CN104415018A - Application of vitamin K3 in preparation of drug for treating bacterial infection - Google Patents
Application of vitamin K3 in preparation of drug for treating bacterial infection Download PDFInfo
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- CN104415018A CN104415018A CN201310364096.5A CN201310364096A CN104415018A CN 104415018 A CN104415018 A CN 104415018A CN 201310364096 A CN201310364096 A CN 201310364096A CN 104415018 A CN104415018 A CN 104415018A
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- 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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (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)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses an application of vitamin K3 in preparation of drug for treating bacterial and multiple resistant bacterial infection. By means of a CLSI standard method, research to anti-bacterial activity and anti-multiple-resistant-bacterial activity of the vitamin K3 is carried out with a result proving that: the vitamin K3 has significant inhibiting effect on growth of all test bacterial strains, which means that the vitamin K3 is significant in anti-bacterial activity and anti-multiple-resistant-bacterial activity and shows that the vitamin K3 is excellent in application and development prospect. The vitamin K3 can be used for preparing the drug for treating the bacterial and multiple resistant bacterial infection.
Description
Technical field
The present invention relates to vitamin K
3application in application in preparation treatment bacteriological infection medicine, especially preparation treatment multi-drug resistant bacteria infection medicine.
Background technology
In recent years, multi-drug resistant bacteria infects extend over the entire globe various places, and infection rate is in continuing ascendant trend, and in succession drug resistance is occurred to the clinical antibiotics of various structures type, its speed has exceeded the research and development speed of current antibiotics, and become super wide spectrum fastbacteria, the life and health of the mankind in serious threat.In view of many reasons such as the little and prospect of antibiotic research and development success rate are uncertain, setting foot in the large-scale pharmacy corporation in 15, the whole world in this field only has 5 still adhering to antibiotic research and development, cause the listing of antibiotics seriously delayed, the research and development of novel antibacterial medicine seem very urgent, the especially research and development of drug-resistance bacteria medicine.And methicillin-resistant staphylococcus aureus (MRSA) to be infection rate the highest, infect the most serious multi drug resistant bacterial pathogens, the research and development of anti-MRSA medicine are very urgent thus.
Vitamin K
3(2-MNQ) belongs to coagulant, is mainly used to treat the hemorrhage etc. caused by vitamin K deficiency.This medicine, by synthetic, because of its water solublity and absorption difference, is often prepared into soluble in water and absorbs good menadione sodium bisulfite, with the form administration of tablet or injection.In recent years, report is had to find vitamin K
3there is treatment senile dementia and antineoplastic assosting effect.But there are no about vitamin K
3antibacterial is reported, more has no the report that it has anti-multi-drug resistant bacteria.We find vitamin K by research
3there is significant antibacterial activity (as: anti-Staphylococcus aureus and anti-bacillus subtilis etc.), and to multi-drug resistant bacteria (as: MRSA), there is good antagonism.Due to vitamin K
3apply clinically for a long time as medicine, this shows vitamin K
3in the medicament research and development of antibacterial (especially anti-multi-drug resistant bacteria), there is good druggability and DEVELOPMENT PROSPECT, be easy to be developed to new antibacterial or anti-multi-drug resistant bacteria medicine, indicate its antibacterial and multi-drug resistant bacteria infect prevent and treat in there is good application prospect, can be used for preparing antibacterial or anti-multi-drug resistant bacteria medicine.
Summary of the invention
The object of this invention is to provide vitamin K
3application in preparation treatment bacteriological infection medicine, especially treats the application in multi-drug resistant bacteria infection medicine.
Vitamin K of the present invention
3for 2-MNQ (
1), or be menadione sodium bisulfite (
2), both molecular structures are shown below:
Wherein,
1for 2-MNQ;
2for menadione sodium bisulfite.Wherein,
2for
1with the addition compound product of sodium sulfite, i.e. menadione sodium bisulfite
3.
Vitamin K of the present invention
3can be bought by business and obtain, also can by synthesizing preparation with technology in accordance with known methods.
The present invention adopts the prescriptive procedure pair of CLSI standard
1with
2antibacterial activity evaluate, result shows:
1with
2all there is antibacterial and anti-multi-drug resistant bacteria activity significantly, display vitamin K
3in antibacterial and anti-multi-drug resistant bacteria medicament research and development, there is good prospect, can be used for the medicine preparing treatment antibacterial and multi-drug resistant bacteria infection.
