[go: up one dir, main page]

CN105833278A - Composition for treating xerostomia and oral diseases - Google Patents

Composition for treating xerostomia and oral diseases Download PDF

Info

Publication number
CN105833278A
CN105833278A CN201610258020.8A CN201610258020A CN105833278A CN 105833278 A CN105833278 A CN 105833278A CN 201610258020 A CN201610258020 A CN 201610258020A CN 105833278 A CN105833278 A CN 105833278A
Authority
CN
China
Prior art keywords
compositions
xerostomia
active component
composition
content
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.)
Granted
Application number
CN201610258020.8A
Other languages
Chinese (zh)
Other versions
CN105833278B (en
Inventor
刘素云
冯朴纯
狄忠
黄巧萍
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beijing Qihui Biomedical Co., Ltd.
Original Assignee
Beijing Chiral-Tech Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Beijing Chiral-Tech Pharmaceutical Co Ltd filed Critical Beijing Chiral-Tech Pharmaceutical Co Ltd
Priority to CN201610258020.8A priority Critical patent/CN105833278B/en
Publication of CN105833278A publication Critical patent/CN105833278A/en
Application granted granted Critical
Publication of CN105833278B publication Critical patent/CN105833278B/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • A61K31/245Amino benzoic acid types, e.g. procaine, novocaine
    • 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
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525Isoalloxazines, e.g. riboflavins, vitamin B2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/06Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/19Acanthaceae (Acanthus family)
    • A61K36/195Strobilanthes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/31Brassicaceae or Cruciferae (Mustard family), e.g. broccoli, cabbage or kohlrabi
    • A61K36/315Isatis, e.g. Dyer's woad
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/70Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • A61K36/704Polygonum, e.g. knotweed
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • 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
    • A61K47/38Cellulose; Derivatives thereof
    • 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
    • A61K47/42Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses a composition for treating xerostomia and oral diseases. The composition for treating xerostomia and oral diseases comprises the following ingredients: a humectant, a solvent, a thickener, a pH regulator, an essence and a preservative. The composition for treating xerostomia and oral diseases can further comprise one or more active ingredients beside the ingredients; and the pharmaceutical composition containing the active ingredients has the function of treating xerostomia and oral diseases. Various xerostomia symptoms can be greatly relieved; meanwhile, the oral diseases of gingivitis, angular cheilitis, oral ulcer, rampant caries and the like caused by the xerostomia symptoms can be treated; multiple choices are provided in flavor, so that the requirements of different people can be met; and therefore, the composition has a wide application market in the future.

