CN107661329A - A kind of plastics for miconazole nitrate - Google Patents

A kind of plastics for miconazole nitrate Download PDF

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Publication number
CN107661329A
CN107661329A CN201610995207.6A CN201610995207A CN107661329A CN 107661329 A CN107661329 A CN 107661329A CN 201610995207 A CN201610995207 A CN 201610995207A CN 107661329 A CN107661329 A CN 107661329A
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China
Prior art keywords
miconazole nitrate
plastics
ethanol
present
chitosan
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
CN201610995207.6A
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Chinese (zh)
Inventor
张蛟
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Chengdu Shengshi Guanghua Biological Technology Co Ltd
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Chengdu Shengshi Guanghua Biological Technology Co Ltd
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Priority to CN201610995207.6A priority Critical patent/CN107661329A/en
Publication of CN107661329A publication Critical patent/CN107661329A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/4174Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7015Drug-containing film-forming compositions, e.g. spray-on

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses a kind of plastics for miconazole nitrate, it is by weight, by 15 ~ 42g of miconazole nitrate, 7 ~ 23g of terbinafine HCl, 83 ~ 125g of ethylene glycol, 2 ~ 8g of chitosan, 0.5 ~ 2.1g of azone, 500 ~ 900g of ethanol composition.The obvious effect that miconazole nitrate, terbinafine HCl have to suppressing bacterium in the present invention, miconazole nitrate, terbinafine HCl are prepared into medicine, due to azone percutaneous technique, medicine skin limb penetration power is added, it is shown that superior curative effect of the plastics to chronic eczema;Using miconazole nitrate medicine made of chitosan, no greasy feeling, exhibition is easily applied, adhesive force is strong, has certain tearing toughness, easy to use, to no skin irritation.

