CN1814289A - Medicine composition for treating degestive ulcer - Google Patents
Medicine composition for treating degestive ulcer Download PDFInfo
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- CN1814289A CN1814289A CN 200510200782 CN200510200782A CN1814289A CN 1814289 A CN1814289 A CN 1814289A CN 200510200782 CN200510200782 CN 200510200782 CN 200510200782 A CN200510200782 A CN 200510200782A CN 1814289 A CN1814289 A CN 1814289A
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Abstract
This invention is a medicine combination for curing peptic ulcer. Its feature is that it contains fade melanin or L-tryptophan, and at least one kind of pylorus spirabacteria inhibitor or gastric acid secretion inhibitor. Pylorus spirabacteria inhibitor is selected from penicillin, ampicillin, metronidazole furazolidone etc. And gastric acid secretion inhibitor is lafutidine, famotidine, roxatidine, tenatoprazole, latamoxef sodium, rabeprazole, pantoloc, aluminum hydroxide, magnesium hydroxide, baking soda and calcium carbonate. The compound can be make into granule, effervesce agent, tablet, capsule, molasses, injection, suspensoid injection, suppository or sustained-release preparations. It is taken by oral administration or non-oral administration path. It achieves the goal of preventing and curing gastric ulcer and duodenal ulcer by effectively clear oxygen-derived free radicals, inhibiting grown of pylorus spirabacteria and gastric acid secretion.
Description
Technical field
The present invention relates to a kind of treatment digestive ulcer medicament compositions, belong to medical technical field.
The research background
Peptic ulcer mainly refers to gastric ulcer and duodenal ulcer, and pathological changes is confined to stomach and 12 and refers to mucosa.Along with the Chinese society development, the change of circumstances, the variation of population structure and people life style, main because of smoking, drink, peptic ulcer rate that nervous, medicine irritation etc. causes increases gradually, become a kind of commonly encountered diseases and frequently-occurring disease, bring great misery to the patient, cause patients ' life quality to descend.Therefore for these reasons, the treatment of peptic ulcer more and more receives publicity clinically and payes attention to, and invents a kind of medicament for resisting peptic ulcer safely and effectively to have received very big concern, and becomes one of the emphasis of present drug development research and focus.
Think always that for many years gastric ulcer and duodenal ulcer are main because due to the gastric acid excessive secretion.So mainly be the gastric acid inhibitory secretion aspect treatment.It is a lot of to secrete the medicine for the treatment of digestive system and ulcer by gastric acid inhibitory at present, comprises histamine receptor antagonist, antacid and H
+-K
+ATP enzyme (claiming proton pump again) inhibitor etc.Up-to-date discovers, the gastric acid excessive secretion is not the main cause of ulcer, and wherein helicobacter pylori infection is being brought into play more and more important effect in gastric ulcer and duodenal ulcer form.The two mutually promotes helicobacter pylori infection and gastric acid excessive secretion, therefore, for a long time, secretes by gastric acid inhibitory merely and treats gastric ulcer and the duodenal ulcer effect is not very good.In addition, helicobacter pylori infection and gastric cancer has a confidential relation.Not only can effectively treat gastric ulcer and duodenal ulcer so effectively suppress helicobacter pylori infection, important function is taken place to have equally prevention gastric cancer.
In addition, new result of study shows that stomach and 12 refers to that mucosa injury is relevant unusually with local oxygen metabolism.In the gastric ulcer active stage, the active of the superoxide dismutase (SOD) of ulcer mucosa periphery obviously reduces, and in the gastric ulcer healing phase, and the burst activity of local SOD of stomach obviously increases than its peripheral normal mucosa and (sees Naito Y etc.; J Clin Gastroenterol.1992; 14 Suppl 1:S131-4).
