CN106474122A - A kind of pharmaceutical composition of amoxicillin and clavulanate potassium and its application - Google Patents
A kind of pharmaceutical composition of amoxicillin and clavulanate potassium and its application Download PDFInfo
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- CN106474122A CN106474122A CN201610805861.6A CN201610805861A CN106474122A CN 106474122 A CN106474122 A CN 106474122A CN 201610805861 A CN201610805861 A CN 201610805861A CN 106474122 A CN106474122 A CN 106474122A
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- Prior art keywords
- pharmaceutical composition
- asthma
- amoxicillin
- composition according
- clavulanate potassium
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a kind of pharmaceutical composition, in pharmaceutical composition, the ratio of two kinds of active components amoxicillin and clavulanate potassium is 7：1.The pharmaceutical composition of the present invention can significantly mitigate the rising of the IgE level of allergen-induced, can be used for preventing or treat asthma, the asthma causing especially for air pollutions such as hazes, and asthma merges bacterium infection and has good effect.
Description
Technical field
The present invention relates to the pharmaceutical composition of a kind of amoxicillin and clavulanate potassium and its application, belong to field of medicaments.
Background technology
In recent years, with the raising of industrialized level, the problem of ecological deterioration and air pollution increasingly highlights.Substantial amounts of dirt
Dye thing and particulate matter suspend in the air, lead to air quality and On The Deterioration of Visibility Over, haze weather in national multiple cities, and have goes back
Continue more than one week.The wherein particulate matter less than or equal to 2.5 microns for the diameter is referred to as PM2.5, and it is suspended in air, through breathing
Directly pulmonary can be entered by air flue after entering human body.The poisonous and harmful substances such as sulfate and nitrate are contained, in addition in PM2.5
The also pathogenic microorganism such as portability virus and antibacterial.
The direct harm of air pollution shows as causing respiratory system disease.As commonly encountered diseases frequently-occurring disease asthma then more
Prominent.It is reported that, in haze weather, the sickness rate of childhood asthma rises more than one times（Rise to 7% from 3%）.How to protect people
The impact that body respiratory system brings from air pollution is most important.
Asthma is a kind of inflammatory allergic disease, is embodied in breathing heavily caused by airway hyperreactivity and airway obstruction
The symptoms such as breath, tachypnea, uncomfortable in chest, cough.Extraneous sensitinogen including PM2.5 is the direct inducement of asthma attack.Existing grind
Study carefully and have been found that IgE（IgE）The anaphylaxiss of mediation have highly important work in the pathogenic process of asthma
With.Sensitinogen enters induction B cell secretion IgE after human body.IgE then promotes the inflammatories such as histamine, leukotriene, prostaglandin further
A large amount of releases of medium, the reaction such as cause mucous secretion, airway smooth muscle contraction, vascular permeability to increase.In addition, IgE also may be used
Promote extracellular matrix protein increase to lead to Airway Remodeling, and participate in the asthma in acute attack process of antibacterial and virus induction.
The medicine of clinical treatment asthma is mainly corticosteroidss medicine, bronchiectasis medicine, leukotriene suppression at present
Preparation etc., but exist expensive, large side effects, action time short the shortcomings of.It is thus desirable to finding new anti-asthmatic medicament.
Content of the invention
It is an object of the invention to provide the pharmaceutical composition of a kind of prevention or treatment asthma, provide new medicine for this disease
Select.
Amoxicillin is a kind of penicillins antimicrobial drug, and clavulanate potassium is beta lactamase restrainer.Both compound recipe systems
Agent has been used for treating bacterial urinary tract infection, respiratory system infection, skin infection, ear nose infection etc., has and preferably faces
Bed curative effect.But, also not with regard to its prevention or the report treating asthma.
We pass through research and are surprised to find that the pharmaceutical composition of amoxicillin and clavulanate potassium can reduce anaphylactogen induction
IgE release, can effectively prevent or treat asthma, thus having obtained the present invention.
First,
The invention provides a kind of active component is the pharmaceutical composition of amoxicillin and clavulanate potassium, it is characterized in that, described
Pharmaceutical composition is used for preventing or treating asthma, and the weight of active component amoxicillin and clavulanate potassium is than with A Moxi
Woods anhydride and clavulanic acid are calculated as 7:1.
As the optimal way of the present invention, described amoxicillin is Utimox.
As the optimal way of the present invention, described pharmaceutical composition is oral formulations.Specific form can have multiple, example
As ordinary tablet, dispersible tablet, chewable tablet, dry suspension, granule, capsule etc..When dosage form is for ordinary tablet, further preferably often
Piece contains the amount of amoxicillin, is calculated as 0.875g with anhydride.
