CN110269835A - A kind of antibacterial prosthetic gel of carbomer gynaecology and preparation method thereof - Google Patents
A kind of antibacterial prosthetic gel of carbomer gynaecology and preparation method thereof Download PDFInfo
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/716—Glucans
- A61K31/722—Chitin, chitosan
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
- A61K31/728—Hyaluronic acid
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
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- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/02—Local antiseptics
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- 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
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- 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
- A61P31/10—Antimycotics
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Abstract
The invention discloses a kind of carbomer gynaecology antibacterial prosthetic gels and preparation method thereof, by weight percentage, including carbomer 934 0.5%~2%, carboxymethyl chitosan 0.3~2%, benzyl alcohol 0.3%~4%, Sodium Hyaluronate 0.1%~0.2%, lubricant 2%~5%, natrium adetate 0.1~0.2%, neutralizer 0.1~0.5%, surplus are ultrapure water.The present invention is using carbomer 934 as gel-type vehicle, and carboxymethyl chitosan, benzyl alcohol collaboration anti-inflammatory is antibacterial and repairs mucous membrane with Sodium Hyaluronate, promotes wound healing while reaching Efficient antibacterial.Product of the present invention is easy to use, safe to have no toxic side effect, and has efficient therapeutic effect for gynecological diseases such as vaginitis and cervicitises, reduces because of inflammation bring malaise symptoms.
Description
Technical field
The present invention relates to antibacterial prosthetic gels of a kind of carbomer gynaecology and preparation method thereof.
Background technique
Live away from home a variety of germs in normal health vagina, but normal condition can voluntarily reach colony balance, and to disease
The function that the intrusion of substance has nature to defend, so under normal circumstances and not pathogenic.When because a variety of causes broken it is this flat
Weighing apparatus, just will appear vaginitis.Vaginitis is most common, the highest a kind of disease of disease incidence in gynaecology, accounts for about outpatients of gynecology
One third, women is likely to illness with all ages and classes stage at all seasons.Vaginitis to the daily life of patient and
Work is made troubles, if being treated not in time, there will be the possibility for causing other lesions, such as situations such as infertile.
Vaginitis disease incidence is very high or even repeated multiple times breaking-out, this is related with the mistake in understanding of many patients.Many patients
Once infect vaginitis, frequent progress clean and takes antibiotic and is treated, however frequently using washing lotion clean vulva or
It is to carry out vaginadouche, vagina acid-base degree can be changed, the ecological balance of vagina itself is destroyed, aggravated the state of an illness instead.It is practical
On, cause the pathogen of vaginitis in addition to bacterium, is exactly mould and trichomonad, general antibiotic is to them without therapeutic effect, phase
Instead, long-term abuse of antibiotics easily makes germ generate drug resistance, can then aggravate infection symptoms using antibiotic when especially infecting fungi.
(application number: 201110116366.1) disclose Carbomer cervical gel mainly has card wave to Carbomer cervical gel
Nurse, glycerol, triethanolamine, benzyl alcohol, disodium ethylene diamine tetraacetate (EDTA-2Na), water composition, the content of various composition is every
Contain 0.1-10 grams of carbomer, 2-10 grams of glycerol, 0.1-1.0 grams of triethanolamine, disodium ethylene diamine tetraacetate in 100 grams of gels
0.01-1.0 grams, 0.03-5.0 grams of benzyl alcohol, remaining is water, wherein the content of-COOH group is 0.1-0.3g.For reducing
Rotten to the corn face promotes the healing of cervical erosion face, mitigates local inflammation degree, reduces leucorrhea increasing, improves haemorrhagia sub coitu, bone sacrum pain
Bitterly, blood sample and the inferior symptom of purulence belt transect.Disinfection antisepsis is played using benzyl alcohol in this gel, anti-inflammatory fungistatic effect is not excellent
It is different.Herein using carbomer 934 as gel-type vehicle, carboxymethyl chitosan, benzyl alcohol collaboration anti-inflammatory is antibacterial and is repaired with Sodium Hyaluronate
Multiple mucous membrane, promotes wound healing while reaching Efficient antibacterial.By patent search, have not been reported both at home and abroad.
Summary of the invention
The present invention provides a kind of antibacterial prosthetic gel of carbomer gynaecology and preparation method thereof, reach anti-inflammatory it is antibacterial while
Promote healing, it is easy to operate, have no toxic side effect, for preventing and treating gynaecological imflammation.
Above-mentioned purpose to realize the present invention, The technical solution adopted by the invention is as follows:
A kind of antibacterial prosthetic gel of carbomer gynaecology, by weight percentage, including carbomer 934 0.5%~2%,
Carboxymethyl chitosan 0.3~2%, benzyl alcohol 0.3%~4%, Sodium Hyaluronate 0.1%~0.2%, lubricant 2%~5%,
Natrium adetate 0.1~0.2%, neutralizer 0.1~0.5%, surplus are ultrapure water.