Gastric acid secretion is a complex physical process, wherein, histamine, gastrin and acetylcholine etc. can stimulate the activity of parietal cell, and gastrin and acetylcholine except direct effect, also can promote gastric mucosal cell to discharge the histamine that stores to parietal cell.Therefore, histamine is the important mediation person of gastric acid secretion.Another important step that causes gastric acid secretion is the commentaries on classics shape that occurs in the film on the parietal cell.After cell was stimulated, intracellular pipe capsule melted to be incorporated on the plasma membrane of top and forms an expansible secretory tubyle, and H is wherein arranged
+/ K
+-ATP enzyme.By this mode, H
+/ K
+-ATP enzyme (proton pump) is with H
+With K
+Exchange finally mediates gastric acid secretion.Therefore, histamine is the important mediation person of gastric acid secretion, and is positioned at the tubulovesicle of parietal cell and secretes H on the periosteum
+/ K
+-ATP enzyme (proton pump) participates in last link of gastric acid secretion.Simple one of them link that suppresses has certain inhibitory action to gastric acid secretion, but DeGrain.Increased dosage amount will be subjected to the restriction of toxic reaction, and dosage is not enough or treat and irregularly will cause disease relapse.
Histamine receptor antagonist can be secreted by gastric acid inhibitory, though it is stronger the influence of gastric acid secretion to be compared the influence of other physiological function, but because histamine's receptor also is present in many other tissues, comprise blood vessel, tracheal smooth muscle and right atrium etc., so such medicine has than significant side effects to circulation, breathing and central nervous system.Not ideal enough as cimetidine and ranitidine treatment peptic ulcer effect.Cause ulcer recurrence easily.H
+/ K
+-atpase inhibitor, promptly proton pump inhibitor (PPI) is the excretory medicine of the novel gastric acid inhibitory of a class.The excretory effect of this type of medicine gastric acid inhibitory is stronger, but stable inadequately under sour environment, and therefore, therapeutic effect is difficult to consolidate.In addition, proton pump inhibitor such as omeprazole also can cause hypergastrinemia (Arnold R et al., 1986 by starting the gastric antrum feedback mechanism; Creutzfeldt W et al., 1986; Larsson H., 1986), cause the diffusivity endocrine cell hyperplasia of body of stomach then, be carcinoid feature (Ekmanet al., 1985).Thereby the long-term H that uses separately
+/ K
+-atpase inhibitor is very limited, and dosage is not enough or treat and irregularly will cause ulcer repeatedly.
Summary of the invention
The present invention is directed to the deficiencies in the prior art a kind of treatment digestive system and ulcer pharmaceutical composition is provided; this pharmaceutical composition is not only brought into play its protective effect to stomach and 12 finger mucosas by effective removing oxygen-derived free radicals, also can have potentiation to other treatment digestive system and ulcer medicine.Thereby on the basis of effectively alleviating the mucosa injury that radical metabolism causes unusually facilitating digestion system ulcer healing.
The present invention treats the combination that digestive ulcer medicament compositions main component is melatonin (melatonin, melatonin) or L-tryptophan and helicobacter pylori inhibitor or gastric acid secretion inhibitor.
The helicobacter pylori inhibitor is for can eliminate the antibiotic of helicobacter pylori (gastric ulcer pathogenic bacterium) in the compositions, as, but be not limited to, penicillin, ampicillin, amoxicillin (amoxicillin, amoxicillin), metronidazole, furazolidone, erythromycin (Erythromycin), erythromycin (clarithromycin) and analog, gentamycin and tetracycline (tetracycline) etc.The dosage of helicobacter pylori inhibitor is decided according to clinical consumption, can be 0.01-500mg/kg, is preferred with 1-100mg/kg, and 2-50mg/kg is for most preferably.Also can tire according to it, the unit of pressing/kg body weight is determined.Can be from 1-500U/kg, be preferred with 10-100U/kg, 2-50U/kg is for most preferably.
Gastric acid secretion inhibitor be selected from cimetidine, lafutidine, famotidine, roxatidine, rabeprazole, Tenatoprazole, lansoprazole, pantoprazole, S-omeprazole (esomeprazole, Nexium), Lai Minuola azoles (leminoprazole), for one of Nola's azoles, rabmprazole, leminoprazole, dosmalfate (dosmalfate), fumaric acid tenofovir fat and sofalcone or its combination.The dosage of gastric acid secretion inhibitor can be 0.1-100mg/kg, is preferred with 1-80mg/kg, and 2-50mg/kg is for most preferably.If select more than one gastric acid secretion inhibitors, each used dosage can suitably reduce.
Gastric acid secretion inhibitor also is selected from antacid, includes, but not limited to aluminium hydroxide, magnesium hydroxide, sodium bicarbonate and calcium carbonate etc.
