CN106860476A - A kind of new pharmaceutical preparation Colloidal Bismuth Tartrate particle - Google Patents
A kind of new pharmaceutical preparation Colloidal Bismuth Tartrate particle Download PDFInfo
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- CN106860476A CN106860476A CN201510916110.7A CN201510916110A CN106860476A CN 106860476 A CN106860476 A CN 106860476A CN 201510916110 A CN201510916110 A CN 201510916110A CN 106860476 A CN106860476 A CN 106860476A
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- Prior art keywords
- pharmaceutical preparation
- bismuth tartrate
- colloidal bismuth
- new pharmaceutical
- particle
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/245—Bismuth; Compounds thereof
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of new pharmaceutical preparation Colloidal Bismuth Tartrate particle.Contain the pharmaceutic adjuvants such as cosolvent, antitackiness agent, suspending agent, stabilizer, diluent, adsorbent, glidant, flavouring in the Colloidal Bismuth Tartrate particle.The granule can treat that the course of disease is long, easy recurrence, and have the chronic nonspecific ulcerative colitis disease of cAMP content.It is translucent colloidal solution that the particle dissolves in water; combined with mucous membrane is damaged in intestines and stomach immediately after taking after mixing it with water; form diaphragm; isolation hydrochloric acid in gastric juice; after stimulating mucomembranous epithelial cell secreting mucus medicine to run to enteron aisle simultaneously; the damage of enteron aisle can be resisted, what promotion was damaged intestines (small intestine, colon) mucous membrane itself repairs, and has obvious therapeutic action to chronic colitis, enteritis, intestinal irritable syndrome, chronic Fei Teyi Ulcerative Colitis.
Description
Technical field
This product is related to a kind of be mainly used in one kind that Colloidal Bismuth Tartrate is made as main ingredient with various compound pharmaceutic adjuvants
Treatment colonic diseases, while treating a kind of new pharmaceutical formulation of disease of stomach.Category field of medicaments.
Background technology
It is maximum with gastrointestinal disease accounting in Gastroenterology dept.'s disease, its Small Intestine and colonic diseases in gastrointestinal disease accounting at me
State is in the trend for rising year by year.At present, the pharmaceutical preparation kind for the treatment of disease of stomach, quantity are more both at home and abroad, but treat non-
The medicine of specific intestines problem, no matter bulk drug, preparation, formulation, kind, quantity are little.Generally acknowledging at present can be to non-specific
The effective medicine of Ulcerative Colitis is mainly 5-aminosalicylic acid (5-ASP) and its derivative, such as Liu Dan Huang E pyrroles
Pyridine (SASP) fragrant plant willow nitrogen sodium etc..But greatly, predominantly heating, fash, Nausea and vomiting, granulocyte subtract such poisonous side effect of medicine
It is few, the kind more than ten such as alpastic anemia, spermatozoon reduction, and incidence is up to more than 40%, therefore clinically fail to obtain
Extensive popularization and application.Chronic colonic diseases pathogenesis is also not bery clear and definite at present, relevant etiology, predominantly mental element
Theory, bacterium and viral theory, cause diamine oxidase (DAO) theory of enteron aisle easy damaged.Bulk drug of the invention and its glue
Wafer is on November 23rd, 1996 by State Patent Office's Grant Patent Right for Invention (patent No.；ZL92114664.7, patent certificate
Number：35487, patent inventor and patentee：Yu Xuemin), the preparation method of Colloidal Bismuth Tartrate is which disclose, hereafter
The product has been issued the New Drug Certificate and document of production approval of bulk drug and capsule by the Ministry of Public Health, and the capsule of the product is facing
Wide popularization and application is obtained on bed.In recent years depth has been carried out in the chemical constitution and its pharmacology to its bulk drug, toxicity, clinical efficacy
On the basis of entering research, " a kind of Colloidal Bismuth Tartrate compound and composition and preparation and should be authorized by State Intellectual Property Office
With " patent for invention, (Patent No.：ZL20111016869.5, letters patent book number：1297682, patentee and patent