The lubricant be any one of propylene glycol, glycerol, xylitol, polyethylene glycol-400, polyethylene glycol -200 or
It is a variety of.
The neutralizer is any one of triethanolamine, sodium hydroxide, sodium bicarbonate.
A kind of preparation method of the antibacterial prosthetic gel of carbomer gynaecology, comprising the following steps:
(1) carbomer is dispersed in purified water, is sufficiently stirred completely after swelling, obtains A phase component.
(2) it disperses carboxymethyl chitosan in purified water, dissolution is sufficiently stirred, obtain B phase component.
(3) it disperses Sodium Hyaluronate in purified water, dissolution is sufficiently stirred, obtain C phase component.
(4) it disperses benzyl alcohol, lubricant, natrium adetate in the purified water of surplus, dissolution is sufficiently stirred, obtains D
Phase component.Tetra- phase solution of A, B, C, D is all mixed, is stirred 0.5 hour.
(5) it weighs formula ratio neutralizer to pour into mixed liquor, completely, mixed liquor becomes gel from liquid for stirring.It takes
Sample measures the performances such as pH value, viscosity, and filling after qualified, sealing, sterilizes to get solidifying to the antibacterial prosthetic of carbomer gynaecology at packaging
Glue.
In mentioned component:
Carbomer (carbomer) also known as carbopol (carboxypolymethleme, CP), be it is a kind of by acrylic acid with
High molecular polymer made of allyl sucrose crosslinking, carbomer are a kind of multiduty high molecular material and pharmaceutic adjuvant, are
One of most common primary raw material of gelling agent is prepared, uses carbomer that there is good biology as the gynecological gel that matrix is made into
Compatibility solves the problems, such as that drug releases the drug for a long time in intravaginal, targetedly reaches drug and be locally discharged into absorption site,
It is improved curative effect.
Carboxymethyl chitosan (carboxymethyl chitosan, CMC) is the access carboxylic first in chitosan molecule chain
Base group is difficult to the shortcomings that dissolving in water and ordinary organic solvents so as to improve chitosan, has good aqueous solubility and resists
Bacterium property.Carboxymethyl chitosan can generate simultaneously bacteriostasis in bacterium surface and bacterium.The antibacterial factor-on CMC strand
NH+3It is gathered in phage surface, or attracts each other to form one layer of high score with cations such as sialic acid phosphatide in microorganism wall
Sub- film influences external nutrition substance to intracellular transport, hinders the metabolism and breeding of internal microorganism.Or and bacterial cell membrane
On lipoid-protein complex reaction, make protein denaturation, change the selective penetrated property of cell membrane, cytoplasm is caused to be lost,
Cell plasmolysis, leads to bacterial death, reaches fungistatic effect.After CMC is penetrated into bacterial cell body, or absorption is thin
The cytoplasm that negative electrical charge is had in cell space upsets the normal physiological activity of cell, or thin in bacterium by the way that flocculation occurs
The transcription of blocking dna intracellular, to inhibit the breeding of bacterium.Carboxyl and coexisting for amino make its tool in carboxymethyl chitosan structure
There is better hemostasis, antibacterial, the characteristics such as bio-compatible make it obtain consistent approval in field of medicaments.
Benzyl alcohol also known as benzylalcohol are a kind of colourless transparent liquids.Benzyl alcohol is claimed because having effects that anesthesia, analgesia
For " painless water ", the common drug solvent done in medical injection also can be used as the bacteriostatic agent preservative of ointment or medical fluid.Meanwhile
Because playing good characteristic, it is also widely used for the other fields such as food, cosmetics, coating, essence.
Sodium Hyaluronate is the sodium-salt form of hyaluronic acid.By N-Acetyl-D-glucosamine and glucuronic acid disaccharide unit
Reaction alternately couples.The Sodium Hyaluronate of different molecular weight is also different in the application of field of medicaments.Work as body surface
Movement, hyperplasia, differentiation and the phagocytosis that macromolecule when wound, high concentration Sodium Hyaluronate inhibition cell occurs, to promote wound
Healing.
The antibacterial prosthetic gel of carbomer gynaecology is made according to optimal proportion in above-mentioned several components by the present invention, with card wave
Nurse 934 is gel-type vehicle, and carboxymethyl chitosan, benzyl alcohol collaboration anti-inflammatory is antibacterial and repairs mucous membrane with Sodium Hyaluronate, reaches high
Promote wound healing while imitating antibacterial.Product of the present invention is easy to use, safe to have no toxic side effect, for vaginitis and cervicitis
Equal gynecological diseases have efficient therapeutic effect, reduce because of inflammation bring malaise symptoms.