The dosage of melatonin or L-tryptophan is 0.001-1000mg/kg, is preferred with 1-200mg/kg, and 5-50mg/kg is for most preferably.
The ratio of melatonin or L-tryptophan and other treatment digestive system and ulcer medicine is decided because of concrete condition, can be 1-9: 1 to 1: 1-9.
The preferred compositions that the present invention treats the digestive ulcer medicament compositions comprises:
(1) combination of melatonin or L-tryptophan and penicillin, ampicillin, amoxicillin, metronidazole, furazolidone, erythromycin, erythromycin, gentamycin or tetracycline; Or
(2) melatonin or L-tryptophan and cimetidine, lafutidine, famotidine, roxatidine, lansoprazole, rabeprazole, Tenatoprazole, pantoprazole, S-omeprazole, Lan Minuola azoles, for the combination of Nola's azoles, rabmprazole, leminoprazole, dosmalfate and/or sofalcone; Or
(3) combination of melatonin or L-tryptophan and aluminium hydroxide, magnesium hydroxide, sodium bicarbonate or calcium carbonate.
The present invention treats the digestive system and ulcer compositions, and to be used for the treatment of the gastric and duodenal ulcers side effect little, the safe coefficient height.Effective ingredient can directly be taken raw material in the compositions, but uses after preferably its effective ingredient being made various pharmaceutical dosage forms.Effective ingredient and pharmaceutical carrier and excipient and/or carrier holder can be mixed, make various oral formulations or non-intestinal application forms.Oral agents can be, but is not limited to, powder, granule, tablet, pill, capsule, electuary, powder, syrup, slow releasing agent, controlled release agent or slowbreak agent.The dosage of every day is 0.01 to 10 milligram of everyone 1 to 1000 milligram or per kilogram of body weight when oral, and the dosage of every day most preferably is 0.1 to 2.5 milligram of everyone 10 to 250 milligrams or per kilogram of body weight.Non-intestinal application forms can be, but is not limited to, injection, suppository or implant.By 0.5 to the 10% w/v injection of making soluble in water, the suitable dose of injection is 0.5 to 1000 milligram for each person every day with water solublity active drug composition, with for each person every day 100 to 500 milligrams be the best.The dosage of every day can once be taken or be divided into 2 to 4 times and take.Also the active drug composition can be wrapped in and make agent for slow releasing in the slow-release auxiliary material, agent for slow releasing can be slow releasing agent, controlled release agent or slowbreak agent, can be oral or through subcutaneous or intramuscular injection or place in anal canal, as suppository.
The present invention treat the effective ingredient of digestive system and ulcer compositions can medicine and/or the mode of nutrient and healthcare products use.Wherein best form is with its effective ingredient rapid release at gastric.The effective ingredient of compositions can be made powder, granule, tablet (coated tablet, effervescent tablet, slow releasing tablet), pill, capsule, electuary, powder, syrup, slow releasing agent, controlled release agent, slowbreak agent, suspension or injection separately or with pharmaceutical carrier, excipient.For the effective ingredient that can make compositions plays a role at the multiple position of ulcer (as stomach and duodenum), the effective ingredient of compositions is preferably made lamellar, capsule, injection, suspension or slow releasing agent.
Effective ingredient of the present invention can be made various dosage forms through traditional preparation process.When making solid oral dosage form, effective ingredient is mixed with filler, add binding agent, disintegrating agent, lubricant, developer, corrigent or its analog in case of necessity, then mixture is made tablet or capsule.Following preparation method and non-active ingredient just are used for further specifying of the present invention, are not limitation of the present invention.Equally, the used effective ingredient of the present invention with and application etc. just be used for further specifying to of the present invention, be not limitation of the present invention.
Compositions of the present invention mainly by effective protection gastric mucosa, suppress helicobacter pylori and gastric acid secretion be used for the treatment of gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Eillison syndrome etc., stomach and duodenitis and with gastric acid secretion imbalance diseases associated.Therefore the main component of the present composition be used to prepare treatment treatment gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Eillison syndrome etc., stomach and duodenitis and with the pharmaceutical preparation of gastric acid secretion imbalance diseases associated.
