CN101313898A - Composition for treating gastrointestinal tract diseases - Google Patents
Composition for treating gastrointestinal tract diseases Download PDFInfo
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- CN101313898A CN101313898A CNA2008101162154A CN200810116215A CN101313898A CN 101313898 A CN101313898 A CN 101313898A CN A2008101162154 A CNA2008101162154 A CN A2008101162154A CN 200810116215 A CN200810116215 A CN 200810116215A CN 101313898 A CN101313898 A CN 101313898A
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- pharmaceutical composition
- azulene
- glutaminate
- ulcer
- tablet
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Abstract
The invention relates to a composite for treating gastrointestinal tract diseases, comprising L-glutamine and an azulene derivative, wherein, the azulene derivative is a compound shown in formula I, M is zinc, magnesium and bismuth, and n is an integral between 1 and 3.The composite can be made into oral preparation, including troches, capsules, soft capsules, chewable tablets, rapidly disintegrating oral tablets, buccal tablets and dropping pills. The unit preparation content of the L-glutamine is between 0.2 and 3g, and preferable between 0.6 and 2g. The unit preparation content of the azulene derivative is between 0.6 and 10mg, and preferable between 1 and 4.5mg.
Description
Technical field
The present invention relates to a kind of compositions that is used for the treatment of gastroenteropathy, particularly relate to a kind of compositions that includes L-glutaminate and a kind of azulene analog derivative, belong to the pharmaceutical technology field.
Background technology
Azulenoid has following effects: suppress the inflammation that multiple inflammation-causing substance causes, and effect is comparatively lasting; Directly act on the inhibition inflammatory cell by the part and discharge histamine; Increase prostaglandin E in the mucosa
2Synthetic, promote granulation to form and epithelial cell new life; Reduce pepsic activity.Give this product to the ulcer that causes by aspirin, find that aminohexose content increases in the gastric mucosa, and the pepsin amount reduces, and reduces 75% approximately during PH2.0, reduces 78% approximately during PH3.5, has the effect of tangible promotion ulcer healing; NSAID (non-steroidal anti-inflammatory drug) such as aspirin, indomethacin, diclofenac sodium are share separately or with this product give rat, visible combination group medication group aminohexose amount increase separately after 5 or 10 days, ulcer is suppressed, and does not influence the absorption of NSAID (non-steroidal anti-inflammatory drug).Can be used for various idiopathic acute and chronic gastritis clinically, stomach or duodenal ulcer, concurrent Secondary cases gastritis such as gastric cancer or stomach excision, anemia, the concurrent excitability gastritis of disease such as various infectious disease, hepatitis, cholelithiasis.
Some metal ions are to gastroenteropathy, and especially ulcer class disease has special effect.For example, zinc ion can promote mucosa regeneration, quickens ulcer healing, and the cytoprotection of similar prostaglandin is arranged.Zinc is to absorb in duodenum and proximal small bowel, and the main excretion pathway of human body zinc is an intestinal, therefore takes the change that does not cause main organs trace element in the body for a long time, does not also cause accumulating of zinc.Bismuth class medicine neither in and gastric acid; also not gastric acid inhibitory secretion; but under the Gastric pH condition; on the ulcer surface or ulcer substrate granulation tissue form a kind of firm bismuth oxide colloidal precipitation; become the protectiveness thin film; thereby isolated gastric acid; enzyme and food are to the corrosion function of ulcer mucosa; promote the reparation and the healing of chronic ulcer tissue; bismuth ion can promote mucous secretion; can promote ulcer healing to a certain extent; simultaneously because bismuth and bacteria cell wall and wall slurry film formation on every side complex; can suppress the generation of some enzymes of helicobacter pylori; as urease; catalase and lipase etc., these endonuclease capables influence little growing environment of antibacterial, therefore also have the effect of killing helicobacter pylori.Magnesium ion has the catharsis effect, can prevent the constipation symptom that some antiulcerative causes, magnesium also has spasmolytic, abirritative effect simultaneously, can alleviate ulcer patient's pain.
Summary of the invention
The present invention is a kind of compositions that is used for the treatment of gastroenteropathy, includes L-glutaminate and a kind of azulene analog derivative, and wherein said azulene analog derivative is a chemical compound shown in the formula I.
M is zinc, magnesium, bismuth, and n is 1～3 integer.
