CN108159059A - A kind of pharmaceutical composition comprising Esomeprazole sodium and preparation method thereof - Google Patents
A kind of pharmaceutical composition comprising Esomeprazole sodium and preparation method thereof Download PDFInfo
- Publication number
- CN108159059A CN108159059A CN201711350969.1A CN201711350969A CN108159059A CN 108159059 A CN108159059 A CN 108159059A CN 201711350969 A CN201711350969 A CN 201711350969A CN 108159059 A CN108159059 A CN 108159059A
- Authority
- CN
- China
- Prior art keywords
- esomeprazole sodium
- pharmaceutical composition
- xylo
- oligosaccharide
- sodium
- 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.)
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Classifications
-
- 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
- A61K31/7016—Disaccharides, e.g. lactose, lactulose
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
-
- 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material 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)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention provides a kind of pharmaceutical compositions comprising Esomeprazole sodium and preparation method thereof, belong to drug field, which includes：Esomeprazole sodium and xylo-oligosaccharide.The pharmaceutical composition can improve the gastrointestinal tracts common adverse reactions such as Nausea and vomiting caused by Esomeprazole sodium.
Description
Technical field
The present invention relates to drug field, in particular to a kind of pharmaceutical composition comprising Esomeprazole sodium and its
Preparation method.
Background technology
Esomeprazole sodium, molecular formula are：C17H18N3NaO3S is the S- optical isomers of Omeprazole, is global first
A isomers proton pump inhibitor (PPI) inhibits parietal cell proton pump to reduce gastric acid secretion by specificity, is treatment digestion
The choice drug of the acid related disorders such as property ulcer, gastroesophageal reflux disease.It is confirmed through a large amount of clinical trials and drug research：It is maintained
PH in stomach>4 time is longer, and acid suppression is more efficient, and curative effect is better than preceding two generations PPI, and individual difference is small.It is existing as PPI of new generation
It is widely used to many acid related disorders of clinical treatment.
For Esomeprazole sodium relative to the drug of other pipe intestinal digesting diseases, good effect, toxic side effect are light.Patient is main
Adverse reaction is abnormal for gastrointestinal tract, such as Nausea and vomiting, accidental diarrhea, dry.
Invention content
The first object of the present invention is to provide a kind of pharmaceutical composition for including Esomeprazole sodium, the pharmaceutical composition
The gastrointestinal tracts common adverse reactions such as Nausea and vomiting caused by Esomeprazole sodium can effectively be improved by xylo-oligosaccharide.
The second object of the present invention is to provide a kind of preparation method of aforementioned pharmaceutical compositions, this method preparation process letter
It is single, it is suitble to industrialized production.
The third object of the present invention is to provide a kind of gastrointestinal tract pair of xylo-oligosaccharide preparing improvement Esomeprazole sodium
Purposes in the drug of reaction.Xylo-oligosaccharide has alleviate Esomeprazole sodium caused by the side effects such as Nausea and vomiting, by its with
Chemical drug is applied in combination, and can significantly improve the gastrointestinal side effect of chemical drug.
In order to realize the above-mentioned purpose of the present invention, spy uses following technical scheme：
A kind of pharmaceutical composition for including Esomeprazole sodium, pharmaceutical composition include：Esomeprazole sodium and oligomeric wood
Sugar.
A kind of preparation method of the pharmaceutical composition comprising Esomeprazole sodium, including：
Water after the Esomeprazole sodium, the xylo-oligosaccharide are mixed with adhesive, partial disintegration agent with thickener
Solution mixes, dry after wet granulation, obtains the dry particl that grain size is 16~25 mesh；
After the dry particl is mixed with glidant, lubricant and remaining disintegrant, tabletting.
Compared with prior art, beneficial effects of the present invention for example including：
In this pharmaceutical composition provided by the invention and preparation method thereof, using Esomeprazole sodium as main pharmacodynamics into
Point, it can effectively treat by acid related disorders such as peptic ulcer, gastroesophageal reflux disease；Meanwhile it is added in its formula oligomeric
Xylose, alimentary canal side reaction caused by being effectively improved Esomeprazole sodium improve the compliance of patient, to going out in therapeutic process
Existing nausea and vomiting, loss of appetite have good remission effect.
Specific embodiment
Embodiment of the present invention is described in detail below in conjunction with embodiment, but those skilled in the art will
Understand, the following example is merely to illustrate the present invention, and is not construed as limiting the scope of the invention.It is not specified in embodiment specific
Condition person, the condition suggested according to normal condition or manufacturer carry out.Reagents or instruments used without specified manufacturer is
The conventional products that can be obtained by commercially available purchase.
Present embodiment provides a kind of pharmaceutical composition for including Esomeprazole sodium, which includes：Esso
Azoles sodium and xylo-oligosaccharide draw in U.S..