Description

A kind of plastics for miconazole nitrate
Technical field
The present invention relates to plastics preparation field, in particular to a kind of plastics for miconazole nitrate.
Background technology
Miconazole nitrate category antifungal.This product can suppress most of fungi in 4mg/L concentration and grow, Blastomyces, Tissue milk born of the same parents Pseudomonas presents extremely sensitive to it, and Cryptococcus, Mycotoruloides, Coccidioides etc. are also sensitive to this product.It can lead to The activity of interference cytochrome P-450 is crossed, so as to suppress the biosynthesis of fungal cell membrane major sterols class-ergosterol, damage Hinder fungal cell membrane and change its permeability, so that important intracellular matter leakage;Also can suppress fungi triacylglycerol and The biosynthesis of phosphatide, suppress the activity of oxidizing ferment and peroxidase, cause intracellular hydrogen peroxide accumulation to cause cell sub-micro Structural degeneration and meronecrosis.It can then be suppressed to candida albicans and be changed into the process of aggressive mycelia from gemma.By nitric acid miaow Health azoles is used for the preparation of plastics, has not been reported.
The content of the invention
It is an object of the invention to provide a kind of plastics for miconazole nitrate.
The present invention is achieved through the following technical solutions:A kind of plastics for miconazole nitrate, it is by weight, by nitre Sour 15 ~ 42g of Miconazole, 7 ~ 23g of terbinafine HCl, 83 ~ 125g of ethylene glycol, 2 ~ 8g of chitosan, 0.5 ~ 2.1g of azone, second 500 ~ 900g of alcohol is formed.
In order to which the present invention is better achieved, further, it is by weight, the miconazole nitrate 20g, hydrochloric acid spy compare naphthalene Fragrant 10g, ethylene glycol 100g, chitosan 4g, azone 1g, ethanol 800g compositions.
In order to which the present invention is better achieved, further, the viscosity of the chitosan is 50mPa s, and deacetylation is not small In 80%.
In order to which the present invention is better achieved, further, the ethanol is the ethanol solution that mass fraction is 50%.
In order to which the present invention is better achieved, further, the ethanol is the ethanol solution that mass fraction is 85%.
The above-mentioned plastics for miconazole nitrate, comprise the following steps:
(1)Take 20g miconazole nitrates and 10g terbinafine HCls to add in 250g ethanol, stirring and dissolving, obtain mixed solution and treat With;
(2)4g chitosans are uniformly sprinkled into again, make it be swelled naturally;
(3)1.0g azones are added, are stirred continuously, and add ethanol to 1000mL;
(4)PH to 6.0 ~ 7.0 is adjusted, stirs evenly, produces for miconazole nitrate medicine
In order to which the method for the present invention, further, the step is better achieved(1)Whipping process it is complete by magnetic stirring apparatus Into.Magnetic stirring apparatus utilizes the magnetisable material characteristic that identical charges repel each other, and magnetic is promoted by constantly converting the polarity at both ends of pedestal Property stirrer rotate, drive sample to rotate by the rotation of magnetic stirrer, mix medicaments uniformity;Magnetic stirring apparatus is using excellent Matter direct current generator, noise is small, and speed governing is steady;Totally enclosed type heating dish can be made to aid in heating to be used, and can heat use for a long time;By gathering The stirrer that tetrafluoroethene and high-quality magnet steel are refined into, high temperature resistant, wear-resisting, resistant to chemical etching, magnetic is strong;Can be in closed container In carry out adjusting mixed work, using it is very good with conveniently;Agitator can design temperature and temperature display, use can be heated for a long time, Digital display is intuitively accurate.
In order to which the method for the present invention, further, the step is better achieved(3)The stainless steel of middle mixed solution is 1200ml large beaker.
In order to which the method for the present invention, further, the step is better achieved(4)In pH regulation adjusted by pH Agent is adjusted.
In order to which the method for the present invention is better achieved, further, the pH adjusting agent is that mass fraction is 85% sodium carbonate Solution or the liquor alumini chloridi of mass fraction 85%.
The present invention compared with prior art, has advantages below and beneficial effect:
(1)The obvious effect that miconazole nitrate, neomycin have to suppressing bacterium in the present invention, miconazole nitrate, neomycin system For into medicine, due to azone percutaneous technique, medicine skin limb penetration power is added, it is shown that plastics is to the excellent of chronic eczema More curative effect;
(2)The present invention uses miconazole nitrate medicine made of chitosan, no greasy feeling, easily applies exhibition, and adhesive force is strong, has certain Tearing toughness, it is easy to use, to no skin irritation;
(3)Preparation technology is simple in the present invention, steady quality, has good mechanical performance with the film of its making, makes to be made The plastics for miconazole nitrate possess without wrapping, it is easy to use, not pollution clothes, be easily accepted by patients the advantages of, And insoluble drug release can be delayed, the advantages that obtaining lasting drug effect.
Embodiment
The present invention is described in further detail with reference to embodiment, but the implementation of the present invention is not limited to this, Without departing from the idea case in the present invention described above, according to ordinary skill knowledge and customary means, various replace is made Change and change, all should be included within the scope of the invention.
Embodiment 1:
The plastics of the miconazole nitrate of the present embodiment, is by weight, by miconazole nitrate 20g, terbinafine HCl 10g, Ethylene glycol 100g, chitosan 4g, azone 1g, ethanol 800g composition.
The preparation method of above-mentioned compound miconazole nitrate plastics, comprises the following steps:
(1)Take 20g miconazole nitrates and 10g terbinafine HCls to add in 250g ethanol, dissolved using magnetic stirrer, It is stand-by to obtain mixed solution;
(2)4g chitosans are uniformly sprinkled into again, make it be swelled naturally;
(3)1.0g azones are added, is contained, is stirred continuously, and add ethanol extremely using 1200ml large beaker 1000mL;
(4)PH to 6.0 ~ 7.0 is adjusted using pH adjusting agent, stirs evenly, produces for miconazole nitrate medicine.
When solution in it is acid when, use quality fraction be 85% sodium carbonate liquor as pH adjusting agent, work as solution alkaline When, use quality fraction is used as pH adjusting agent for 85%
Specific implementation process, affected part is cleaned, affected part surface is applied to for miconazole nitrate medicaments uniformity by obtained, treat it certainly The thick gel-like films of 1 ~ 3mm can be formed after so drying, after 3 ~ 5 hours, the drug administration in film is completed, by it from affected part surface Tear, smear new medicine, one day 1 ~ 2 time, if stop smearing the medicine, determined according to the healing degree of eczema, typically connected It is continuous to smear 1 ~ 2 week, you can recovery from illness.
Embodiment 2:
The present embodiment further, is by weight, the miconazole nitrate 20g, terbinafine HCl in above-described embodiment 10g, ethylene glycol 100g, chitosan 4g, azone 1g, ethanol 800g compositions.Other steps of the present embodiment and above-described embodiment It is identical, repeat no more here.
Embodiment 3:
The present embodiment is in above-described embodiment, and further, the viscosity of the chitosan is 50mPas, and deacetylation is not less than 80%.Other steps of the present embodiment are same as the previously described embodiments, repeat no more here.
Embodiment 4:
The present embodiment is in above-described embodiment, and further, the ethanol is the ethanol solution that mass fraction is 50%.The present embodiment Other steps are same as the previously described embodiments, repeat no more here.
Embodiment 5:
The present embodiment is in above-described embodiment, and further, the ethanol is the ethanol solution that mass fraction is 85%.The present embodiment Other steps are same as the previously described embodiments, repeat no more here.
Embodiment 6:
Make following experiment for the plastics of obtained miconazole nitrate, and clinical efficacy investigation is carried out to it:
First, skin irritation test
Healthy rabbits 3,2.0~2.5kg of body weight are taken, by rabbit backbone both sides unhairing without damaging skin, exposure both sides 5cm is extremely 7cm epidermis, this product 1mL is coated in left side and goes to hair-fields, right side applies saline control, is seen in 24 hours, 48 hours, 72 hours The reaction for applying unconcerned position is examined, as a result each coating area skin is without redness, dermexanthesis, phenomena such as blister.Illustrate this product to skin without Excitant.
2nd, into film test
This coating liquid, which is dipped, with banister brush gently coats thin layer on a glass, while in eczema patients 6 in the back of the hand or toe Film formation time is 150s on a glass for one layer of this product of film observation film formation time result this plastics, is 120s on human body. Illustrate that the film forming of this product is good.
3rd, clinical efficacy is investigated
Treatment group 40, man 32, female 8, age 12-72 year, the course of disease is between 1 month to 6 months.Control group 38, man 26 Example, female 12, age 8-68 year, the course of disease is average 4.2 months, and above case meets the diagnostic criteria of chronic eczema:Clinically Itch, when have and ooze out tendency, incrustation, easy inflammation, while with erythema, blood rash, blood blister rash, erosion, the scales of skin that peel off, infiltration.
Treatment group:After cleaning focus face with 0.1% bromogeramine solution, the clear plastics of film eczema is appropriate, 2 times a day, altogether Treatment 7 days.
Control group:Butyric acid hydrocortisone ointment, outer wiping, 2 times a day, treat 7 altogether.
Observational technique and curative effect determinate standard:Carried out with reference to clinical efficacy criterion [ 2 ].
Treatment results:Treatment group, average cure time 8 days, symptom disappear, cure rate 92.1%, effective percentage 96.1%;Control Group average cure time 12 days, cure rate 56.3%, effective percentage 72.6%.Treatment group is substantially better than control group.
Although an embodiment of the present invention has been shown and described, it will be understood by those skilled in the art that:Not A variety of change, modification, replacement and modification can be carried out to these embodiments by departing under the principle and objective of the present invention, of the invention Scope is limited by claim and its equivalent.