Said composition can be made into oral formulations, comprises tablet, capsule, soft capsule, chewable tablet, oral cavity disintegration tablet, buccal tablet, drop pill.The unit formulation content of described L-glutaminate is 0.2g～3g, preferred 0.6g-2g.The unit formulation content of described azulene class salt derivative is 0.6mg～10mg, preferred 1mg～4.5mg.This Pharmaceutical composition is used for the treatment of the gastrointestinal tract tract disease, especially is suitable for treating gastritis and peptic ulcer.This compound has been inherited azulenoid and the advantage of L-glutaminate aspect treatment gastrointestinal tract tract disease on the one hand; this prescription was loaded with on the other hand particulate metal ion pair gastrointestinal tract tract disease, especially gastritis and peptic ulcer also have certain protection and therapeutical effect.
By following pharmacological evaluation, further specify the curative effect of azulene class salt derivative of the present invention aspect the treatment digestion disease.
1. experiment modeling:
Fasting feedwater 24h before 135 rat modelings, etherization in the cover+beaker cotton balls nose appends anesthesia, iodine tincture, ethanol routine disinfection, the xiphoid-process lower abdomen hits exactly the 2～2.5cm that hits, and separates abdominal muscle, cuts off peritoneum, gently move to stomach outside the abdomen, at the stomach facies ventralis, body of stomach and pyloric antrum intersection thrust 0.4～0.5mm under the serous coat with microsyringe is flat, inject 10 glacial acetic acid 0.1mL, form pimple, stomach is sent back to, sew up abdominal muscle, skin.
2. experimental technique:
135 rats are divided into 5 groups at random: blank model group, the azulene class bismuth salt+L-glutaminate group (A) of deriving, the azulene class zinc salt+L-glutaminate group (B) of deriving, the azulene class magnesium salt+L-glutaminate group (C) of deriving, Marzulene group.Beginning administration in the 3rd day after the modeling, each group is all irritated stomach by 3mL/ (100g.d), blank model group is given the equal-volume normal saline, each organizes equal every day 1 time, totally 4 weeks. modeling 3d (before the administration), 17d (administration 14d), 31d (administration 28d) divides 3 batches to put to death rat, cut off the abdominal cavity along ventrimeson, take out stomach, cut off along greater gastric curvature, clean with the ice normal saline flushing. gastric mucosa is flattened on flat board, maximum major diameter and the wide footpath of vertical maximum with vernier caliper measurement ulcer. ulcer index (uI) is measured the major diameter and the wideest footpath of ulcer with slide gauge, multiplying each other calculates the ulcer area as ulcer index, ulcer area: S=1/4 * DL * DS * towering, and DL refers to the ulcer major diameter in the formula, DS refers to the ulcer minor axis, the towering 3.14. that gets
3. experimental result:
Table 1 respectively organize rat ulcer index (mm2) and ulcer inhibition rate comparison (mean ± SD, n=15)
The specific embodiment
Can further describe the present invention by the following examples, yet invention of the present invention is not limited to the following examples.
Embodiment 1L-glutamine and the azulene class bismuth salt tablets of deriving
Prescription:
Preparation method:
Derive bismuth salt, microcrystalline Cellulose of azulene class crossed 80 mesh sieves respectively, and mix homogeneously is adopting the equivalent method of progressively increasing to mix with L-glutaminate, and fully stirring makes even, standby; 50% alcoholic solution is joined in the mixed powder, the system soft material, 24 mesh sieves are granulated, drying, 20 mesh sieve granulate add micropowder silica gel, CMS-Na, adopt suitable punch die compressed tablets behind the mix homogeneously, promptly.
If carry out coating for above-mentioned tablet, then obtain coated tablet, can be Film coated tablets, enteric coatel tablets etc.
Embodiment 2:L-glutamine and the azulene class bismuth salt capsule of deriving
Prescription:
Preparation method:
Derive bismuth salt, L-glutaminate of azulene class all crossed 80 mesh sieves, progressively increase behind the method mix homogeneously, add magnesium stearate according to equivalent, mix homogeneously, packing, promptly.
Used capsule shells can be conventional capsule, also can be enteric coated capsule.
Embodiment 3:L-glutamine and the azulene class zinc salt chewable tablet of deriving
Prescription:
Preparation method:
Supplementary materials such as zinc salt, L-glutaminate, xylitol, mannitol that the azulene class is derived are crossed 80 mesh sieves respectively, adopt equivalent incremental method mix homogeneously, add the 2%PVP-k30 alcoholic solution, the system soft material, 16 mesh sieves are granulated, drying, 20 mesh sieve granulate, the correctives, sweeting agent, the fluidizer mix homogeneously that add other, tabletting, promptly.