Description

For treating the compositions of xerostomia and oral disease
Technical field
The present invention is provided to treat xerostomia and the compositions of oral disease, belong to field of medicaments.
Background technology
Sjogren syndrome (Sj gren'sSyndrome, SS) also known as Sjogren syndrome, it is a kind of with exocrine gland stove Property lymphocytic infiltration is characterized, and involves the systemic autoimmune disease of multiple organ, multisystem, is also salivary gland most generation The autoimmune disease of table.Clinic is divided into primary Sjogren's syndrome (primary SS, pSS) and Secondary cases to be dried comprehensive Simulator sickness (secondary SS, sSS) two classes.Display SS women is multiple in Epidemiological study, accounts for the 90% of all cases, sends out The sick age concentrates on 30~60 years old, and this disease is 0.29%~0.77% in population of China prevalence, prevalence in old group It is 3%~4%, is one of modal connective tissue disease.PSS clinically with xerostomia, eye is dry is characterized, and with serum from The generation of body antibody, the person of being in a bad way does not only has mouth, eye infringement, it may also occur that interstitial pulmonary fibrosis, pulmonary hypertension, renal tubules Acidosis, hepatic injury and central nervous system such as get involved at the serious viscera.
Some crowd is probably due to long-time drug administration, accept radiation cure or infect some disease and cause its saliva Liquid gland is impaired, and the SS patient of about 80% occurs that salivation declines, i.e. xerostomia (Xerostomia).Saliva is by conduit The mucus composition of the water of epithelial cells, electrolyte, enzyme and acinus secretion.In early days, conduit is thin because of around stove lymph in morbidity The impact of born of the same parents' infiltration, moisture is secreted and is likely to reduced.It is magneta colour that xerostomia can cause tongue surface, and has deep rill to occur, the sense of taste It is likely to be affected.Salivary gland secretion decline causes the antibacterial action of enzyme in saliva to be lost, and is therefore often accompanied by gingivitis, mouth The oral diseases such as angle inflammation and rampant caries.
Treatment to SS has multiple method the most clinically, but there is no radical cure method.Xerostomia shape is significantly suffered from Person, can use artificial saliva, mouthspray, rush salivation medicine etc. to carry out symptomatic treatment.
Xerostomia glue (Dry Mouth Gel) is i.e. the medicine researched and developed for this symptom of xerostomia, belongs to medical treatment in the U.S. Apparatus category, at present, domestic there is no same types of drug listing.The alleviation various xerostomia symptom of its energy high degree, can help Help xerostomia crowd to increase the lubricity in oral cavity, lasting protecting film can be formed, the oral soft tissue that long-effective protection is fragile.
Summary of the invention
Present inventors have surprisingly discovered that, for alleviating the xerostomia glue of xerostomia symptom, adjust its formula components, add Enter the active substance for oral disease, xerostomia can be alleviated, can treat again the concurrent gingivitis of xerostomia symptom, The oral diseases such as angular cheilitis, oral ulcer, rampant caries, achieve many things at one stroke, and then complete the present invention.
Specifically, one embodiment of the invention is, a kind of compositions for treating xerostomia, and it comprises: protect Humectant, the content of described wetting agent is 60%;Solvent, the content of described solvent is 32 ~ 37%;Thickening agent, containing of described thickening agent Amount is 2 ~ 3%;PH adjusting agent, the content of described pH adjusting agent is 0.2%;Essence, the content of described essence is 0.05 ~ 0.5%;Anti- Rotten agent, the content of described preservative is 0.05%.
According to compositions of the present invention, wherein, described wetting agent be two polyglycereol, glycerol, propylene glycol, aminoacid, One or more in sorbitol.
According to compositions of the present invention, wherein, described thickening agent is sodium carboxymethyl cellulose, gelatin, carbomer, sea One or more in alginate, carrageenan;Described pH adjusting agent is in sodium citrate, sodium hexameta phosphate, potassium citrate Plant or several.
According to compositions of the present invention, wherein, described solvent is water.