As the optimal way of the present invention, pharmaceutically useful adjuvant in described pharmaceutical composition, can also be contained.
One or more of disintegrating agent, lubricant, binding agent, dispersant for example can be contained in tablet.Further preferably
Ground, contains Microcrystalline Cellulose, silicon dioxide, carboxymethyl starch sodium and magnesium stearate in described pharmaceutical composition.Pharmaceutical composition
Preparation, can adopt this area conventional method.For example when preparing ordinary tablet, in view of the chemical stability of clavulanate potassium is relatively
Difference, can take direct compression process, will be pressed into bulk, then be ground into granule after each component mixing（I.e. dry granulation）After carry out
Tabletting.Carry out tabletting after can selecting whole components are pelletized；With residue after can also selecting a portion component is pelletized
Component mixed pressuring plate.As by active component, mixed with disintegrating agent, lubricant, binding agent, dispersant, tabletting.Or, will
Active component mix with binding agent and disintegrating agent after dry granulation, then mixed with lubricant, dispersant, tabletting.In addition, also
Using method commonly used in the art, tablet can be coated.
One or more of dispersant, suspending agent, lubricant, correctivess, stabilizer for example can be contained in dry suspension.
It is further preferred that containing sodium carboxymethyl cellulose, silicon dioxide, xanthan gum, aspartame in described pharmaceutical composition.Medicine
The preparation of compositionss, can adopt the conventional method of this area.For example when preparing dry suspension, active component is mixed with adjuvant
Uniformly, you can.
As the optimal way of the present invention, described asthma is the asthma that air pollution causes.It may further be preferable that it is described
Asthma is the asthma that haze causes.Still further preferably, described asthma is the asthma that PM2.5 causes.
As the optimal way of the present invention, described asthma is IgE mediation.
As the optimal way of the present invention, described asthma is the asthma being associated with bacterium infection.
Secondly,
Present invention also offers a kind of compound, it is characterized in that, remove above-mentioned containing the present invention in described compound
Outside pharmaceutical composition, also contain other anti-asthmatic medicaments.
As the optimal way of the present invention, described others anti-asthmatic medicament can be to be used for having been used in prior art
Antasthmatic any medicine.For example, hormone medicine, bronchiectasis class medicine, leukotriene inhibitors etc..As propanoic acid fluorine replaces card
Pine, aminophylline, formoterol, montelukast, albuterol etc..
Finally,
The invention provides the two of pharmaceutical composition kinds of application modes：
One：Active component is used for preparation prevention or the medicine for the treatment of asthma for the pharmaceutical composition of amoxicillin and clavulanate potassium
Application in thing, in described pharmaceutical composition, the weight of active component is calculated as 7 than with amoxicillin anhydride and clavulanic acid:
1.
In view of the pharmaceutical composition of amoxicillin and clavulanate potassium itself can prevent or treat bacterium infection, therefore right
Merge the situation of bacterium infection in asthma it is also possible to being prevented or treating.
It two：Active component is used for preparation prevention or treatment asthma for the pharmaceutical composition of amoxicillin and clavulanate potassium
Merge the application in the medicine of bacterium infection, in described pharmaceutical composition the weight of active component than with amoxicillin anhydride and
Clavulanic acid is calculated as 7:1.
In the application mode that the present invention mentions, the technical characteristic such as asthma, pharmaceutical composition can adopt and carry above
The optimal way arriving.
The invention has the beneficial effects as follows：
It is found by experiment that, the pharmaceutical composition of the present invention can significantly inhibit the liter of the experimental rat model of asthma SERUM IgE of PM2.5 induction
Height, in addition, when the ratio of active component is 7：There is when 1 best inhibition.
Inventor is found that the compound medicine of amoxicillin and clavulanate potassium has antianaphylactic effect first, for clinically
Prevention or treatment asthma provide a kind of new medicament selection, also extend the range of application of existing medicine.
Specific embodiment：
For the object, technical solutions and advantages of the present invention are better described, below in conjunction with specific embodiment and test example to this
Invention is described further.
Embodiment 1：Pharmaceutical composition（Amoxicillin and Clavulanate Potassium Tablets 7：1）
Prescription：Utimox 1004.3g, clavulanate potassium 149.5g, Microcrystalline Cellulose 149.6g, silicon dioxide
25.2g, carboxymethyl starch sodium 30.3g and magnesium stearate 3.5g.