Specific embodiment:
Embodiment 1: a kind of antibacterial prosthetic gel of carbomer gynaecology, by weight percentage, including carbomer 934 1%,
Carboxymethyl chitosan 0.3%, benzyl alcohol 4%, Sodium Hyaluronate 0.1%, lubricant 5%, natrium adetate 0.2%, neutralizer
0.2%, surplus is ultrapure water.The lubricant is propylene glycol, in glycerol, xylitol, polyethylene glycol-400, polyethylene glycol -200
It is any one or more.The neutralizer is any one of triethanolamine, sodium hydroxide, sodium bicarbonate.
Carbomer is dispersed in purified water, is sufficiently stirred completely after swelling, obtains A phase component;By carboxylic first
Base enclosure glycan is scattered in purified water, and dissolution is sufficiently stirred, and obtains B phase component;It disperses Sodium Hyaluronate in purified water, fills
Divide stirring and dissolving, obtains C phase component;It disperses benzyl alcohol, lubricant, natrium adetate in the purified water of surplus, sufficiently stirs
Dissolution is mixed, D phase component is obtained.Tetra- phase solution of A, B, C, D is all mixed, is stirred 0.5 hour;Formula ratio neutralizer is weighed to pour into
In mixed liquor, completely, mixed liquor becomes gel from liquid for stirring.The performances such as pH value, viscosity are measured by sampling, are filled after qualified
Dress, packaging, sterilizes to get the antibacterial prosthetic gel of carbomer gynaecology is arrived at sealing.
Embodiment 2: a kind of antibacterial prosthetic gel of carbomer gynaecology, by weight percentage, including carbomer
9341.5%, carboxymethyl chitosan 0.6%, benzyl alcohol 3%, Sodium Hyaluronate 0.15%, lubricant 3%, natrium adetate
0.2%, neutralizer 0.3%, surplus is ultrapure water.The lubricant is propylene glycol, glycerol, xylitol, polyethylene glycol-400, gathers
Ethylene glycol -200 is any one or more of.The neutralizer is any one of triethanolamine, sodium hydroxide, sodium bicarbonate.
Carbomer is dispersed in purified water, is sufficiently stirred completely after swelling, obtains A phase component;By carboxylic first
Base enclosure glycan is scattered in purified water, and dissolution is sufficiently stirred, and obtains B phase component;It disperses Sodium Hyaluronate in purified water, fills
Divide stirring and dissolving, obtains C phase component;It disperses benzyl alcohol, lubricant, natrium adetate in the purified water of surplus, sufficiently stirs
Dissolution is mixed, D phase component is obtained.Tetra- phase solution of A, B, C, D is all mixed, is stirred 0.5 hour;Formula ratio neutralizer is weighed to pour into
In mixed liquor, completely, mixed liquor becomes gel from liquid for stirring.The performances such as pH value, viscosity are measured by sampling, are filled after qualified
Dress, packaging, sterilizes to get the antibacterial prosthetic gel of carbomer gynaecology is arrived at sealing.
Embodiment 3: a kind of antibacterial prosthetic gel of carbomer gynaecology, by weight percentage, including carbomer 934 2%,
Carboxymethyl chitosan 1%, benzyl alcohol 2%, Sodium Hyaluronate 0.2%, lubricant 4%, natrium adetate 0.2%, neutralizer
0.3%, surplus is ultrapure water.The lubricant is propylene glycol, in glycerol, xylitol, polyethylene glycol-400, polyethylene glycol -200
It is any one or more.The neutralizer is any one of triethanolamine, sodium hydroxide, sodium bicarbonate.
Carbomer is dispersed in purified water, is sufficiently stirred completely after swelling, obtains A phase component;By carboxylic first
Base enclosure glycan is scattered in purified water, and dissolution is sufficiently stirred, and obtains B phase component;It disperses Sodium Hyaluronate in purified water, fills
Divide stirring and dissolving, obtains C phase component;It disperses benzyl alcohol, lubricant, natrium adetate in the purified water of surplus, sufficiently stirs
Dissolution is mixed, D phase component is obtained.Tetra- phase solution of A, B, C, D is all mixed, is stirred 0.5 hour;Formula ratio neutralizer is weighed to pour into
In mixed liquor, completely, mixed liquor becomes gel from liquid for stirring.The performances such as pH value, viscosity are measured by sampling, are filled after qualified
Dress, packaging, sterilizes to get the antibacterial prosthetic gel of carbomer gynaecology is arrived at sealing.
Biocidal property test is carried out by product of the method as defined in GB 15979-2002 appendix C 4 to embodiment 1-3, and with list
One 2% carboxymethyl chitosan sugar aqueous solution is reference substance 1, and 4% single benzyl alcohol aqueous solution is reference substance 2.By embodiment 1-3
The bacteriostasis rate that product and reference substance act on after ten minutes respectively is as shown in table 1.