According to compositions of the present invention, wherein, described essence can be the essence of various taste, for example, Fructus Citri Limoniae Taste, apple aroma, strawberry flavor, honey peach taste;Described preservative can be by the preservative pharmaceutically accepted, for example, para hydroxybenzene first One or more in acetoacetic ester, potassium sorbate, EDTA-2 sodium, sodium acetate, citric acid.
In another embodiment of the present invention, described compositions can also comprise one or more active component, institute Stating the pharmaceutical composition comprising active component and possess effect for the treatment of oral disease, the content of described active component is 2-5%.
According to compositions of the present invention, wherein, described active component can be oral disease therapeutic medicine, for example, One or both compositions in benzocaine, triamcinolone acetonide, lignocaine, chlorhexidine, molecular iodine, dexamethasone acetate.
According to compositions of the present invention, wherein, described active component can be Antipyretics thing, for example, Buddhist nun One in Mei Shuli, ibuprofen, acetaminophen, diclofenac sodium, diclofenac potassium.
According to compositions of the present invention, wherein, described active component can be antibacterials, for example, metronidazole, One in tinidazole, ofloxacin, lomefloxacin, erythromycin ethylsuccinate, pefloxacin mesilate.
According to compositions of the present invention, wherein, described active component can be Chinese medicine or Chinese medicine composition, for example, One in Indigo Naturalis, Alumen, Borneolum Syntheticum, propolis, Mentholum, Fructus Forsythiae, Herba Taraxaci, Caulis Lonicerae, Spina Gleditsiae, Herba Solidaginis, Flos Lonicerae Or multiple pharmaceutical composition.
In other embodiments of the present invention, the active substance of the compositions of the present invention can also be vitamins, resist Infectious agent, immunosuppressant, antihistaminic, plant or Sargassum extract and other conventional composition.Other combination of the present invention Thing can comprise the various complementary elements that those skilled in the art can select with conventional criteria equally.
The pharmaceutical composition of the present invention is possible not only to alleviate various xerostomia symptom dramatically, gives xerostomia patient Tooth and oral cavity tissue one protective layer, play oral cavity moisturizing, moisten and pure and fresh curative effect, bioavailability is high, moisturizing is long Effect, is simultaneous for different oral diseases and selects different active component formula, can treat the tooth that xerostomia is concurrent The multiple oral diseases such as gingivitis, angular cheilitis, oral ulcer, rampant caries.
The pharmaceutical composition of the present invention has appearance transparent, fine and smooth, launches easily coating, skin comfort after coating, depletion of QI Vexed sense, Transdermal absorption speed is faster than ointment and cream, and compared with oral solution, this product has certain adhesion, The time of staying of oral tissue surfaces is long, and beneficially the release of medicine and absorption, easy to use, without the side effect of Formulations for systemic administration, Good mouthfeel, and have various tastes to select for user, the needs of different crowd can be met, following will have wide market.
The effect of the present invention is described below by specific embodiment.
Detailed description of the invention
Embodiment is implemented under premised on technical solution of the present invention, gives detailed embodiment and concrete Operating process, but protection scope of the present invention is not limited to following embodiment.
In following embodiment, method therefor is conventional method if no special instructions.Formula according to the present invention is developed The state of compositions is gel.
Embodiment 1-3, the preparation of the compositions for the treatment of xerostomia
The composite formula of embodiment 1-3 is as shown in table 1.
The formula of the compositions of xerostomia treated by table 1
Composition Function Embodiment 1 Embodiment 2 Embodiment 3
Two polyglycereol Wetting agent 60g
Sorbitol Wetting agent 60g
Propylene glycol Wetting agent 60g
Water Solvent 37g 36.1g 36.5g
Sodium carboxymethyl cellulose Thickening agent 3g 2g
Gelatin Thickening agent 2g 1g
Carrageenan Thickening agent 0.7g 0.5g
Potassium citrate PH regulator 0.2g
Sodium citrate PH regulator 0.3g 0.3g
Fructus Citri Limoniae essence Correctives 0.05g