The compositions range of choice of the present invention is wide, good effect, few side effects, effect stability, does not recur, and suppresses with independent application helicobacter pylori, histamine H 2-receptor antagonist or proton pump inhibitor compare, and has obvious superiority.Its superiority can be embodied by following experimental result.
1, to the influence of gastric acid secretion:
Treating excess syndrome is tested with female, 6 weeks, body weight 150-170 gram Wistar rat, and single being fixed in makes its fasting can't help water 48 hours in the ferrum cage.Take medicine and after 1 hour its stomachus pyloricus (stomach lower end) is used the surgical thread ligation.Rat was used CO in 19 hours after the ligation
2Put to death.With stomach cardia portion (Weishang end) ligation, purpose is to prevent that gastric juice from flowing out with surgical thread in the dissection back.And then stomach taken off, the place cuts off stomach along greater gastric curvature, makes gastric juice flow into centrifuge tube, adds 40ml distilled water and 3 (10mg/ml) phenolphthalein behind the centrifugal 40min of 2400 commentaries on classics/min again.Use 0.1mol/L NaOH titration afterwards.Write down the volume of the NaOH that consumes, and calculate inhibitory action as follows gastric acid secretion.
Press down sour rate=[(blank animal NaOH consumes volume-medication animal NaOH and consumes volume)/blank animal NaOH consumes volume] * 100%
2, the inhibitory action of ulcer
Make its fasting can't help water 48 hours in the ferrum cage single being fixed in of same experimental rat.Take medicine and after 1 hour its stomachus pyloricus (stomach lower end) is used the surgical thread ligation.Rat was used CO in 19 hours after the ligation
2Put to death.With stomach cardia portion (Weishang end) ligation, purpose is to prevent that gastric juice from flowing out with surgical thread in the dissection back.And then stomach taken off, the place cuts off stomach along greater gastric curvature, and water with the naked eye and in conjunction with anatomic microscope is observed the damaged surfaces degree after washing away the impurity on Weishang, and calculates ulcer index (UI) as follows, and ulcer inhibition rate.
Ulcer inhibition rate=[(matched group UI-medication group UI)/blank group UI] * 100%
Test one, compare metronidazole, lansoprazole, cimetidine and melatonin inhibitory action rat tolerance secretion and ulcer.Experimental result (seeing Table one) shows, when above medicine is used separately gastric acid secretion all had in various degree inhibitory action, and is best with the action effect of lansoprazole, cimetidine and melatonin.When share, the inhibitory action of gastric acid secretion is not had obvious enhancing, but the inhibitory action of gastric ulcer is increased to some extent, with the drug combination effect that contains melatonin for well, wherein, the effect of melatonin and lansoprazole drug combination is best, secondly is the associating with cimetidine or metronidazole.
Table one, melatonin etc. are to the inhibitory action of rat tolerance secretion and ulcer
| Metronidazole (5mg) | Lansoprazole (7.5mg) | Cimetidine (25mg) | Melatonin (5mg) | Gastric acid secretion suppression ratio (%) | Ulcer index | Ulcer suppression ratio (%) |
| - | - | - | - | 30 | ||
| + | - | - | - | 12 | 12 | 28 |
| - | + | - | - | 18 | 16 | 37 |
| - | - | + | - | 32 | 20 | 29 |
| - | - | - | + | 36 | 18 | 46 |
| + | - | - | + | 38 | 2.8 | 80 |
| - | + | - | + | 30 | 1.2 | 96 |
| - | - | + | + | 26 | 2 | 90 |
Test two, compare erythromycin, Tenatoprazole, rabeprazole and melatonin inhibitory action rat tolerance secretion and ulcer.Experimental result (seeing Table two) shows, when above medicine is used separately gastric acid secretion all had in various degree inhibitory action.When share, the inhibitory action of gastric acid secretion is not had obvious enhancing, but the inhibitory action of gastric ulcer is increased to some extent.Wherein, the effect of melatonin and rabeprazole drug combination is best, secondly is the associating with Tenatoprazole and erythromycin.
