CN103040816A - Drug composition for curing peptic ulcer - Google Patents
Drug composition for curing peptic ulcer Download PDFInfo
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- CN103040816A CN103040816A CN2012105926587A CN201210592658A CN103040816A CN 103040816 A CN103040816 A CN 103040816A CN 2012105926587 A CN2012105926587 A CN 2012105926587A CN 201210592658 A CN201210592658 A CN 201210592658A CN 103040816 A CN103040816 A CN 103040816A
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- China
- Prior art keywords
- vitamin
- aldioxa
- acetate
- ulcer
- peptic ulcer
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 37
- 208000008469 Peptic Ulcer Diseases 0.000 title claims abstract description 18
- 208000011906 peptic ulcer disease Diseases 0.000 title claims abstract description 18
- 239000003814 drug Substances 0.000 title abstract description 17
- 229940079593 drug Drugs 0.000 title abstract description 9
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims abstract description 36
- AMZWNNKNOQSBOP-UHFFFAOYSA-M [n'-(2,5-dioxoimidazolidin-4-yl)carbamimidoyl]oxyaluminum;dihydrate Chemical compound O.O.NC(=O)NC1N=C(O[Al])NC1=O AMZWNNKNOQSBOP-UHFFFAOYSA-M 0.000 claims abstract description 28
- 229940015825 aldioxa Drugs 0.000 claims abstract description 26
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 claims abstract description 22
- ZAKOWWREFLAJOT-UHFFFAOYSA-N d-alpha-Tocopheryl acetate Natural products CC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-UHFFFAOYSA-N 0.000 claims abstract description 22
- 229940042585 tocopherol acetate Drugs 0.000 claims abstract description 22
- 239000000377 silicon dioxide Substances 0.000 claims abstract description 18
- 238000002360 preparation method Methods 0.000 claims abstract description 6
- 235000012239 silicon dioxide Nutrition 0.000 claims description 17
- 239000008187 granular material Substances 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 239000002775 capsule Substances 0.000 claims description 5
- 238000012856 packing Methods 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 239000006186 oral dosage form Substances 0.000 claims 1
- 229960001866 silicon dioxide Drugs 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 abstract description 16
- 231100000397 ulcer Toxicity 0.000 abstract description 16
- 210000004877 mucosa Anatomy 0.000 abstract description 11
- 239000007787 solid Substances 0.000 abstract description 4
- 230000002195 synergetic effect Effects 0.000 abstract description 3
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- 229930003427 Vitamin E Natural products 0.000 description 16
- 230000000694 effects Effects 0.000 description 16
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 16
- 229940046009 vitamin E Drugs 0.000 description 16
- 239000011709 vitamin E Substances 0.000 description 16
- 235000019165 vitamin E Nutrition 0.000 description 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 230000035876 healing Effects 0.000 description 7
- 208000007107 Stomach Ulcer Diseases 0.000 description 6
- 201000005917 gastric ulcer Diseases 0.000 description 6
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- 229930003231 vitamin Natural products 0.000 description 3
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- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 206010063560 Excessive granulation tissue Diseases 0.000 description 2
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
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- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 2
- 229910021502 aluminium hydroxide Inorganic materials 0.000 description 2
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- 101150056637 Hrh2 gene Proteins 0.000 description 1
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 description 1
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- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 description 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 description 1
- 206010067171 Regurgitation Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
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- 229960000458 allantoin Drugs 0.000 description 1
- 229960003022 amoxicillin Drugs 0.000 description 1
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 description 1
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- 230000000767 anti-ulcer Effects 0.000 description 1
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- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 description 1
- 230000002183 duodenal effect Effects 0.000 description 1
- 208000000718 duodenal ulcer Diseases 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
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- 239000003925 fat Substances 0.000 description 1
- 238000011010 flushing procedure Methods 0.000 description 1
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 description 1
- 230000030136 gastric emptying Effects 0.000 description 1
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- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
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- FXJAOWANXXJWGJ-UHFFFAOYSA-N n-[4-(2-methyl-1h-imidazol-5-yl)phenyl]-n'-propan-2-ylmethanimidamide Chemical compound C1=CC(NC=NC(C)C)=CC=C1C1=CN=C(C)N1 FXJAOWANXXJWGJ-UHFFFAOYSA-N 0.000 description 1
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- MNQYNQBOVCBZIQ-JQOFMKNESA-A sucralfate Chemical compound O[Al](O)OS(=O)(=O)O[C@@H]1[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](COS(=O)(=O)O[Al](O)O)O[C@H]1O[C@@]1(COS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)O1 MNQYNQBOVCBZIQ-JQOFMKNESA-A 0.000 description 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a drug composition for curing peptic ulcer and a preparation method thereof. The composition includes aldioxa, vitamin E acetate and silica, can be prepared into solid drug for oral medication through dry granulation, can be taken in the form of orally-taken solid drug, and can quickly release aldioxa for neutralizing gastric acid, protecting mucosa and resisting ulcer, at the same time, the vitamin E acetate in the composition is released in the mucosa to repair damaged mucosa, and the two drugs can be combined and taken for cooperative and synergistic action.