Strawberry essence Correctives 0.05g 0.1g
Ethylparaben Preservative 0.05g
Potassium sorbate Preservative 0.05g
Sodium acetate Preservative 0.1g
Gross weight 100g 100g 100g
The preparation method of the compositions of the treatment xerostomia of the present invention is as follows:
1) each component is weighed by formula;
2) thickening agent is scattered in wetting agent;
3) by soluble in water for remaining component;
4) again by 2) pour 3 into) in, stir.
Embodiment 4-9, the preparation of the compositions for the treatment of xerostomia and oral ulcer, angular cheilitis, gingivitis etc.
Composite formula such as table 2 ~ 7 institute for the treatment of xerostomia and oral ulcer, angular cheilitis, the gingivitis etc. of embodiment 4-9 Show:
The composite formula of xerostomia and oral ulcer treated by table 2
Composition Function Embodiment 4
Propylene glycol Wetting agent 60g
Water Solvent 35g
Benzocaine Active component 2g
Sodium carboxymethyl cellulose Thickening agent 2g
Carrageenan Thickening agent 0.7g
Sodium citrate PH adjusting agent 0.2g
Honey peach essence Correctives 0.05g
Ethylparaben Preservative 0.05g
Gross weight 100g
The composite formula of xerostomia and oral ulcer treated by table 3
Composition Function Embodiment 5
Two polyglycereol Wetting agent 60g
Water Solvent 35.2g
Chlorhexidine Active component 1.5g
Dexamethasone acetate Active component 0.05g
Vitamin B2 Active component 0.15g
Sodium carboxymethyl cellulose Thickening agent 2g
Carrageenan Thickening agent 0.7g
Sodium citrate PH adjusting agent 0.2g
Strawberry essence Correctives 0.05g
Ethylparaben Preservative 0.05g
Gross weight 100g
Table 4 treats xerostomia and oral ulcer, gingivitis, the composite formula of periodontitis
Composition Function Embodiment 6
Two polyglycereol Wetting agent 60g
Water Solvent 32g
Indigo Naturalis Active component 3g
Alumen Active component 1g
Borneolum Syntheticum Active component 1g
Carbomer Thickening agent 2g
Sodium alginate Thickening agent 0.7g
Sodium citrate PH adjusting agent 0.2g
Fructus Citri Limoniae essence Correctives 0.05g
Potassium sorbate Preservative 0.05g
Gross weight 100g
Table 5 treats xerostomia and oral ulcer, gingivitis, the composite formula of periodontitis
Composition Function Embodiment 7
Two polyglycereol Wetting agent 60g
Water Solvent 35g
Tinidazole Active component 1.95g
Mentholum Active component 0.05g
Sodium carboxymethyl cellulose Thickening agent 2g
Carrageenan Thickening agent 0.7g
Sodium citrate PH adjusting agent 0.2g
Steviosin Correctives 0.05g
Ethylparaben Preservative 0.05g
Gross weight 100g
Table 6 treats xerostomia and oral ulcer, gingivitis, the composite formula of periodontitis
Composition Function Embodiment 8
Two polyglycereol Wetting agent 60g
Water Solvent 36g
Erythromycin ethylsuccinate Active component 1g
Sodium carboxymethyl cellulose Thickening agent 2g
Carrageenan Thickening agent 0.7g
Sodium citrate PH adjusting agent 0.2g
Strawberry essence Correctives 0.05g
Ethylparaben Preservative 0.05g
Gross weight 100g
Table 7 treats xerostomia and oral ulcer, gingivitis, the composite formula of periodontitis
Composition Function Embodiment 9
Two polyglycereol Wetting agent 60g
Water Solvent 32g
Ibuprofen Active component 5g
Sodium carboxymethyl cellulose Thickening agent 2g
Carbomer Thickening agent 0.7g
Sodium citrate PH adjusting agent 0.2g
Fructus Citri Limoniae essence Correctives 0.05g
Ethylparaben Preservative 0.05g
Gross weight 100g
The preparation method of the compositions for the treatment of xerostomia and oral ulcer, gingivitis, the periodontitis etc. of the present invention is as follows:
1) each component is weighed by formula;
2) thickening agent is scattered in wetting agent;
3) by soluble in water after remaining component and active component dispersion;
4) again by 2) pour 3 into) in, stir.
Bioadhesive is tested
The pharmaceutical composition of the present invention is gel, belongs to percutaneous drug delivery, needs there is skin certain bioadhesive, treating excess syndrome Execute the gel of example 1 ~ 3, to 3 healthy volunteers, 20 ~ 30 years old age, smear this gel at oral cavity, can during experiment Normal diet, the time that record gel disappears from oral cavity completely.
The experimental record of table 8 volunteer A
Embodiment 1 Embodiment 2 Embodiment 3
Gel extinction time (hour) 5.8 6.5 6.3
The experimental record of table 9 volunteer B
Embodiment 1 Embodiment 2 Embodiment 3
Gel extinction time (hour) 5.9 6.8 6.2
The experimental record of table 10 volunteer C
Embodiment 1 Embodiment 2 Embodiment 3