Table two, melatonin etc. are to the inhibitory action of rat tolerance secretion and ulcer
| Erythromycin (100,000 unit) | Tenatoprazole (7.5mg) | Rabeprazole (7.5mg) | Melatonin (5mg) | Gastric acid secretion suppression ratio (%) | Ulcer index | Ulcer suppression ratio (%) |
| - | - | - | - | 26 | ||
| + | - | - | - | 23 | 33 | 21 |
| - | + | - | - | 33 | 20 | 17 |
| - | - | + | - | 46 | 16 | 28 |
| - | - | - | + | 18 | 14 | 33 |
| + | - | - | + | 58 | 1.8 | 80 |
| - | + | - | + | 56 | 1.6 | 86 |
| - | - | + | + | 68 | 1.5 | 94 |
Test three, compare melatonin, pantoprazole and lafutidine inhibitory action rat tolerance secretion and ulcer.Experimental result (seeing Table three) shows, when above medicine is used separately gastric acid secretion all had in various degree inhibitory action.When share, the inhibitory action of gastric acid secretion is not had obvious enhancing, but the inhibitory action of gastric ulcer is increased to some extent.Wherein, the effect of melatonin and lafutidine drug combination is best, secondly is the associating with pantoprazole and penicillin.
Table three, melatonin etc. are to the inhibitory action of rat tolerance secretion and ulcer
| Melatonin (7.5mg) | Penicillin (10,000 U) | Pantoprazole (15mg) | Lafutidine (50mg) | Gastric acid secretion suppression ratio (%) | Ulcer index | Ulcer suppression ratio (%) |
| - | - | - | - | 28 | ||
| + | - | - | - | 22 | 12 | 37 |
| - | + | - | - | 12 | 22 | 24 |
| - | - | + | - | 43 | 28 | 38 |
| - | - | - | + | 36 | 20 | 39 |
| + | + | - | - | 62 | 1.4 | 85 |
| + | + | - | 54 | 1.2 | 90 | |
| + | - | - | + | 58 | 1.8 | 94 |
Test four, compare furazolidone, replace Nola's azoles, famotidine and melatonin inhibitory action rat tolerance secretion and ulcer.Experimental result (seeing Table four) shows, when above medicine is used separately gastric acid secretion all had in various degree inhibitory action, when the associating time spent, the inhibitory action of gastric acid secretion obviously strengthened, and is more obvious to the inhibitory action of gastric ulcer.
Table four, furazolidone etc. are to the inhibitory action of rat tolerance secretion and ulcer
| Furazolidone (5mg) | For Nola's azoles (10mg) | Famotidine (50mg) | Melatonin (50mg) | Gastric acid secretion suppression ratio (%) | Ulcer index | Ulcer suppression ratio (%) |
| - | - | - | - | 36 | ||
| + | - | - | - | 12 | 12 | 54 |
| - | + | - | - | 31 | 15 | 42 |
| - | - | + | - | 36 | 13 | 50 |
| - | - | - | + | 26 | 16 | 38 |
| + | - | - | + | 50 | 2 | 90 |
| - | + | - | + | 52 | 1.8 | 90 |
| - | - | + | + | 67 | 1.9 | 92 |
Test one shows to test four results: the gastric acid secretion inhibitor of trying, comprise proton pump inhibitor and histamine receptor antagonists, and gastric acid secretion and ulcer are all had than the obvious suppression effect.Though melatonin and helicobacter pylori inhibitor are not obvious to the inhibitory action of gastric acid secretion, when melatonin and helicobacter pylori inhibitor or gastric acid secretion inhibitor use in conjunction, melatonin can obviously improve its inhibitory action to ulcer.This unexpected discovery also sees the potentiation of L-tryptophan to other helicobacter pylori inhibitor or gastric acid secretion inhibitor.Therefore, the main component of pharmaceutical composition of the present invention is the associating of melatonin or L-tryptophan and any one (or more than one) helicobacter pylori inhibitor or any one (or more than one) gastric acid secretion inhibitor.Though also may play a role by other mechanism, removing oxygen-derived free radicals may be melatonin or the inhibiting basis of L-tryptophan performance ulcer.
It should be noted that the dosage that is tried less (draw azole drug only for clinical consumption 1/10th to 1/5th, for the class D medicine only be clinical consumption 1/20th to 1/7th), its side effect or toxic reaction will obviously reduce during clinical practice.Safer, effective, convenient than original medicine, thus better choice provided for effectively treating digestive system and ulcer.
