29 | Genentech, Inc. | Gamma interferon formulation |
-
1993
- 1993-08-31 WO PCT/RU1993/000209 patent/WO1994010977A1/fr not_active Application Discontinuation
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2321283A1 (fr) * | 1975-05-14 | 1977-03-18 | Parcor | Medicament nouveau a activite antibacterienne |
FR2361103A1 (fr) * | 1976-07-15 | 1978-03-10 | Basf Ag | Solutions de sulfonamide-trimethoprime |
US4401663A (en) * | 1981-06-30 | 1983-08-30 | The Procter & Gamble Company | Novel sulfonamide derivatives |
DE3800256A1 (de) * | 1987-01-08 | 1988-07-21 | Squibb & Sons Inc | Bioadhaesive suppositorienmassen |
US5151265A (en) * | 1987-11-03 | 1992-09-29 | Genentech, Inc. | Gamma interferon formulation |
Non-Patent Citations (1)
Title |
---|
See also references of EP0630644A4 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0630644A4 (fr) * | 1992-11-16 | 1996-02-28 | Leonidov Nikolai B | Compose pharmaceutique anti-microbien et induisant des interferons. |
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