Gel extinction time (hour) 6 7 6.2
Conclusion: this gel and oral mucosa stick preferably, completely fall off, have for about about 6 hours from oral mucosa Preferably adhesiveness.
Moisture desorption performance is tested
Indication according to this medicine, it should test its moisture desorption performance.
The gel taking a certain amount of embodiment 1 ~ 3 is placed on tared dish, in 20% humidity, deposits 2 hours at 37 DEG C.Just Starting weight amount is moisture desorbing degree divided by the percent of the value that weightlessness change is obtained.The data recorded are as follows:
The moisture desorbing degree of table 11 embodiment 1-3 gel
Sample Moisture desorbing degree
Embodiment 1 7.0%
Embodiment 2 6.9%
Embodiment 3 7.1%
Knowable to data, moisture desorbing degree is more than 6.9%, and the moisture retention of the pharmaceutical composition of the data explanation present invention is good.
Oral mucosa irritation test
According to this product feature, need to its carry out in oral cavity medical apparatus biological assessment oral mucosa irritation test.
With reference to YY/T0127.13-2009 pharmaceuticals industry standard oral cavity mucosa irritation test, use gold healthy, that just grow up Yellow suslik carries out the test of Long Term Contact method, evaluates the irritant reaction of mucous membrane tissue, this product oral cavity with naked eyes and histological observation Mucous membrane tissue reaction is classified as 0, i.e. inorganization irritant reaction.
Internal evaluation test (case study)
With the product of embodiment 1-3,3 xerostomia patients being tested test, concrete outcome is as follows:
3 are suffered from xerostomia women (50 years old, 52 years old, 56 years old) give the gel of embodiment 1 ~ 3, advise its every day At least use 2 times.Experimenter submitted result in about 1 week to, and three experimenters all represent, the most each use 1 time, can be effectively Alleviate dry mouth symptom, make oral cavity keep certain wettability, swallow normal, good mouthfeel, product better tolerance.
This test shows, the pharmaceutical composition of the present invention has the most persistently moisture-retaining capacity, can greatly alleviate mouth Chamber is dried the xerostomia symptom of patient.
With the product of embodiment 4,6,7 to xerostomia the trouble that has complication oral ulcer, angular cheilitis, gingivitis etc. Person is tested, and result is as follows:
The 48 years old women suffering from xerostomia concurrent aphthous ulcer to 1 gives the gel of embodiment 4, advises its every day At least use 2 times.Experimenter submitted result in about 1 week to, and experimenter represents, taste is fine, and after smearing, oral cavity is the most easypro Suitable, without dry mouth symptom, pain relief at ulcer, healing is very fast, product better tolerance.
The 56 years old women suffering from xerostomia concurrent chronic periodontitis to 1 gives the gel of embodiment 6, advises it Every day at least uses 2 times.Experimenter submitted result in about 1 week to, and experimenter represents, product has Chinese medicine odor, taste fragrance, is coated with Smearing rear implication more pure and fresh, moisture retention is the best, normal swallow food, substantially without dry mouth symptom, within 6 hours, smears once, and effect is more Good, periodontitis no longer swells and ache, and is eased, product better tolerance.
The 60 years old women suffering from xerostomia concurrent angular cheilitis and gingivitis to 1 gives the gel of embodiment 7 Agent, advises at least use 2 times its every day.Experimenter submitted result in about 1 week to, except experimenter represent taste do not like with Outward, smearing twice daily, it is ensured that oral cavity moistens, swallows normal, angular cheilitis recovery from illness in three days, and gingivitis is also eased, Product better tolerance.
Data above shows, the pharmaceutical composition of the present invention not only has the most persistently moisture-retaining capacity, can be greatly Alleviate the xerostomia symptom of xerostomic patient, the oral diseases such as oral ulcer, angular cheilitis, periodontitis are had preferably simultaneously Curative effect.
It is only presently preferred embodiments of the present invention in sum, is not used for limiting the practical range of the present invention.The most all The equivalence change made according to the content of scope of the present invention patent and modification, all should be the technology category of the present invention.