Inventor：Yu Xuemin).The patent is by infrared spectrum, ultraviolet spectra, mass spectrum and nuclear magnetic resoance spectrum (hydrogen is composed and C13 is composed) test
And parsing, it is determined that its chemical constitution；Patent of invention right claimed its bulk drug and certain formulations chemical constitution and
Its component.Formulation is to realize that drug therapy purpose is specifically formed or object, same Main Ingredients and Appearance, is equipped with a variety of medicinal
Auxiliary material and different preparation methods, are made different formulations, such as tablet, hard capsule, soft capsule, granule, supensoid agent, dissipate
Agent, pill, injection etc..Through research and screening to Colloidal Bismuth Tartrate formulation, a material agent is preferably to embody the medicine
A kind of formulation of curative effect, also is adapted for the medication custom of quite a few patient, and expands therapeutic domain, with capsule, tablet
Compare good with melting, medicine play a role it is fast and lasting, to thering is good protection to make from the whole alimentary canal of oesophagus-rectum
With, with other formulations do not have to oesophagus and stomach, the therapeutic action of enterorrhagia the features such as.Other preparations can be treated can not be controlled
The reflux stomach of the treatment-disease such as esophagitis and gastrointestinal bleeding, the pharmaceutical preparation clinically have preferable popularizing application prospect and
Market potential.
The content of the invention
Colloidal Bismuth Tartrate treatment clinic can be fully demonstrated it is an object of the invention to Colloidal Bismuth Tartrate is made into one
Upper incidence is high, the course of disease is long, easily repeatedly, it is difficult cure, and have the chronic colonic diseases and concurrent disease of stomach of cAMP content, food
Pipe disease safely and effectively pharmaceutical preparation, can meet more extensively the need for granule medication crowd accustomed to using.
A kind of new colloidal bismuth tartrate medicine preparation-Colloidal Bismuth Tartrate particle, it is characterised in that every bag of labelled amount is
165mg (in terms of bismuth), content is the 95%-105% of labelled amount；Translucent glue is dissolved into stirring immediately in hot water (80 DEG C)
Body disperse system, it is oral after be deposited on oesophagus, stomach and the intestinal epithelial cell being damaged, protection mucous membrane makes ulcer and inflammation surface
Repaired, after medicine flows through oesophagus, stomach and small intestine, colon, damage and killing of confrontation diamine oxidase (DAO) to mucous membrane are glued
Gastrointestinal disease pathogenic bacteria-the helicobacter pylori (Hp) of mucous membrane basalis is attached to, promotes the improvement of inflammation and the healing of ulcer, it is right
Anti- Hp causes mucosal atrophy, intestinal metaplasia and canceration.
A kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle, it is characterised in that its primary raw material is the chemical combination of bismuth metal
Thing, is changed into the bismuth salt aqueous solution, then form Colloidal Bismuth Tartrate raw material with winestone acid reaction by the compound of insoluble bismuth first
Medicine, granule is made with the excipient substance such as pectin, sodium alginate, dextrin, chitin, poloxamer, polysaccharide, sugar alcohol.
Its quality standard of Colloidal Bismuth Tartrate particle of the present invention is：Outward appearance is white, odorless, slightly sweet tart flavour
Cylindrical particle, average grain diameter is 1-2mm.PH value is 3.5-5.5, nitrate ＜ 0.3%, sulfate ＜ 0.08%, chloride
＜ 0.01%, lead salt ＜ 0.002%, arsenic ＜ 0.0002%, this product discrimination method is：(1) this product after crushed, is weighed
75mg, add water 100mL, is acidified with dilute sulfuric acid, plus 10% thiourea solution generation buff.(2) this product about 75mg of crushing is weighed,
Plus dilute sulfuric acid 3mL dissolvings, KI test solution is added dropwise, that is, burgundy precipitation is generated, then add excessive KI test solution, precipitate instant
Solution yellowly solution.(3) this product about 0.2g of crushing is taken, add water 2mL, plus sodium carbonate test solution is adjusted to neutrality, ammonification silver nitrate
Test solution few drops, heat in a water bath, occur silver mirror on test tube wall.