Description
Technical field
The invention belongs to the pharmaceutical preparations technology field, be specifically related to a kind of pharmaceutical composition for the treatment of peptic ulcer and preparation method thereof.
Background technology
Peptic ulcer specifically comprises by diseases such as gastritis, peptic ulcer, duodenal ulcers.Main clinical manifestation is the symptoms such as epigastric discomfort, scorching hot or pain, anorexia, nausea and vomiting, acid regurgitation.Various gastritis, peptic ulcer belong to global frequently-occurring disease, commonly encountered diseases.There is documents and materials report peptic ulcer total incidence may account for the 10%-12% of population summation, not only sickness rate is high, and symptom has afterwards easy characteristics such as recurrence of chronicity, periodical attack, treatment, therefore peptic ulcer is considered to the disease of a kind of intractable, healing property of refractory, some patient in addition may concurrently bleed profusely, the severe complications such as gastric perforation and pylorus infraction.
Treat clinically gastritis at present.The drug main of peptic ulcer will have following a few class: 1, antacid, such as aluminium hydroxide, magnesium oxide etc., Main Function be in and gastric acid, reduce stomach and duodenal acidity.2, anticholinergic agent such as Semen daturae etc. can reduce gastric acid secretion, remove the gastrointestinal smooth muscle spasm, prolong the gastric emptying time.3, H
2Receptor blocking agent is such as methyl miaow guanidine, ranitidine etc., by blocking-up, H
2Receptor reduces gastric acid secretion.4, mucous membrane protection medicine such as sucralfate, aldioxa etc.The medicine of 5 anti-helicobacter pylori such as amoxicillin, metronidazole and quinolones etc.And when a kind of effect of drugs is bad in clinical, generally can take drug combination, can consider two kinds or three kinds of drug combinations.Such as the drug combination of antacid and gastrointestinal peristalsis inhibition, or H
2Receptor blocking agent and antacid coupling etc. so both can increase curative effect, can reduce untoward reaction again.
Aldioxa was synthesized in 1956, and it has good antiulcer effect discovery such as R.cachen of France in 1962, was the gastric mucosa repairing agent commonly used of the states such as U.S., DS, method, day in recent years.Aldioxa is decomposed into allantoin in gastrointestinal mucosal and aluminium hydroxide plays a role; specifically can suppress the effect of H+ diffuse in reverse direction, gastric acid secretion inhibiting reduces pepsic activity; suppress the reduction of prostaglandin (PG) level in the body, gastric mucosa is had protective effect.Simultaneously, promote the regeneration of granulation tissue and mucous epithelium tissue, improve mucosal blood flow, increase the synthetic and secretion of mucus, the time re-epithelialize tissue and the acid mucosa polysaccharides of ulcer granulation tissue increase the defense reaction of enhancing mucosa, promotion ulcer healing.Aldioxa is seen as a kind ofly can protect the reparation mucosa, can prevent and treat again the safely and effectively clinical medicine of peptic ulcer.