Claims (10)

1., for treating a compositions for xerostomia, it comprises: wetting agent, the content of described wetting agent is 60%;Solvent, The content of described solvent is 32 ~ 37%;Thickening agent, the content of described thickening agent is 2 ~ 3%;PH adjusting agent, described pH adjusting agent Content is 0.2%;Essence, the content of described essence is 0.05 ~ 0.5%;Preservative, the content of described preservative is 0.05%.
Compositions the most according to claim 1, wherein, described wetting agent be two polyglycereol, glycerol, propylene glycol, aminoacid, One or more in sorbitol.
Compositions the most according to claim 1, wherein, described thickening agent be sodium carboxymethyl cellulose, gelatin, carbomer, One or more in alginate, carrageenan, described pH adjusting agent is in sodium citrate, sodium hexameta phosphate, potassium citrate One or more.
Compositions the most according to claim 1, wherein, described solvent is water.
Compositions the most according to claim 1, wherein, described essence can be the essence of various taste;Described preservative It can be any pharmaceutically acceptable preservative.
6. according to the compositions described in any one of claim 1 ~ 5, wherein, described compositions can also comprise one or more work Property composition, described in comprise active component pharmaceutical composition possess treatment oral disease effect, always containing of described active component Amount is 2-5%.
Compositions the most according to claim 6, wherein, described active component can be oral disease therapeutic medicine, such as For one or both the combination in benzocaine, triamcinolone acetonide, lignocaine, chlorhexidine, molecular iodine, dexamethasone acetate Thing.
Compositions the most according to claim 6, wherein, described active component can be Antipyretics thing, for example, One in nimesulide, ibuprofen, acetaminophen, diclofenac sodium, diclofenac potassium, indomethacin.
Compositions the most according to claim 6, wherein, described active component can be antibacterials, for example, metronidazole, One in tinidazole, ofloxacin, lomefloxacin, erythromycin ethylsuccinate, pefloxacin mesilate.
Compositions the most according to claim 6, wherein, described active component can be Chinese medicine or Chinese medicine composition, such as For in Indigo Naturalis, Alumen, Borneolum Syntheticum, propolis, Mentholum, Fructus Forsythiae, Herba Taraxaci, Caulis Lonicerae, Spina Gleditsiae, Herba Solidaginis, Flos Lonicerae Kind or multiple pharmaceutical composition.
CN201610258020.8A 2016-04-25 2016-04-25 For treating the composition of xerostomia and mouth disease Active CN105833278B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610258020.8A CN105833278B (en) 2016-04-25 2016-04-25 For treating the composition of xerostomia and mouth disease