The present invention adopts vitamin K
3during the pharmaceutical preparation that preparation treatment antibacterial and multi-drug resistant bacteria infect, can be made into tablet, injection, also can be medicinal other various dosage form acceptable.
Detailed description of the invention
embodiment 1:
Vitamin K
3antibacterial and anti-multi-drug resistant bacteria test
1, experiment material and method
Test strain:
Staphylococcus aureus:
staphylococcus aureusaTCC 25923,
s. aureuss014; Bacillus subtilis:
bacillus subtiliss028.
Methicillin-resistant staphylococcus aureus reference culture: Methicillin-resistant
s. aureusaTCC 33592 (MRSA ATCC 33592); Methicillin-resistant staphylococcus aureus clinical strains: MRSA 01, MRSA 02 and MRSA 03.
MHB culture medium: beef extract powder 2.0 g, soluble starch 1.5g, acid hydrolyzed casein 17.5 g, pure water 1000 mL, pH 7.4.
The preparation of test sample solution: accurately take respectively
1with
2in right amount, add a small amount of DMSO and dissolve, be then mixed with by MHB culture medium the test sample solution (DMSO concentration is less than 5%) that final concentration is 256 μ g/mL.
According to the predetermined operation of CLSI standard, antibacterial and the anti-multi-drug resistant bacteria activity of above-claimed cpd all adopts micro-broth dilution method to test, process is as follows: MHB culture medium be added in 96 good hole polystyrene plates of sterilizing, every hole adds 100 μ L, then respectively 100 μ L sample solutions are added the 1st hole of corresponding row on the same plate, last 1 behavior solvent blank contrast, mixing, then dilute by coubling dilution, the 1st hole is made to be respectively 128 to the concentration of the 11st hole compound, 64, 32, 16, 8, 4, 2, 1, 0.5, 0.25 and 0.13 μ g/mL, 12nd hole is growth control, do not add any sample solution.Last adding in every hole is diluted to through MHB culture medium the test organisms suspension that spore concentration is 1.0 × 107 CFU/mL, every hole adds 100 μ L, namely obtains the bacterium sample mixture that compound concentration is respectively 64,32,16,8,4,2,1,0.5,0.25,0.13 and 0.06 μ g/mL.In the constant-temperature table of the rearmounted temperature of cap seal 35 DEG C, rotating speed 150 rpm, hatch 20 h judged results.When in growth control hole and solvent control hole, test strain obviously grows, be the minimum inhibitory concentration (MIC) of this compound to test strain with the minimum compound concentration of inhibition test strain growth complete in aperture.
2, experimental result
Compound
1with
2what antibacterial and anti-multi-drug resistant bacteria activity (representing with minimum inhibitory concentration) was tested the results are shown in Table 1.
table 1 vitamin K
3
antibacterial and anti-multi-drug resistant bacteria active
3, conclusion
As shown in Table 1, compound
1with
28,16 μ g/mL are respectively to the minimum inhibitory concentration of staphylococcus aureus, 4,8 μ g/mL are respectively to the minimum inhibitory concentration of bacillus subtilis, 8,16 μ g/mL are respectively to the minimum inhibitory concentration of multi-drug resistant bacteria MRSA.Show: vitamin K
3(
1with
2)to the growth of above-mentioned each test strain, all there is obvious antagonism.Therefore, vitamin K of the present invention
3there is antibacterial and anti-multi-drug resistant bacteria activity significantly, can be used for the medicine preparing treatment antibacterial and multi-drug resistant bacteria infection.
embodiment 2:
Vitamin K
3the preparation of tablet
1. the every sheet consumption of prescription 300 consumptions
Vitamin K
3(2-MNQ,
1) 0.0750g 22.5g
Starch 0.0200g 6g
10% starch slurry is appropriate
Magnesium Stearate proper quantity;
2. method for making:
The preparation of (1) 10% starch slurry: added by 2g starch in about 20ml purified water, Heat Gelatinization, makes the starch slurry of 10%.
(2) granulate: get recipe quantity 2-MNQ (
1) mix homogeneously with starch, add appropriate 10% starch slurry soft material, cross 16 mesh sieves and granulate, the grain that will wet, in 40 ~ 50 DEG C of dryings, mixes with magnesium stearate with 16 mesh sieve granulate.
(3) tabletting: by said vitamin K
3granule is tabletting on tablet machine, obtains vitamin K
3element sheet.
(4) coating: by vitamin K
3element sheet sugar coating, obtains vitamin K
3sheet.