Vitamin E is a kind of fatsoluble vitamin, is one of most important antioxidant.Be dissolved in the organic solvents such as fat and ethanol, water insoluble, heat, acid are stablized.In patent CN1308531A, mentioned the application in vitamin E and the topical therapeutic of lipid in membrane disease thereof, for example in rectum, nose and eye mucosa ulcer, the application in the various mucosa injuries such as stomatocace.Smear in the document for the treatment of oral ulcer at vitamin E in addition; reported that the oral ulcer that the vitamin E treatment chemotherapy causes is evident in efficacy; vitamin E is because have antioxidant activity; the peroxidization that can stop unsaturated fatty acid; reduce the generation of peroxyester, thereby have the effect of stable protecting film, promote local blood circulation; alleviating pain accelerates the healing of ulcer surface.Vitamin E is fatsoluble vitamin, can enhance metabolism, and keeps the normal configuration function of cell, makes skin and subcutaneous tissue absorb enough nutrition, promotes the tissue adherence reparation.The prompting vitamin E has the effect of accelerating ulcer healing, and safe and reliable without clinical side effects, has obvious astriction, thereby has shortened the oral ulcer healing time.
Recently research discovery, vitamin E can promote gastrointestinal tract blood capillary and little blood vessel hyperplasia, and improves the peripheral blood circulation, increases the supply of tissue oxygen, thereby to ulcer surface healing long morning of good nutritional condition.In addition, still can suppress the growth of helicobacter pylori, the relapse rate of ulcer healing is reduced.According to another report, vitamin E is to the H2 receptor and resist invalid patient and still have good curative effect.These superior curative effects come from vitamin E and have absolute affinity for biomolecule, and the water of easily being secreted by mucosa is integrated, and participates in the repair process of impaired mucosa.
As mentioned above, clinical drug combination about digestive tract ulcer only is confined to the use of uniting of mucous membrane protection medicine or antacid and some spasmolytic medicines or bisfentidine so far; In view of the special role of vitamin in gastric ulcer, a kind of peptic gastric ulcer medicine and Vitamin E acetate compositions for the treatment of of the special proposition of the present invention.
Summary of the invention
The composition and method of making the same that the purpose of this invention is to provide a kind of digestive ulcer medicament, the compositions of aldioxa and Vitamin E acetate particularly, adopt Vitamin E acetate to mix with silicon dioxide first, then add the aldioxa mix homogeneously, adopt the mode of dry granulation to produce, technique can realize in large production, and product is stable, determined curative effect, and prescription is novel, two kinds of composition mechanism of action are complementary, Synergistic; Silicon dioxide is a kind of fluidizer and the diluent of pharmaceutically commonly using, and silicon dioxide can have good Absorption for the Vitamin E acetate of the thick liquid state in the product, guarantees to form the solid of stable state, is convenient to processing and the preservation of back.
For guaranteeing medicine in the enough curative effects of clinical generation, and avoid the excessive generation toxic and side effects of medicine, the weight percentage ranges of aldioxa and Vitamin E acetate is at 1:0.5~1:2 in the invention.When obtaining percentage by weight that silicon dioxide accounts for Vitamin E acetate and be 5%~15% through a large amount of experimentatioies, the Vitamin E acetate of the liquid state in the product can well become solid, be easy to the aldioxa mix homogeneously, add the adjunct ingredients such as diluent commonly used in some preparations and carry out dry method extruding granulation, further be distributed into capsule or granule, perhaps be pressed into suitable tablet hyoscine by tablet machine.The present invention preferably makes oral administered dosage form to the compositions of aldioxa and Vitamin E acetate and uses the forms such as preferred particulates agent, capsule, tablet.
The present invention can realize by following steps: the vitamin E gradation is added mix homogeneously in the silicon dioxide; Add the aldioxa mix homogeneously; The method that mixture adopts the dry method extruding to granulate, granule packing or tabletting.
Smooth for guaranteeing manufacturing process, add the conventional appetite adjuvant that uses of various dosage forms when also will make various dosage form again.The compare advantage of pharmaceutical composition of existing treatment gastric ulcer of compositions of the present invention is that the mechanism of action prescription of product is novel, determined curative effect, and clinical use is safe and effective; The preparation of product can realize the large production of mechanization, and technique is simple.
The specific embodiment
Below come by specific embodiment the present invention is done more detailed description, but can't consist of any restriction to the present invention.