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201610258020.8A CN105833278B (en) 2016-04-25 2016-04-25 For treating the composition of xerostomia and mouth disease

Publications (2)

Publication Number Publication Date
CN105833278A true CN105833278A (en) 2016-08-10
CN105833278B CN105833278B (en) 2018-05-08

Family

ID=56588884

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201610258020.8A Active CN105833278B (en) 2016-04-25 2016-04-25 For treating the composition of xerostomia and mouth disease

Country Status (1)

Country Link
CN (1) CN105833278B (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107007503A (en) * 2017-04-26 2017-08-04 烟台新时代健康产业日化有限公司 A kind of bacteria inhibiting composition and its preparation method and application
CN110693834A (en) * 2019-10-24 2020-01-17 大连怡爽口腔医疗科技有限公司 Oral moistening spray
CN112107543A (en) * 2019-06-19 2020-12-22 陕西佰傲再生医学有限公司 Throat spray and its preparation method
CN115192598A (en) * 2022-09-13 2022-10-18 山东百多安医疗器械股份有限公司 A apply ointment or plaster for alleviating angulus oris inflammation

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101396370A (en) * 2007-09-27 2009-04-01 北京天川军威医药技术开发有限公司 Medicine composition for treating mouth, throat disease and preparation method thereof
CN102198126A (en) * 2011-05-04 2011-09-28 刘布鸣 Liniment for treating mouth and tooth diseases and applicator
CN104225246A (en) * 2014-09-12 2014-12-24 皖南医学院 Dental ulcer film agent and preparation method thereof
CN104955447A (en) * 2012-12-18 2015-09-30 日星瑞士股份公司 Topical oral composition for alleviating dry mouth symptoms and for treating mouth ulcers
CN105307645A (en) * 2013-06-03 2016-02-03 麦克内尔股份公司 Solid pharmaceutical dosage form for release of at least one active pharmaceutical ingredient in the oral cavity
CA2970146A1 (en) * 2014-12-10 2016-06-16 Elevate Oral Care, Llc Composition of clathrate and xylitol for the relief of dry mouth

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101396370A (en) * 2007-09-27 2009-04-01 北京天川军威医药技术开发有限公司 Medicine composition for treating mouth, throat disease and preparation method thereof
CN102198126A (en) * 2011-05-04 2011-09-28 刘布鸣 Liniment for treating mouth and tooth diseases and applicator
CN104955447A (en) * 2012-12-18 2015-09-30 日星瑞士股份公司 Topical oral composition for alleviating dry mouth symptoms and for treating mouth ulcers
CN105307645A (en) * 2013-06-03 2016-02-03 麦克内尔股份公司 Solid pharmaceutical dosage form for release of at least one active pharmaceutical ingredient in the oral cavity
CN104225246A (en) * 2014-09-12 2014-12-24 皖南医学院 Dental ulcer film agent and preparation method thereof
CA2970146A1 (en) * 2014-12-10 2016-06-16 Elevate Oral Care, Llc Composition of clathrate and xylitol for the relief of dry mouth

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107007503A (en) * 2017-04-26 2017-08-04 烟台新时代健康产业日化有限公司 A kind of bacteria inhibiting composition and its preparation method and application
CN112107543A (en) * 2019-06-19 2020-12-22 陕西佰傲再生医学有限公司 Throat spray and its preparation method
CN110693834A (en) * 2019-10-24 2020-01-17 大连怡爽口腔医疗科技有限公司 Oral moistening spray
CN115192598A (en) * 2022-09-13 2022-10-18 山东百多安医疗器械股份有限公司 A apply ointment or plaster for alleviating angulus oris inflammation

Also Published As

Publication number Publication date
CN105833278B (en) 2018-05-08

Similar Documents

Publication Publication Date Title
RU2520745C2 (en) Therapeutic composition for treating bronchitis and method for preparing it
EP1395271B1 (en) Herbal compositions for the treatment of mucosal lesions
Moghadamnia et al. The efficacy of the bioadhesive patches containing licorice extract in the management of recurrent aphthous stomatitis
CN102079794A (en) Mucoadhesive xyloglucan-containing formulations useful in medical devices and in pharmaceutical formulations
CN106924378B (en) Chinese herbal medicine lipstick for preventing and/or treating chronic cheilitis
CN102698122B (en) Traditional Chinese medicinal composition for treating paradentitis, and preparation method and administration method thereof and toothpaste
CN105833278A (en) Composition for treating xerostomia and oral diseases
JP2009530350A (en) Spray composition for topical use for the treatment and / or prevention of cold sore infection
US11806376B2 (en) Pharmaceutical composition for treating oral ulcer and preparation method and application thereof
CN102743663B (en) Chinese medicinal preparation for treating urinary infection and preparation method thereof
JP3103373B2 (en) Antivirals derived from Kukuinat skin
CN113842440B (en) A Chinese medicinal composition for treating psoriasis
CN113842405B (en) Application of broussonetia papyrifera root-bark extract in preparation of anti-allergic and itching-relieving medicine for skin
CN116747263B (en) A Chinese medicine composition for treating recurrent oral ulcers, a Chinese medicine preparation and a preparation method thereof
CN114748527B (en) Compound gentian gel for treating eczema and dermatitis in infants and young children
CN110237119A (en) A pharmaceutical composition for treating oral mucosal diseases, its preparation method and application
CN115414410B (en) Gorgon fruit shell extract for improving oral ulcer and its preparation method and application
CN112717030B (en) Pharmaceutical composition for preventing and treating oral diseases and preparation method and application thereof
CN106491857A (en) A kind of treat Chinese medicine preparation of oral ulcer and preparation method thereof
Chandrashekar Comparative study on the efficacy of Topical Curcumin as a gel and as Buccal Mucoadhesive Patch in the management of oral Submucous Fibrosis-A clinicobiochemical evaluation
CN118217357A (en) Traditional Chinese medicine compound for treating sicca syndrome and preparation method and application thereof
CN118045122A (en) A terminalia chebula composition spray for treating chronic pharyngitis and its preparation method
CN100450538C (en) Chinese medicinal formulation for treating apoplexy sequelae
JP2023145935A (en) Takusyato extract preparation
CN114767772A (en) A medicinal composition for treating acne