3. tablet quality measures
(1) inspection item and method: the weight differential and the disintegration that measure above-mentioned tablet respectively according to current edition Pharmacopoeia of the People's Republic of China appended claims.
(2) result: above-mentionedly prepare the content difference of tablet and the results are shown in Table 2 disintegration.
table 2 prepares weight differential and the disintegration of tablet
embodiment 3:
Vitamin K
3the preparation of injection
1. prescription often props up consumption 500 consumptions
Vitamin K
3(menadione sodium bisulfite,
2) 0.0200g 10.0g
Sodium sulfite 0.0005g 0.25g
Water for injection adds to 1000mL;
2. method for making:
(1) preparation of injection: the water for injection measuring recipe quantity 80%, logical carbon dioxide is saturated, add recipe quantity menadione sodium bisulfite (
2) make it dissolve, gradation slowly adds sodium bicarbonate, stirs and makes to dissolve completely, then regulates medicinal liquid pH 2.5 ~ 3.5, adds the saturated water for injection of carbon dioxide to enough.Use G
3sintered filter funnel leaks in advance, then uses the microporous filter membrane fine straining of 0.45 μm.Check filtrate clarity.
(2) perfusion and sealing by fusing: will filter qualified medicinal liquid, fill is immediately in 2 mL ampoules, and logical carbon dioxide is in ampoule upper space.With filling with envelope, the ampoule top after sealing by fusing should round and smooth, without tip, bubbling or depressed phenomenon.
(3) sterilizing and leak detection: by ampoule good for embedding 100 DEG C of steam sterilizations 15 minutes of circulating.Sterilizing is complete puts into 1% serge blue aqueous solution immediately by ampoule, reject variable color ampoule, qualified ampoule is cleaned, dried, for quality examination.
3. vitamin K
3the quality examination of injection:
(1) inspection item and method: the pH value, color, clarity, endotoxin, the content that detect above-mentioned injection respectively according to current edition Pharmacopoeia of the People's Republic of China appended claims.
(2) result: the vitamin K getting ormal weight
3injection number, pH is 3.2 on inspection, solution colour water white transparency, and clarification foreign, tiny electrolytic cell 12 EU, content is 95.3% of labelled amount.
(3) conclusion: prepared vitamin K
3injection is qualified.
Claims (2)
1. vitamin K
3application in preparation treatment bacteriological infection medicine.
2. vitamin K
3application in preparation treatment multi-drug resistant bacteria infection medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310364096.5A CN104415018A (en) | 2013-08-20 | 2013-08-20 | Application of vitamin K3 in preparation of drug for treating bacterial infection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310364096.5A CN104415018A (en) | 2013-08-20 | 2013-08-20 | Application of vitamin K3 in preparation of drug for treating bacterial infection |
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| Publication Number | Publication Date |
|---|---|
| CN104415018A true CN104415018A (en) | 2015-03-18 |
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ID=52965845
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310364096.5A Pending CN104415018A (en) | 2013-08-20 | 2013-08-20 | Application of vitamin K3 in preparation of drug for treating bacterial infection |
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| Country | Link |
|---|---|
| CN (1) | CN104415018A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108451938A (en) * | 2018-04-28 | 2018-08-28 | 华中科技大学 | Application of the menadione sodium bisulfite in preventing and treating alzheimer disease |
| CN113262213A (en) * | 2021-07-07 | 2021-08-17 | 汕头大学医学院 | Application of menadione in preparing medicine for treating esophageal squamous cell carcinoma and/or inhibiting proliferation and metastasis thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005206521A (en) * | 2004-01-22 | 2005-08-04 | Nippon Menaade Keshohin Kk | Antimicrobial agent |
-
2013
- 2013-08-20 CN CN201310364096.5A patent/CN104415018A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005206521A (en) * | 2004-01-22 | 2005-08-04 | Nippon Menaade Keshohin Kk | Antimicrobial agent |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108451938A (en) * | 2018-04-28 | 2018-08-28 | 华中科技大学 | Application of the menadione sodium bisulfite in preventing and treating alzheimer disease |
| CN113262213A (en) * | 2021-07-07 | 2021-08-17 | 汕头大学医学院 | Application of menadione in preparing medicine for treating esophageal squamous cell carcinoma and/or inhibiting proliferation and metastasis thereof |
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Application publication date: 20150318 |
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| RJ01 | Rejection of invention patent application after publication |