The specific embodiment
Embodiment 1, tablet, and preparation method thereof
Composition weight (mg)
1. active component 100
Wherein, active component is metronidazole 20 and melatonin 80
2. microcrystalline Cellulose 45
3. pregelatinized Starch 43
④Na
2HPO
4 2
5. cross-linked pvp 4.5
6. PVPK
3010% aqueous solution QS QS
7. cross-linked pvp 4.0
8. magnesium stearate 1.5
The preparation manipulation process:
(1) will 2. 3. 4. 5. accurately take by weighing respectively, cross 100 mesh sieves 2 times, fully mixing.
(2) take by weighing again 1. according to the equivalent method of progressively increasing, add in 1 step common mixing.
(3) drip an amount of 6. 10%PVPK
30Aqueous solution is made suitable soft material, makes wet granular by nylon mesh.
(4) soft material is put into drying baker in 40 ℃ of oven dry, temperature control 12 hours.
(5) again 7. 8. add in the dried granule, mixing, tabletting, make the 200mg tablet.
Embodiment 2,
As described in embodiment 1, different is that active component is:
1) 60mg melatonin and 40mg penicillin; Or
2) 20mg melatonin and 80mg erythromycin; Or
3) 5mg melatonin, 25mg lansoprazole and 70mg cimetidine; Or
4) 5mg melatonin, 25mg lansoprazole and 70mg aluminium hydroxide; Or
5) 5mg melatonin, 70mg cimetidine and 25mg aluminium hydroxide;
6) 5mg melatonin, 15mg lansoprazole 60mg cimetidine and 20mg aluminium hydroxide.
Embodiment 3,
As described in embodiment 1, different is that active component is:
1) 15mg melatonin and 85mg erythromycin; Or
2) 35mg melatonin and 65mg rabeprazole; Or
3) 25mg melatonin and 75mg lafutidine; Or
4) 25mgL-tryptophan and 75mg famotidine; Or
5) 5mgL-tryptophan and 95mg roxatidine
Embodiment 4,
As described in embodiment 1, different is that active component is:
1) 15mg melatonin and 85mg amoxicillin; Or
2) 35mg melatonin and 65mg ampicillin; Or
3) 25mg melatonin and 75mg metronidazole; Or
4) 25mgL-tryptophan and 75mg furazolidone; Or
5) 5mgL-tryptophan and 95mg erythromycin; Or
6) 15mgL-tryptophan and 85mg erythromycin; Or
7) 25mgL-tryptophan and 75mg gentamycin; Or
8) 35mgL-tryptophan and 65mg tetracycline
Embodiment 5,
As described in embodiment 1, different is that active component is:
1) 15mg melatonin and 85mg lansoprazole; Or
2) 35mg melatonin and 65mg rabeprazole; Or
3) 25mg melatonin and 75mg Tenatoprazole; Or
4) 25mgL-tryptophan and 75mg pantoprazole; Or
5) 5mgL-tryptophan and 95mg S-omeprazole; Or
6) 15mgL-tryptophan and 85mg are for Nola's azoles; Or
7) 25mgL-tryptophan and 75mg dosmalfate; Or
8) 35mgL-tryptophan and 65mg sofalcone
Embodiment 6,
As described in embodiment 1, different is that active component is:
1) combination of 1 part of melatonin or L-tryptophan and 9 parts of penicillins, ampicillin, amoxicillin, metronidazole, furazolidone, erythromycin, erythromycin, gentamycin or tetracyclines; Or
2) combination of 2 parts of melatonin or L-tryptophan and 8 parts of cimetidine, lafutidine, famotidine or roxatidines; Or
3) combination of 2 parts of melatonin or L-tryptophan and 8 parts of aluminium hydroxide, magnesium hydroxide, sodium bicarbonate or calcium carbonate; Or
4) 2 parts of melatonin or L-tryptophan and 8 parts of lansoprazoles, rabeprazole, Tenatoprazole, pantoprazole, S-omeprazole, Lan Minuola azoles, for the combination of Nola's azoles, rabmprazole, leminoprazole, dosmalfate or sofalcone; Or
5) 2 parts of melatonin or L-tryptophan and 6 parts of cimetidine, lafutidine, famotidine or roxatidines and 2 parts of lansoprazoles, rabeprazole, Tenatoprazole, pantoprazole, S-omeprazole, Lan Minuola azoles, for the combination of Nola's azoles, rabmprazole, leminoprazole, dosmalfate or sofalcone.