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
CB02 Change of applicant information
CB02 Change of applicant information

Address after: 102609 Beijing City, Daxing District biological medicine industry base AEON Road No. 26 Hospital of Zhongguancun Medical Park Building No. 16

Applicant after: BEIJING CHIRAL-TECH PHARMACEUTICAL CO., LTD.

Address before: 101111 Beijing City, Daxing District branch of Beijing economic and Technological Development Zone, fourteen Street No. 99 Building No. 7 Room 501

Applicant before: BEIJING CHIRAL-TECH PHARMACEUTICAL CO., LTD.

CB03 Change of inventor or designer information
CB03 Change of inventor or designer information

Inventor after: Liu Suyun

Inventor after: Feng Puchun

Inventor before: Liu Suyun

Inventor before: Feng Puchun

Inventor before: Di Zhong

Inventor before: Huang Qiaoping

TA01 Transfer of patent application right
TA01 Transfer of patent application right

Effective date of registration: 20171009

Address after: 102609 Beijing City, Daxing District biological medicine industry base AEON Road No. 26 Hospital of Zhongguancun Medical Park Building No. 16

Applicant after: Beijing jia'an Medical Technology Co Ltd

Address before: 102609 Beijing City, Daxing District biological medicine industry base AEON Road No. 26 Hospital of Zhongguancun Medical Park Building No. 16

Applicant before: BEIJING CHIRAL-TECH PHARMACEUTICAL CO., LTD.

GR01 Patent grant
GR01 Patent grant
TR01 Transfer of patent right
TR01 Transfer of patent right

Effective date of registration: 20180626

Address after: 102609 301, room 16, building 16, Zhongguancun medical instrument garden, No. 26, Yong Wang Xi Road, Daxing District bio pharmaceutical industrial base, Beijing.

Patentee after: Beijing Rev Medical Instrument Co., Ltd.

Address before: 102609 Beijing Daxing District biomedical industry base No. 26, Zhongguancun medical instrument garden 16, wing Wan West Road.

Patentee before: Beijing jia'an Medical Technology Co Ltd

CP01 Change in the name or title of a patent holder
CP01 Change in the name or title of a patent holder

Address after: 102609 301, room 16, building 16, Zhongguancun medical instrument garden, No. 26, Yong Wang Xi Road, Daxing District bio pharmaceutical industrial base, Beijing.

Patentee after: Beijing Qihui Biomedical Co., Ltd.

Address before: 102609 301, room 16, building 16, Zhongguancun medical instrument garden, No. 26, Yong Wang Xi Road, Daxing District bio pharmaceutical industrial base, Beijing.

Patentee before: Beijing Rev Medical Instrument Co., Ltd.