Embodiment 4:L-glutamine and the azulene class zinc salt dispersible tablet of deriving
Prescription
Preparation method:
Supplementary materials such as zinc salt, L-glutaminate, microcrystalline Cellulose that the azulene class is derived are crossed 80 mesh sieves respectively, adopt equivalent incremental method mix homogeneously, and are standby; Add 75% alcoholic solution, the system soft material, 16 mesh sieves are granulated, drying, 20 mesh sieve granulate add other correctives orange flavor, sweeting agent stevioside, fluidizer micropowder silica gel, mix homogeneously such as disintegrating agent PPVP, L-HPC, tabletting, promptly.
Embodiment 5:L-glutamine and the azulene class magnesium salt effervescent tablet of deriving
Prescription
Preparation method:
L-glutaminate and the azulene class magnesium salt of deriving is crossed 80 mesh sieves, mix homogeneously; Get half mixed powder amount, with the citric acid mix homogeneously, with 50% alcoholic solution system soft material, 18 orders are granulated, drying, 16 order granulate; Get the surplus mixed powder again, mix with sodium carbonate, sodium bicarbonate, the same method is granulated; Two kinds of granules of gained mix, and add other adjuvant, and as mix homogeneously such as PEG6000, orange flavor, acesulfame potassium, sodium chloride, tabletting promptly.
Embodiment 6:L-glutamine and the azulene class bismuth salt particle of deriving
Prescription
Preparation method:
Derive bismuth salt, mannitol, sorbitol of L-glutaminate, azulene class was waited 80 mesh sieves, mix homogeneously; With the 75% alcoholic solution system soft material of 5%PVPk 1,16 orders are granulated, drying, and 12 order granulate add other adjuvant, and as mix homogeneously such as orange flavor, acesulfame potassiums, packing is promptly.
Claims (9)
1. a compositions that is used for the treatment of gastroenteropathy includes L-glutaminate and a kind of azulene analog derivative, and it is characterized in that: described azulene analog derivative is a chemical compound shown in the formula I.
M is zinc, magnesium, bismuth, and n is 1～3 integer.
2. the described Pharmaceutical composition of claim 1 is characterized in that, can be made into oral formulations.
3. the described Pharmaceutical composition of claim 3 is characterized in that, described oral formulations comprises tablet, capsule, soft capsule, chewable tablet, oral cavity disintegration tablet, buccal tablet, drop pill.
4. the described Pharmaceutical composition of claim 1 is characterized in that, the unit formulation content of described L-glutaminate is 0.2g～3g.
5. the described Pharmaceutical composition of claim 4 is characterized in that, the unit formulation content of described L-glutaminate is 0.6g-2g.
6. the described Pharmaceutical composition of claim 1 is characterized in that, the unit formulation content of described azulene class salt derivative is 0.6mg～10mg.
7. the described Pharmaceutical composition of claim 1 is characterized in that, the unit formulation content of described azulene class salt derivative is 1mg～4.5mg.
8. described any one Pharmaceutical composition of claim 1～7 is used for the treatment of the gastrointestinal tract tract disease.
9. described any one Pharmaceutical composition of claim 1～7 is used for the treatment of gastritis and peptic ulcer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101162154A CN101313898A (en) | 2008-07-07 | 2008-07-07 | Composition for treating gastrointestinal tract diseases |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101162154A CN101313898A (en) | 2008-07-07 | 2008-07-07 | Composition for treating gastrointestinal tract diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101313898A true CN101313898A (en) | 2008-12-03 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008101162154A Pending CN101313898A (en) | 2008-07-07 | 2008-07-07 | Composition for treating gastrointestinal tract diseases |
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| CN (1) | CN101313898A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120203102A1 (en) * | 2009-09-11 | 2012-08-09 | Mallinckrodt Llc | Azulene and azaazulene systems for imaging, monitoring and therapy |
| CN106692099A (en) * | 2016-12-22 | 2017-05-24 | 南京济群医药科技股份有限公司 | Glutamine acid amide compound film-coated tablets and preparation method thereof |
-
2008
- 2008-07-07 CN CNA2008101162154A patent/CN101313898A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120203102A1 (en) * | 2009-09-11 | 2012-08-09 | Mallinckrodt Llc | Azulene and azaazulene systems for imaging, monitoring and therapy |
| US9226980B2 (en) * | 2009-09-11 | 2016-01-05 | Medibeacon Inc. | Azulene and azaazulene systems for imaging, monitoring and therapy |
| US10059739B2 (en) | 2009-09-11 | 2018-08-28 | Medibeacon Inc. | Non-benzenoid aromatic systems for imaging, monitoring and therapy |
| CN106692099A (en) * | 2016-12-22 | 2017-05-24 | 南京济群医药科技股份有限公司 | Glutamine acid amide compound film-coated tablets and preparation method thereof |
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| PB01 | Publication | ||
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Open date: 20081203 |