Wherein, Esomeprazole sodium, molecular formula are C17H18N3NaO3S is a kind of isomers proton pump inhibitor, to digestion
The acid related disorders such as property ulcer, gastroesophageal reflux disease have the effect of good.
Xylo-oligosaccharide, also known as wood oligose are the functional polyalkylenes being combined by 2-7 xylose molecule with β-Isosorbide-5-Nitrae glycosidic bond
Sugar is closed, relative molecular mass is 300~2000.Due to the enzyme for not having to hydrolyze xylo-oligosaccharide in human gastrointestinal tract, so it can
It is preferably that Bifidobacterium utilizes to be directly entered big enteral, promotes the breeding of Bifidobacterium and that it is made to generate simultaneously is a variety of organic
Acid, and then promote gastrointestinal motility.Xylo-oligosaccharide can activate or promote body cell and the immune function of body fluid, be conducive to body
From the invasion and damage of the bacteria microorganism that causes a disease.Beneficial bacterium also has superoxide dismutase (SOD), peroxide in activation body cell
Change the effect of hydrogen enzyme and glutathione peroxidase, polyphenoils is promoted to generate, reduces the damage of free radical.Xylo-oligosaccharide exists
It also has certain effect in activation immune response.In the present invention, inventor is the study found that xylo-oligosaccharide can be reduced by Esso
The digestive tract reaction caused by azoles sodium draws in U.S., improves the compliance of patient, to occur in therapeutic process nausea and vomiting, loss of appetite
With good result.
Further, the pharmaceutical composition count in parts by weight including：Esomeprazole sodium is 2 parts, xylo-oligosaccharide 30
~150 parts.
Further, it counts in parts by weight, xylo-oligosaccharide is 80~100 parts and is either 85~95 parts or is 87~93
Part is 90 parts.Inventor's experimental study shows the content when xylo-oligosaccharide in the range of 10~90 parts, the pharmaceutical composition
Object has stronger preventing or arresting vomiting ability.
Further, pharmaceutical composition further includes pharmaceutically acceptable auxiliary material.
Herein, it is physiologically acceptable that term " pharmaceutically acceptable ", which refers to the compound when compound is to human administration,
, and the allergic reactions such as gastrointestinal disturbance, dizziness or these similar anaphylactoid systemic anaphylaxis will not occur.
In order to make the medical composition rapidly, continuously and the discharge active component in a very long time, doctor of the invention
Drug composition can be manufactured according to those conventional methods in the art are disclosed in.The administration of the medical composition of the present invention
Approach is injection, intravenous drip, oral, nasal inhalation or parenteral administration.The preparation of the medical composition can be injection,
Freeze-dried powder, powder, particle, tablet, emulsion, syrup, aerosol, soft capsule and hard shell capsules etc..It is more preferred, the drug
The dosage form of composition includes injection, freeze-dried powder, tablet, capsule or granule.
Present embodiment also provides a kind of preparation method of aforementioned pharmaceutical compositions, with reference to embodiments to the present invention's
Feature and performance are described in further detail：
Embodiment 1
The present embodiment provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：
Esomeprazole sodium 20g, xylo-oligosaccharide 300.03g.
Embodiment 2
The present embodiment provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：Esomeprazole sodium 20g,
Xylo-oligosaccharide 800.24g.
Embodiment 3
The present embodiment provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：Esomeprazole sodium 20g,
Xylo-oligosaccharide 1500.11g.
Embodiment 4
The present embodiment provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：Esomeprazole sodium 20g,
Xylo-oligosaccharide 1000.14g.
Comparative example 1
This comparative example provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：Esomeprazole sodium 20g.
Comparative example 2
This comparative example provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：Esomeprazole sodium 20g,
Starch 300.01g.
Comparative example 3
This comparative example provides a kind of pharmaceutical composition for including Esomeprazole sodium.
Comparative example 4
This comparative example provides a kind of pharmaceutical composition for including Esomeprazole sodium, including：Esomeprazole sodium 20g,
Starch 1500.27g.
Experimental example
The pharmaceutical composition provided with reference to animal experiment the embodiment of the present invention 1~3 and comparative example 1~4 is improving
Effect in terms of the digestive tract reaction caused by the Esomeprazole sodium is evaluated.