Embodiment 1
Aldioxa 200g
Vitamin E acetate 100g
Silicon dioxide (in add) 5g
Silicon dioxide (adding) 2g
Lactose 93g
Making step:
1) the Vitamin E acetate gradation joins in the silicon dioxide of interior dosage, crosses 80 mesh sieve mix homogeneously.
2) the aldioxa fine powder is joined above mixing species mix homogeneously.
3) silicon dioxide and the lactose mix homogeneously of the outer dosage of adding.
4) mixture is through non-slurry pelletizing mechanism granule.
5) granule is packed as granule with aluminum-plastic composite membrane, and theoretical loading amount is the 400mg/ bag.
Embodiment 2
Aldioxa 100g
Vitamin E acetate 200g
Silicon dioxide 8.5g
Magnesium stearate 1.5g
Making step:
1) the Vitamin E acetate gradation joins in the silicon dioxide, crosses 80 mesh sieve mix homogeneously.
2) the aldioxa fine powder is joined above mixing species mix homogeneously.
3) above mixture non-slurry pelletizing.
4) add the magnesium stearate mix homogeneously in the gained granule.
5) detect intermediate content.
6) according to intermediate assay fill capsule as a result, theoretical loading amount is 310mg.
Embodiment 3
Aldioxa 100g
Vitamin E acetate 150g
Silicon dioxide 22.5g
Starch 31g
Microcrystalline Cellulose 45g
Magnesium stearate 1.5g
Making step:
1) the Vitamin E acetate gradation joins in the silicon dioxide, crosses 80 mesh sieve mix homogeneously.
2) the aldioxa fine powder is joined above mixing species mix homogeneously.
3) add microcrystalline Cellulose and starch mix homogeneously.
4) above mixture non-slurry pelletizing.
5) add the magnesium stearate mix homogeneously in the gained granule.
6) detect intermediate content.
[0050] 7) according to intermediate assay tabletting as a result, theoretical sheet heavily is 350mg.
Following result of the test will help to prove remarkable result of the present invention.
For the therapeutic effect of proved invention pharmaceutical composition to peptic ulcer, estimate simultaneously whether produce synergistic function after aldioxa and Vitamin E acetate make up, carry out following animal experiment, main approaches and result are as follows:
Compositions is tested the therapeutical effect of rat gastric ulcer:
(1) laboratory animal grouping and model
Get rat and be divided into 1 group of embodiment, 2 groups of embodiment, 3 groups of embodiment, aldioxa granules group, vitamin E group, blank group, totally 6 groups, 10 every group.
Water is can't help in the animal fasting, and constraint water logging legal system is made gastric ulcer model, and rat is fixed on the Mus plate, puts into tank liquid level xiphoid-process, and water temperature 13-15 ℃, water logging 24 hours.
(2) administration
Granule is blended directly in administration in the feedstuff among 1 group of the embodiment, 2 groups of desirable capsule 's contents of embodiment are blended in administration in the feedstuff, after can pulverizing, the tablet samples that embodiment 3 gives is blended in administration in the feedstuff, one of matched group gives aldioxa granules 0.2g ((the large positive lot number 1N12 of pharmaceutical industries Co., Ltd. of 50% Japan), two of matched group gives Vitamin E acetate 200mg/ time, and the normal feed of blank group is not stung all the other five groups of one weeks of administration, put to death, take out the body of stomach standard.
(3) index detects
Body of stomach standard: ligation pylorus, inject fixedly 10min of 10% formaldehyde by cardia, again whole body of stomach is taken out and put into fixedly 30min of 10% formalin, take out stomach, cut off along bight, normal saline flushing launches the coat of the stomach medial surface, dab off mucus and blood clot on the gastric mucosa with cotton pellet, observe the degree of injury of gastric mucosa.With ulcer index (ulcer index, UI) expression, namely the major diameter (d) according to mucosa injury calculates: d≤1mm is 1 minute, and 1mm<d≤2mm is 2 minutes, the like; Damage width>2mm person, mark doubles.The cumulative point of every animal is the ulcer index of this animal.