Embodiment 7,150mg tablet
Composition weight (milligram)
Active component 45
Lactose 49.2
Starch 30
PVP 6
Microcrystalline Cellulose 18
Colloid silicon 1.2
Magnesium stearate 0.6
Total amount 150
Above-mentioned active component is respectively the combination among the embodiment 1-6.
The feasible where necessary Cotton seeds of tablet that the foregoing description 1-7 is made and granule is as sugar coating or gelatin etc.The preparation of embodiment 8, enteric coatel tablets
1000 consumptions of composition monolithic consumption (mg) (g)
Label: 1. active component 100 100
Wherein, active component is melatonin 35 and lansoprazole 65
2. microcrystalline Cellulose 54.5 54.5
3. pregelatinized Starch 34.5 34.5
④Na
2HPO
4 1.4 1.4
5. cross-linked pvp 4.6 4.6
6. PVPK
3010% aqueous solution QS QS
7. cross-linked pvp 4.0 4.0
8. magnesium stearate 1.0 1.0
Sealing coat: EH SL-S type
Enteric coating: EH ES-C type
The preparation manipulation process:
(1) 2. 3. 4. 5. accurately takes by weighing respectively, cross 100 mesh sieves 2 times, fully mixing.
(2) take by weighing again 1. according to the equivalent method of progressively increasing, add in 1 step common mixing.
(3) drip an amount of 6. PVPK
3010% aqueous solution is made suitable soft material, makes wet granular by nylon mesh.
(4) soft material is put into drying baker in 40 ℃ of oven dry, temperature control 12 hours.
(5) again 7. 8. add in the dried granule, mixing, tabletting, coating.
Embodiment 9
As described in embodiment 8, different is that active component is the combination among the embodiment 1-6.
The preparation of embodiment 10, oral capsule
Amounts of components (mg)
Active component 100
Wherein active component is lansoprazole 35 and rabeprazole 65
Lactose 100
Pregelatinated forms sediment 25
TC-5 20
Magnesium stearate 5
Total amount 250
(1) accurately takes by weighing above active ingredient and other dressing respectively, mix the back and dissolve with sodium hydrogen phosphate.
(2) using fluid bed drying after the soft material extrusion molding.
(3) granule of drying incapsulates.
The preparation method of oral capsule also can be made the capsule that contains the active ingredient of 50-100 milligram by other known technologies, makes the dosage form that 150-250mg does not wait.
Embodiment 11
As described in embodiment 10, different is that active component is the combination among the embodiment 1-6.
Injection can be made through traditional method.Effective ingredient of the present invention is mixed with pH regulator agent, buffer, stabilizing agent, solvent and analog thereof etc., make injection then according to a conventional method and be used for subcutaneous, muscle and intravenous fluid.Sustained-release preparation can be made through traditional method, and also slow-release auxiliary material such as available high molecular polymer is that holder is made various dosage forms.
Claims (7)
1. treatment treatment digestive ulcer medicament compositions is characterized in that said composition is the combination of the gastric acid secretion inhibitor of the helicobacter pylori inhibitor of melatonin or L-tryptophan and effective dose or effective dose.
2. treatment digestive ulcer medicament compositions as claimed in claim 1 is characterized in that the helicobacter pylori inhibitor is a kind of or its combination that is selected from penicillin, ampicillin, amoxicillin, metronidazole, furazolidone, erythromycin, erythromycin and analog thereof, gentamycin and the tetracycline.
3. treatment digestive ulcer medicament compositions as claimed in claim 1, it is characterized in that gastric acid secretion inhibitor is selected from cimetidine, lafutidine, famotidine, roxatidine, lansoprazole, rabeprazole, Tenatoprazole, pantoprazole, S-omeprazole, Lan Minuola azoles, replaces one of Nola's azoles, rabmprazole, leminoprazole, dosmalfate, sofalcone aluminium hydroxide, magnesium hydroxide, sodium bicarbonate or calcium carbonate or its combination.