One, test methods：
The pigeon 84 of weight 200-300g is chosen, half male and half female is randomly divided into 7 groups, every group 12.Fasting is not before experiment
Prohibit water for 24 hours, pigeon administration each composition of gavage (Examples 1 to 3, comparative example 1~4, composition such as 1 institute of table of effective component
Show), it is 2mg/ to convert into Esomeprazole sodium, and the vomiting number and number of elements of pigeon in 5h are recorded after administration, and experimental result carries out
Comparison among groups are shown in Table 2：
Effective component forms in 1. Examples 1 to 3 of table and comparative example 1~4
| Esomeprazole sodium | Xylo-oligosaccharide | Starch | |
| Embodiment 1 | 20 | 300.03 | - |
| Embodiment 2 | 20 | 800.24 | - |
| Embodiment 3 | 20 | 1500.11 | - |
| Comparative example 1 | 20 | - | - |
| Comparative example 2 | 20 | - | 300.01 |
| Comparative example 3 | 20 | - | 800.39 |
| Comparative example 4 | 20 | - | 1500.27 |
2. pigeon of table vomits situation
By 2 result of table as it can be seen that Examples 1 to 3 group pigeon vomiting number of elements and average vomiting number are considerably less than other each groups.
By above-mentioned animal experiment, pharmaceutical composition according to the present invention can promote gastroenteritic power, promote food digestion
And absorption, there is preventing or arresting vomiting effect, the alimentary canal side reaction that can be effectively improved caused by Esomeprazole sodium improves patient's chemicotherapy
Compliance has good result to nausea and vomiting, loss of appetite
Although illustrate and describing the present invention with specific embodiment, it will be appreciated that without departing substantially from the present invention's
Many other change and modification can be made in the case of spirit and scope.It is, therefore, intended that in the following claims
Including belonging to all such changes and modifications in the scope of the invention.
Claims (5)
1. a kind of pharmaceutical composition for including Esomeprazole sodium, which is characterized in that described pharmaceutical composition includes：Esso U.S. draws
Azoles sodium and xylo-oligosaccharide.
2. pharmaceutical composition according to claim 1, which is characterized in that count in parts by weight, the Esomeprazole sodium 2
Part, the xylo-oligosaccharide are 30~150 parts.
3. pharmaceutical composition according to claim 2, which is characterized in that count in parts by weight, the xylo-oligosaccharide is 80
~100 parts.
4. pharmaceutical composition according to claim 2, which is characterized in that described pharmaceutical composition, which further includes, can pharmaceutically connect
The auxiliary material received.
5. a kind of purposes of xylo-oligosaccharide in the drug for preparing the gastrointestinal side effect for improving Esomeprazole sodium.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711350969.1A CN108159059A (en) | 2017-12-15 | 2017-12-15 | A kind of pharmaceutical composition comprising Esomeprazole sodium and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711350969.1A CN108159059A (en) | 2017-12-15 | 2017-12-15 | A kind of pharmaceutical composition comprising Esomeprazole sodium and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108159059A true CN108159059A (en) | 2018-06-15 |
Family
ID=62522382
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711350969.1A Pending CN108159059A (en) | 2017-12-15 | 2017-12-15 | A kind of pharmaceutical composition comprising Esomeprazole sodium and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN108159059A (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020045646A1 (en) * | 1996-01-04 | 2002-04-18 | Phillips Jeffrey O. | Novel substituted benzimidazole dosage forms and method of using same |
| CN103520203A (en) * | 2012-07-02 | 2014-01-22 | 舒泰神（北京）生物制药股份有限公司 | Pharmaceutical composition for facilitating feces excretion and clearing bowels |
| CN104602671A (en) * | 2012-08-30 | 2015-05-06 | 亚历山大·弗拉基米罗维奇·季科夫斯基 | Pharmaceutical composition for treating gastro-oesophageal reflux disease |
| US20160136194A1 (en) * | 2009-03-30 | 2016-05-19 | Alexander Vladimirovich Dikovskiy | Pharmaceutical composition comprising a proton pump inhibitor and a prebiotic for the treatment of ulcerous lesions of the stomach and duodenum |
-
2017
- 2017-12-15 CN CN201711350969.1A patent/CN108159059A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020045646A1 (en) * | 1996-01-04 | 2002-04-18 | Phillips Jeffrey O. | Novel substituted benzimidazole dosage forms and method of using same |
| US20160136194A1 (en) * | 2009-03-30 | 2016-05-19 | Alexander Vladimirovich Dikovskiy | Pharmaceutical composition comprising a proton pump inhibitor and a prebiotic for the treatment of ulcerous lesions of the stomach and duodenum |
| CN103520203A (en) * | 2012-07-02 | 2014-01-22 | 舒泰神（北京）生物制药股份有限公司 | Pharmaceutical composition for facilitating feces excretion and clearing bowels |
| CN104602671A (en) * | 2012-08-30 | 2015-05-06 | 亚历山大·弗拉基米罗维奇·季科夫斯基 | Pharmaceutical composition for treating gastro-oesophageal reflux disease |
Non-Patent Citations (1)
| Title |
|---|
| 徐弘君 等: "低聚木糖在慢性肝炎伴肠道功能紊乱中的应用", 《中国中西医结合消化杂志》 * |
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| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
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| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180615 |