Preparation method：Take Utimox, clavulanate potassium, silicon dioxide and carboxymethyl starch sodium, mixing is all
After even, it is pressed into bulk, be ground into granule.Granule is mixed homogeneously with Microcrystalline Cellulose and magnesium stearate, tabletting, make 1000
Piece.
Embodiment 2：Pharmaceutical composition（Amoxicillin and Clavulanate Potassium Tablets 2：1）
Prescription：Utimox 459.1g, clavulanate potassium 239.3g, Microcrystalline Cellulose 91.4g, silicon dioxide
14.8g, carboxymethyl starch sodium 20.3g and magnesium stearate 2.0g.
Preparation method：Using method same as Example 1, make 1000.
Embodiment 3：Pharmaceutical composition（Amoxicillin and Clavulanate Potassium Tablets 10：1）
Prescription：Utimox 1147.8g, clavulanate potassium 119.6g, Microcrystalline Cellulose 132.7g, silicon dioxide
20.4g, carboxymethyl starch sodium 34.5g and magnesium stearate 4.1g.
Preparation method：Using method same as Example 1, make 1000.
Embodiment 4：Pharmaceutical composition（Amoxicillin and Clavulanate Potassium for Oral Suspension）
Prescription and preparation method：With the Utimox in embodiment 1 and clavulanate potassium as active component（Two kinds of work
Property component ratio be 7：1）, adjuvant is from sodium carboxymethyl cellulose, xanthan gum, aspartame, silicon dioxide.Preparation method：Adopt
With the conventional method of dry suspension, active component and adjuvant are pulverized, mix homogeneously, obtain final product.
Embodiment 5：The experimental rat model of asthma SERUM IgE water that the pharmaceutical composition of amoxicillin and clavulanate potassium induces to PM2.5
Flat impact
Trial drug：The amoxicillin and clavulanate potassium pharmaceutical composition of preparation in embodiment 1-3.
Test method：
Wister rat, average weight is 190g.It is randomly divided into normal group（Do not suck PM2.5）, negative control group（Not using examination
Test medicine）、7：1 medicine group（Using the pharmaceutical composition in embodiment 1）、2：1 medicine group（Using the medicine group in embodiment 2
Compound）、10：1 medicine group（Using the pharmaceutical composition in embodiment 3）, every group of 10 animals, male and female half and half.
Gather the PM2.5 granule of densely populated place in the air in haze sky, be prepared into the suspension containing PM2.5 with normal saline
Liquid, makes rat Neulized inhalation suspension contaminate, and inhalation dose is 0.8mg/kg.Each group animal uses trial drug in first 7 days in contamination
Carry out gavage, continue to contamination the 3rd day.Once, dosage is calculated as 5mg/kg, normal group and feminine gender by amoxicillin to daily gavage
The normal saline of daily gavage 5mg/kg of matched group.
The 3rd day after animal contaminated, take animal's whole blood, separate serum, measure the level of total IgE in serum, main result is shown in
Shown in table 1.
The impact of the experimental rat model of asthma serum IgE level that table 1 pharmaceutical composition of the present invention induces to PM2.5
| Group | Size of animal | IgE（IU/ml） |
| Normal group | 10 | 7.261±1.324 |
| Negative control group | 10 | 32.153±4.272 |
| 7：1 medicine group | 10 | 12.665±2.831 |
| 2：1 medicine group | 10 | 23.901±3.742 |
| 10：1 medicine group | 10 | 20.862±3.115 |
Result of the test shows：PM2.5 can induce the significantly raised of rat blood serum IgE level.Pharmaceutical composition in the present invention can
Effectively suppress the rising of IgE level, in addition, when the ratio of amoxicillin and clavulanic acid is 7:Best effect can be produced when 1.
In view of key effect in asthma for the IgE, the compositionss of the present invention can effectively be prevented or be treated asthma.Can individually make
With it is also possible to be used in combination with clinically other anti-asthmatic medicaments existing or make compound preparation for prevention or treatment heavy breathing
Breathe heavily.
Claims (10)
1. a kind of active component is the pharmaceutical composition of amoxicillin and clavulanate potassium, it is characterized in that, described pharmaceutical composition
For preventing or treating asthma, and the weight of active component is calculated as 7 than with amoxicillin anhydride and clavulanic acid:1.
2. pharmaceutical composition according to claim 1, is characterized in that, described amoxicillin is hydrated for amoxicillin three
Thing.
3. pharmaceutical composition according to claim 1, is characterized in that, described pharmaceutical composition is oral formulations.
4. pharmaceutical composition according to claim 1, is characterized in that, described pharmaceutical composition be conventional tablet, dispersible tablet,
Chewable tablet, dry suspension, granule, capsule.