The present invention is a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle, is mainly used in treating chronic small intestine and colon
Inflammation, intestinal irritable syndrome, chronic nonspecific ulcerative colitis, can eliminate Mucous Stool, bloody stool, eliminate goblet cell, make intestines
Recover normal function in road；Peptic ulcer, the gastritis caused by helicobacter pylori (Hp) can also be treated simultaneously, moreover it is possible to which treatment is anti-
Fluidity stomach-esophagitis and gastrorrhagia.
Implementation method to illustrate the invention, there is provided following examples and with existing capsule comparative study data, but be not limited to
Prescription composition, preparation method and clinical efficacy that embodiment is provided.
Embodiment 1
Prescription constitutes (ten thousand bags)：Colloidal Bismuth Tartrate bulk drug 1650g, white bole 350g (adsorbent), Bismuth alginate 100g (are helped
Suspension), microcrystalline cellulose 150g (adhesive), magnesium stearate 100g (glidant), 200g starch (diluent).Solids feed powder
Broken, sieving, adds alcohol-water mixed solvent to be made underflow or softwood spray-drying process in right amount or be made softwood, granulation, dry.
Embodiment 2
Prescription constitutes (ten thousand bags)：1650g Colloidal Bismuth Tartrates bulk drug, SCMC100g, CPVP100g.Low-ester pectin 200g, three
Magnesium silicate 200g, hard paraffin 150g, sodium glycine carbonate 100g, sodium cellulose glycolate 150g, pulverize and sieve, and are well mixed.
2% aqueous solution and appropriate amount of ethanol are added, underflow is made, spray-dried granulation or softwood, granulation is made, is dried.Product cut size
＜ 2mm, content (in terms of bismuth) 20.56%, solution time≤1min, sedimentation volumn is than ＞ 98%, specification：165mg/ bags, plastic-aluminum
Packaging material is packed.
Embodiment 3
Drugs compared preparation-Colloidal Bismuth Tartrate capsule, prescription composition (ten thousand bags)：Colloidal Bismuth Tartrate 1650g, starch 825g,
Jelly powder 825g, uniform mixing, sieving, loads hollow capsule and pill or addition water-alcohol mixed solvent is made softwood, granulation, drying, powder
Broken, the hollow capsule and pill of loading.
The embodiment of table 1 and comparative example Performance comparision
Embodiment 1-2 is identical with each dosage of comparative example (165mg)；Times for spraying is different, 1-23 times/d of embodiment, comparative example 4
Secondary/d；Daily dose, the former is below the latter to take number of times.Drug effect plays speed and is significantly faster than that the latter medicines are detained in alimentary canal
Time the former position for being contacted with alimentary canal apparently higher than the latter medicines and therapeutic domain, the former from oesophagus → orifice of the stomach → stomach →
Pylorus → duodenum → small intestine → whole alimentary canal of colon → rectum, the latter is from stomach → pylorus → duodenum → small intestine → knot
Intestines → rectum, the former is substantially better than the latter.The former is effective to esophagitis, disease of stomach, intestines problem, the latter only to stomach and
Intestines problem is effectively, invalid to esophagitis；And the former effective percentage to colonic diseases is significantly better than control formulation capsule.With
Clinically application Colloidal Bismuth Tartrate capsule for many years compares, with obvious novelty, advance and practicality.
Claims (8)
1. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle.
2. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1, can dissolve, shape immediately in the hot water
Into colloidal dispersion, with colloidal stability, standing does not produce precipitation.
3. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1 or 2 and tartro-bismuthate capsule (bit
Nore) compare, fast with melting speed, it is rapid, lasting that drug effect plays a role, and can not only treat disease of stomach, while can treat
Reflux stomach and esophagitis, be particularly suitable for treating the clinically multiple, course for the treatment of it is long, easily repeatedly, difficult doctor and have cAMP content
Chronic nonspecific Ulcerative Colitis.
4. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1-3, is treating chronic colonic diseases side
Face reduced without salicylazosulfapyridine (SASP) and 5-aminosalicylic acid (5-ASP) heating, between fash, Nausea and vomiting, granulocyte,
Aplastic anemia, spermatozoon such as reduce at the toxic and side effect again, and long-term taking do not produce retention toxicosis.
5. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1-4, can be in oesophagus, orifice of the stomach, stomach, deep and remote
Protective effect is produced to mucomembranous epithelial cell at door, small intestine, colon, rectum, promotes the healing of ulcer and the improvement of inflammation, and it is right
The helicobacter pylori (Hp) for sticking to epithelial cell mucous membrane basalis produces strength killing action, promotes healing and the inflammation of ulcer
The improvement of disease, improves healing rate, reduces recurrence rate.
6. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1-5, belongs in oesophagus and gastrointestinal mucosa
Surface (part) plays the medicine of therapeutic action, it is impossible to be absorbed into blood circulation, bioavailability study by gastrointestinal mucosa
Blood-bi concns ＜ ＜ 0-001ppm, the minimum dose 50ppm that may be poisoned away from bismuth ion differs greatly, by drug toxicity classification,
This product belongs to nontoxic pharmaceutical preparation, and clinical test proves that the medicine long-term taking does not produce retention toxicosis.
7. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1-6, contains cosolvent, resists in prescription
The pharmaceutic adjuvants such as glutinous agent, suspending agent, stabilizer, diluent, adsorbent, glidant, flavouring.
8. a kind of new pharmaceutical preparation-Colloidal Bismuth Tartrate particle described in claim 1-7, can use spray-drying process skill
Art is pelletized, it is also possible to which adhesive is made softwood, granulation, furnace drying method preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510916110.7A CN106860476A (en) | 2015-12-14 | 2015-12-14 | A kind of new pharmaceutical preparation Colloidal Bismuth Tartrate particle |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510916110.7A CN106860476A (en) | 2015-12-14 | 2015-12-14 | A kind of new pharmaceutical preparation Colloidal Bismuth Tartrate particle |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106860476A true CN106860476A (en) | 2017-06-20 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201510916110.7A Pending CN106860476A (en) | 2015-12-14 | 2015-12-14 | A kind of new pharmaceutical preparation Colloidal Bismuth Tartrate particle |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108250244A (en) * | 2018-01-19 | 2018-07-06 | 于学敏 | COLLOIDAL BISMUTH TARTRATE-β-macrolide compounds and preparation method thereof, its pharmaceutical composition and their purposes |
| CN111759858A (en) * | 2020-06-02 | 2020-10-13 | 杭州英健生物科技有限公司 | PH-sensitive digestive tract mucosa protective gel and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1088433A (en) * | 1992-12-23 | 1994-06-29 | 于学敏 | Jellied bismuth tartrate medicine |
| CN102276445A (en) * | 2011-06-22 | 2011-12-14 | 于学敏 | Colloidal bismuth tartrate compound, medicaments thereof, preparation method thereof and application thereof |
-
2015
- 2015-12-14 CN CN201510916110.7A patent/CN106860476A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1088433A (en) * | 1992-12-23 | 1994-06-29 | 于学敏 | Jellied bismuth tartrate medicine |
| CN102276445A (en) * | 2011-06-22 | 2011-12-14 | 于学敏 | Colloidal bismuth tartrate compound, medicaments thereof, preparation method thereof and application thereof |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108250244A (en) * | 2018-01-19 | 2018-07-06 | 于学敏 | COLLOIDAL BISMUTH TARTRATE-β-macrolide compounds and preparation method thereof, its pharmaceutical composition and their purposes |
| CN108250244B (en) * | 2018-01-19 | 2020-11-06 | 于学敏 | Bismuth bitartrate-beta-cyclic lactone compound, preparation method thereof, pharmaceutical composition thereof and application thereof |
| CN111759858A (en) * | 2020-06-02 | 2020-10-13 | 杭州英健生物科技有限公司 | PH-sensitive digestive tract mucosa protective gel and application thereof |
| CN111759858B (en) * | 2020-06-02 | 2022-09-20 | 杭州英健生物科技有限公司 | PH-sensitive digestive tract mucosa protective gel and application thereof |
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Application publication date: 20170620 |
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