1 bacteriostasis rate of table (%)
Group | Escherichia coli | Staphylococcus aureus | Candida albicans |
Embodiment 1 | 97.26 | 96.47 | 96.05 |
Embodiment 2 | 98.13 | 99.23 | 98.89 |
Embodiment 3 | 94.65 | 95.76 | 94.58 |
Reference substance 1 | 68.63 | 73.52 | 65.15 |
Reference substance 2 | 79.25 | 78.56 | 75.12 |
Wound experiment is carried out to the product of embodiment 2, control group is in addition to being not added with Sodium Hyaluronate ingredient, other compositions
It is consistent with 2 ingredient of embodiment.
By mouselet skin of back shaving, is gently rubbed with fine sandpaper and cause one square centimeter of slight bleeding.By example 2 with
Substance described in control group is coated uniformly on the skin of mouse breakage, cleans the surface of a wound and coating twice sooner or later daily, after 4 days, is seen
Examine skin repair situation.Experimental result is as shown in table 2.
Table 2
Group | Dosage | Skin repair situation after treatment 4 days |
Embodiment 2 | 0.5g/cm2 | Healing completely, no clear scar scar |
Control group | 0.5g/cm2 | Local woanded surface incrustation, scar are more apparent |
Claims (4)
1. a kind of carbomer gynaecology antibacterial prosthetic gel and preparation method thereof, it is characterised in that: by weight percentage, packet
Include carbomer 934 0.5%~2%, carboxymethyl chitosan 0.3~2%, benzyl alcohol 0.3%~4%, Sodium Hyaluronate 0.1%~
0.2%, lubricant 2%~5%, natrium adetate 0.1~0.2%, neutralizer 0.1~0.5%, surplus is ultrapure water.
2. the antibacterial prosthetic gel of carbomer gynaecology according to claim 1, which is characterized in that the lubricant is the third two
Alcohol, glycerol, xylitol, polyethylene glycol-400, polyethylene glycol -200 are any one or more of.
3. the antibacterial prosthetic gel of carbomer gynaecology according to claim 1, which is characterized in that the neutralizer is three second
Any one of hydramine, sodium hydroxide, sodium bicarbonate.
4. a kind of prepare the preparation method of antibacterial prosthetic gel of carbomer gynaecology described in claim 1-3, feature exists
In, comprising the following steps:
(1) carbomer is dispersed in purified water, is sufficiently stirred completely after swelling, obtains A phase component.
(2) it disperses carboxymethyl chitosan in purified water, dissolution is sufficiently stirred, obtain B phase component.
(3) it disperses Sodium Hyaluronate in purified water, dissolution is sufficiently stirred, obtain C phase component.
(4) it disperses benzyl alcohol, lubricant, natrium adetate in the purified water of surplus, dissolution is sufficiently stirred, obtain D phase group
Point.Tetra- phase solution of A, B, C, D is all mixed, is stirred 0.5 hour.
It weighs formula ratio neutralizer to pour into mixed liquor, completely, mixed liquor becomes gel from liquid for stirring.PH is measured by sampling
The performances such as value, viscosity, filling after qualified, sealing, sterilize to get the antibacterial prosthetic gel of carbomer gynaecology is arrived at packaging.
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2021036294A1 (en) * | 2019-08-28 | 2021-03-04 | 南京天朗制药有限公司 | Vaginal acid-base buffer gel and preparation method |
CN113230205A (en) * | 2021-05-22 | 2021-08-10 | 绍兴鸿瑞生物科技有限公司 | Gynecological gel preparation and preparation method and application thereof |
CN114903801A (en) * | 2021-06-17 | 2022-08-16 | 苏州鑫斯达医疗科技有限公司 | Silk protein gynecological gel and preparation method thereof |
-
2019
- 2019-08-05 CN CN201910718773.6A patent/CN110269835A/en not_active Withdrawn
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2021036294A1 (en) * | 2019-08-28 | 2021-03-04 | 南京天朗制药有限公司 | Vaginal acid-base buffer gel and preparation method |
CN113230205A (en) * | 2021-05-22 | 2021-08-10 | 绍兴鸿瑞生物科技有限公司 | Gynecological gel preparation and preparation method and application thereof |
CN114903801A (en) * | 2021-06-17 | 2022-08-16 | 苏州鑫斯达医疗科技有限公司 | Silk protein gynecological gel and preparation method thereof |
CN114903801B (en) * | 2021-06-17 | 2024-08-27 | 苏州鑫斯达医疗科技有限公司 | Silk protein gynecological gel and preparation method thereof |
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Application publication date: 20190924 |