5. pharmaceutical composition according to claim 4, is characterized in that, described pharmaceutical composition is conventional tablet, and every contains
There is the amount of amoxicillin, 0.875g is calculated as with anhydride.
6. pharmaceutical composition according to claim 1, is characterized in that, described asthma is that air pollution causes.
7. pharmaceutical composition according to claim 1, is characterized in that, described asthma mediates for IgE.
8. pharmaceutical composition according to claim 1, is characterized in that, described asthma is the asthma being associated with bacterium infection.
9. a kind of compound, is characterized in that, containing described pharmaceutical composition arbitrary in claim 1-8, also contains it
His anti-asthmatic medicament.
10. the compound described in claim 9, is characterized in that, other described anti-asthmatic medicaments are corticosteroidss medicine
Thing, bronchiectasis medicine or leukotriene inhibitors.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610805861.6A CN106474122B (en) | 2016-09-07 | 2016-09-07 | Pharmaceutical composition of amoxicillin and clavulanate potassium and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610805861.6A CN106474122B (en) | 2016-09-07 | 2016-09-07 | Pharmaceutical composition of amoxicillin and clavulanate potassium and application thereof |
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| Publication Number | Publication Date |
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| CN106474122A true CN106474122A (en) | 2017-03-08 |
| CN106474122B CN106474122B (en) | 2020-04-14 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111377947A (en) * | 2018-12-29 | 2020-07-07 | 江苏先声药业有限公司 | Amoxicillin trihydrate pharmaceutical composition with low water activity and preparation method thereof |
Citations (4)
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| CN1189100A (en) * | 1995-05-03 | 1998-07-29 | 史密丝克莱恩比彻姆有限公司 | Composition comprising amoxycillin and clavulanic acid |
| CN101129359A (en) * | 2007-07-12 | 2008-02-27 | 颜锵 | Pharmaceutical composition containing amoxicillin, ambroxol and beta lactamase restrainer and uses thereof |
| CN102058587A (en) * | 2009-11-13 | 2011-05-18 | 天津金世制药有限公司 | Solid preparation for treating asthma |
| CN104208060A (en) * | 2013-05-29 | 2014-12-17 | 天津金耀集团有限公司 | Compound inhalation preparation containing penicillin antibiotic |
-
2016
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1189100A (en) * | 1995-05-03 | 1998-07-29 | 史密丝克莱恩比彻姆有限公司 | Composition comprising amoxycillin and clavulanic acid |
| CN101129359A (en) * | 2007-07-12 | 2008-02-27 | 颜锵 | Pharmaceutical composition containing amoxicillin, ambroxol and beta lactamase restrainer and uses thereof |
| CN102058587A (en) * | 2009-11-13 | 2011-05-18 | 天津金世制药有限公司 | Solid preparation for treating asthma |
| CN104208060A (en) * | 2013-05-29 | 2014-12-17 | 天津金耀集团有限公司 | Compound inhalation preparation containing penicillin antibiotic |
Non-Patent Citations (4)
| Title |
|---|
| ANA VIANA-TEJEDOR等: "Kounis syndrome secondary to amoxicillin use in an asthmatic patient", 《INTERNATIONAL JOURNAL OF CARDIOLOGY》 * |
| 国家药典委员会: "《中华人民共和国药典》", 30 June 2015 * |
| 宁碧雯: "阿莫西林克拉维酸钾与哌拉西林舒巴坦钠联合阿奇霉素对小儿支原体肺炎的临床疗效", 《深圳中西医结合杂志》 * |
| 张蔓莉 等: "儿童肺炎支原体感染与IgE水平的相关性研究", 《中国妇幼保健》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111377947A (en) * | 2018-12-29 | 2020-07-07 | 江苏先声药业有限公司 | Amoxicillin trihydrate pharmaceutical composition with low water activity and preparation method thereof |
| CN111377947B (en) * | 2018-12-29 | 2022-10-21 | 江苏先声药业有限公司 | Amoxicillin trihydrate pharmaceutical composition with low water activity and preparation method thereof |
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Effective date of registration: 20180408 Address after: 410331 Liuyang Dong Yang Township (Hunan pharmaceutical Park) Applicant after: Xiangbei Welman Pharmaceutical Co., Ltd. Applicant after: Nanjing star Fuxing Pharmaceutical Technology Co., Ltd. Address before: 410331 Liuyang, Hunan, Yang Yang hole (Biomedical Park) Applicant before: Xiangbei Welman Pharmaceutical Co., Ltd. |
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