(4) experimental result
Calculate the ulcer inhibition rate of embodiment group, aldioxa group, vitamin E group, as shown in the table:
Contain the bioadhesive gel agent of aldioxa to the therapeutical effect of gastric ulcer
| Group | n | Average ulcer index (mm) | Suppression ratio (%) |
| Blank group | 10 | 42.36 | -- |
| 1 group of embodiment | 10 | 25.89 | 38.89 |
| 2 groups of embodiment | 10 | 24.18 | 42.91 |
| 3 groups of embodiment | 10 | 25.84 | 40.0 |
| The aldioxa group | 10 | 35.56 | 16.05 |
| The vitamin E group | 10 | 39.79 | 6.06 |
Relatively can find out from above curative effect, compositions of the present invention to the ulcer inhibition rate of peptic ulcer rat apparently higher than usefulness
Bursin aluminum group and alone vitamin E group, the significant difference (P<0.01) that has respectively very significant.
The above description of test present composition, aldioxa and vitamin E combined therapy peptic ulcer determined curative effect are reliable.Technique prepares the aspect in order to realize large-scale production, has added a certain proportion of silicon dioxide in the compositions as absorbent, and the technique of employing non-slurry pelletizing prepares the oral administered dosage form of compositions, technique simple possible.
Claims (4)
1. a pharmaceutical composition for the treatment of peptic ulcer is characterized in that said composition comprises aldioxa, Vitamin E acetate and silicon dioxide.
2. the pharmaceutical composition for the treatment of peptic ulcer as claimed in claim 1 is characterized in that the part by weight of aldioxa and Vitamin E acetate is 1:0.5~1:2 in the prescription, and the percentage by weight that silicon dioxide accounts for Vitamin E acetate is 5%~15%.
3. the pharmaceutical composition for the treatment of peptic ulcer as claimed in claim 1 is characterized in that described compositions is oral dosage form, is specially capsule, granule, tablet.
4. preparation method for the treatment of the pharmaceutical composition of peptic ulcer, its distinctive preparation method is as follows: Vitamin E acetate mixes with silicon dioxide; Add the aldioxa mix homogeneously; The method that mixture adopts the dry method extruding to granulate, granule packing or tabletting.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105926587A CN103040816A (en) | 2012-12-31 | 2012-12-31 | Drug composition for curing peptic ulcer |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012105926587A CN103040816A (en) | 2012-12-31 | 2012-12-31 | Drug composition for curing peptic ulcer |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110623976A (en) * | 2019-10-24 | 2019-12-31 | 无锡济民可信山禾药业股份有限公司 | Chewable tablet for treating gastric and duodenal ulcers and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1225017A (en) * | 1996-07-12 | 1999-08-04 | 第一制药株式会社 | Rapidly disintegrating compression molded substance and method for its production |
| EP2042164A1 (en) * | 2006-06-23 | 2009-04-01 | Takeda Pharmaceutical Company Limited | Stabilized solid preparation |
| EP2246049A2 (en) * | 2003-05-22 | 2010-11-03 | Lipocine, Inc. | Pharmaceutical composition and dosage forms for administration of hydrophobic drugs |
| EP2465539A1 (en) * | 2009-08-11 | 2012-06-20 | Fuji Chemical Industry Co., Ltd. | Disintegrating particle composition and orally rapidly disintegrating tablet |
-
2012
- 2012-12-31 CN CN2012105926587A patent/CN103040816A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1225017A (en) * | 1996-07-12 | 1999-08-04 | 第一制药株式会社 | Rapidly disintegrating compression molded substance and method for its production |
| EP2246049A2 (en) * | 2003-05-22 | 2010-11-03 | Lipocine, Inc. | Pharmaceutical composition and dosage forms for administration of hydrophobic drugs |
| EP2042164A1 (en) * | 2006-06-23 | 2009-04-01 | Takeda Pharmaceutical Company Limited | Stabilized solid preparation |
| EP2465539A1 (en) * | 2009-08-11 | 2012-06-20 | Fuji Chemical Industry Co., Ltd. | Disintegrating particle composition and orally rapidly disintegrating tablet |
Non-Patent Citations (1)
| Title |
|---|
| 程留芳等: "尿囊素铝颗粒治疗胃炎及消化性溃疡的疗效及安全性", 《中国新药杂志》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110623976A (en) * | 2019-10-24 | 2019-12-31 | 无锡济民可信山禾药业股份有限公司 | Chewable tablet for treating gastric and duodenal ulcers and preparation method thereof |
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Application publication date: 20130417 |