Claims (5)

1. a kind of plastics for miconazole nitrate, it is characterised in that be by weight, by 15 ~ 42g of miconazole nitrate, salt Sour 7 ~ 23g of Terbinafine, 83 ~ 125g of ethylene glycol, 2 ~ 8g of chitosan, 0.5 ~ 2.1g of azone, 500 ~ 900g of ethanol compositions.
2. a kind of plastics for miconazole nitrate according to claim 1, it is characterised in that be by weight, institute State miconazole nitrate 20g, terbinafine HCl 10g, ethylene glycol 100g, chitosan 4g, azone 1g, ethanol 800g composition.
A kind of 3. plastics for miconazole nitrate according to claim 1 or 2, it is characterised in that the chitosan Viscosity be 50mPas, deacetylation is not less than 80%.
4. a kind of plastics for miconazole nitrate according to claim 1 or 2, it is characterised in that the ethanol is Mass fraction is 50% ethanol solution.
5. a kind of plastics for miconazole nitrate according to claim 1 or 2, it is characterised in that the ethanol is Mass fraction is 85% ethanol solution.
CN201610995207.6A 2016-11-11 2016-11-11 A kind of plastics for miconazole nitrate Withdrawn CN107661329A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610995207.6A CN107661329A (en) 2016-11-11 2016-11-11 A kind of plastics for miconazole nitrate

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Application Number Priority Date Filing Date Title
CN201610995207.6A CN107661329A (en) 2016-11-11 2016-11-11 A kind of plastics for miconazole nitrate

Publications (1)

Publication Number Publication Date
CN107661329A true CN107661329A (en) 2018-02-06

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112826810A (en) * 2021-01-27 2021-05-25 西安交通大学 Coating agent combined with myricetin/azole drugs and used for preventing external surface infection of percutaneous catheter and application thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112826810A (en) * 2021-01-27 2021-05-25 西安交通大学 Coating agent combined with myricetin/azole drugs and used for preventing external surface infection of percutaneous catheter and application thereof

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Application publication date: 20180206

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