4. treatment digestive ulcer medicament compositions as claimed in claim 1 is characterized in that the active component of said composition is:
The combination of (1) 1 part of melatonin or L-tryptophan and 9 parts of penicillins, ampicillin, amoxicillin, metronidazole, furazolidone, erythromycin, erythromycin, gentamycin or tetracyclines; Or
The combination of (2) 2 parts of melatonin or L-tryptophan and 8 parts of cimetidine, lafutidine, famotidine or roxatidines; Or
The combination of (3) 2 parts of melatonin or L-tryptophan and 8 parts of aluminium hydroxide, magnesium hydroxide, sodium bicarbonate or calcium carbonate; Or
(4) 2 parts of melatonin or L-tryptophan and 8 parts of lansoprazoles, rabeprazole, Tenatoprazole, pantoprazole, S-omeprazole, Lan Minuola azoles, for the combination of Nola's azoles, rabmprazole, leminoprazole, dosmalfate or sofalcone; Or
(5) 2 parts of melatonin or L-tryptophan and 6 parts of cimetidine, lafutidine, famotidine or roxatidines and 2 parts of lansoprazoles, rabeprazole, Tenatoprazole, pantoprazole, S-omeprazole, Lan Minuola azoles, for the combination of Nola's azoles, rabmprazole, leminoprazole, dosmalfate or sofalcone.
More than be weight percentage.
5. treatment digestive ulcer medicament compositions as claimed in claim 1 is characterized in that the main component of compositions is used to prepare the pharmaceutical preparation of treatment treatment gastric ulcer, duodenal ulcer, reflux esophagitis, Zollinger-Eillison syndrome, stomach and duodenitis.
6. treatment digestive ulcer medicament compositions as claimed in claim 5, it is characterized in that pharmaceutical preparation is oral formulations, be selected from powder, granule, tablet (coated tablet, effervescent tablet, slow releasing tablet), pill, capsule, electuary, powder, syrup, slow releasing agent, controlled release agent or slowbreak agent.
7. treatment digestive ulcer medicament compositions as claimed in claim 5 is characterized in that this pharmaceutical preparation is non-oral formulation, is selected from injection, suspensoid injectio, suppository, injectable microsphere, implant, slow releasing agent, controlled release agent or slowbreak agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510200782 CN1814289A (en) | 2005-12-09 | 2005-12-09 | Medicine composition for treating degestive ulcer |
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| CN 200510200782 CN1814289A (en) | 2005-12-09 | 2005-12-09 | Medicine composition for treating degestive ulcer |
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| CNA2007102011496A Division CN101138563A (en) | 2005-12-09 | 2005-12-09 | Pharmaceutical composition for treating peptic ulcer |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103083643A (en) * | 2008-03-27 | 2013-05-08 | 雀巢产品技术援助有限公司 | Methods for increasing absorption of peptides, peptidomimetics, and other gastrointestinal transport protein substrates |
| CN109431982A (en) * | 2018-11-27 | 2019-03-08 | 山西诺成制药有限公司 | A kind of cimetidine in sodium chloride injection production method preventing contaminant overstandard |
| CN109999027A (en) * | 2019-05-15 | 2019-07-12 | 扬州大学 | The new application of epiphysin |
| CN110711192A (en) * | 2018-07-12 | 2020-01-21 | 山东大学 | Use of tryptophan for enhancing gram-negative bacteria bactericidal effect |
-
2005
- 2005-12-09 CN CN 200510200782 patent/CN1814289A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103083643A (en) * | 2008-03-27 | 2013-05-08 | 雀巢产品技术援助有限公司 | Methods for increasing absorption of peptides, peptidomimetics, and other gastrointestinal transport protein substrates |
| CN103083643B (en) * | 2008-03-27 | 2015-01-07 | 雀巢产品技术援助有限公司 | Methods for increasing absorption of peptides, peptidomimetics, and other gastrointestinal transport protein substrates |
| CN110711192A (en) * | 2018-07-12 | 2020-01-21 | 山东大学 | Use of tryptophan for enhancing gram-negative bacteria bactericidal effect |
| CN109431982A (en) * | 2018-11-27 | 2019-03-08 | 山西诺成制药有限公司 | A kind of cimetidine in sodium chloride injection production method preventing contaminant overstandard |
| CN109999027A (en) * | 2019-05-15 | 2019-07-12 | 扬州大学 | The new application of epiphysin |
| CN109999027B (en) * | 2019-05-15 | 2022-01-28 | 扬州大学 | Use of melatonin |
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