CN101869709A - Composite of peptic ulcer resisting medicaments and preparation method thereof - Google Patents

Composite of peptic ulcer resisting medicaments and preparation method thereof Download PDF

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CN101869709A
CN101869709A CN 201010206305 CN201010206305A CN101869709A CN 101869709 A CN101869709 A CN 101869709A CN 201010206305 CN201010206305 CN 201010206305 CN 201010206305 A CN201010206305 A CN 201010206305A CN 101869709 A CN101869709 A CN 101869709A
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sodium
peptic ulcer
acid
compositions
medicament
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杨进明
王德武
莫国飞
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Guangxi Fanglue Pharmaceutical Group Co Ltd
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Guangxi Fanglue Pharmaceutical Group Co Ltd
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Abstract

The invention discloses a composite of peptic ulcer resisting medicaments and a preparation method thereof, wherein troxipide as an active component and other peptic ulcer resisting medicaments form a composite preparation, and the weight ratio of troxipide and other peptic ulcer resisting medicaments is 1:0.05-1:50. The composite preparation can be used for treating gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux diseases, functional dyspepsia diseases and the like. The invention provides the composite preparation which is superior to single medicament, has good therapeutic effect and consists of troxipide and other peptic ulcer resisting medicaments.

Description

A kind of composition and method of making the same of medicament for resisting peptic ulcer
Technical field
The present invention relates to a kind of drug combination preparation, the composite preparation that especially a kind of troxipide is formed with other medicament for resisting peptic ulcer respectively.
Background technology
Troxipide (Troxipide claims troxipide again) is a novel defense factor and enhancement mode gastritis, gastric ulcer therapeutic agent.Be used for the treatment of gastric ulcer and can improve acute gastritis and the gastric mucosal lesion of chronic gastritis acute attack stage (rotten to the corn, hemorrhage, rubescent, edema) etc.Its Its Mechanisms is shown it and proton pump inhibitor and H 2-receptor antagonist difference does not have influence to gastric acid secretion, but strengthens the defense factor of the anti-damage ability of gastric mucosa, promotes the reparation at gastric ulcer position.Up to the present, do not see the report and the patent of the combination preparation of troxipide and other any medicines in the prior art as yet.
Proton pump inhibitor (PPI) is H +-K +-atpase inhibitor, its mechanism of action are that the final stage that gastric acid inhibitory forms (suppresses the proton pump of gastric mucosa parietal cell, promptly suppresses H +-K +The activity of-ATP enzyme), thus powerful and gastric acid inhibitory secretion enduringly.For acid basis secretion and cause that gastric acid secretion does not all have influence due to the different stimulated that gastric acid forms, this product is rapid-action, effect is lasting, take once and can reversibly control gastric acid secretion every day, and its persistent period can reach 24 hours.Proton pump inhibitor is used for gastric ulcer, duodenal ulcer, anti-fluidity esophagitis, Zollinger-Ellison syndrome and gastrinoma etc.On behalf of medicine, proton pump inhibitor mainly have: azoles, rabeprazole, Ai Suomeila azoles, Tenatoprazole, tenooprazole, rabmprazole, leminoprazole and Lan Minuola azoles and their pharmaceutical salts are drawn in lansoprazole, companion's holder.
H 2-receptor antagonist the mechanism of action is for passing through blocking-up H 2-receptor, thereby the secretion of gastric acid inhibitory.Histamine H 2-receptor is positioned on the film of parietal cell bottom side, activates the H of parietal cell behind the receptor activation by second message,second messenger in the born of the same parents +-K +-ATP enzyme, secretion gastric acid.On behalf of medicine, the H2-receptor antagonist mainly have: cimetidine, ranitidine, famotidine, roxatidine and nizatidine and their pharmaceutical salts.
The mechanism of action of gastric mucosa protectant is to form firm protective by colloid property on gastric mucosa, and by bismuth ion the killing action of helicobacter pylori is brought into play antiulcer action.On behalf of medicine, gastric mucosa protectant mainly have: teprenone, bismuth citrate ranitidine, bismuth potassium citrate, bismuth aluminate, bismuth citrate, salicylic acid bismuth, Bismuth tartrate., colloidal bismmth pectin and sucralfate.
Antacid mostly is alkaline matter, its mechanism of action be in and gastric acid, reduce the stimulation of gentle and gastric acid to stomach.The main representative medicine of antacid has: sodium bicarbonate, sodium carbonate, sodium citrate, sodium acetate, sodium tartrate, calcium bicarbonate, Citric acid calcium, hydrotalcite, aluminum carbonic acid, aluminium hydroxide, aluminum magnesium hydroxide, the coprecipitated thing of aluminium hydroxide/sodium bicarbonate, magnesium oxide, magnesium hydroxide, calcium carbonate, calcium lactate, calcium hydroxide, calcium gluconate, Citric acid calcium, calcium phosphate and Calcium d-tartrate.
Peptic Ulcers is a kind of common chronic systemic disease, is divided into gastric ulcer and duodenal ulcer, is called peptic ulcer again.Why it is referred to as peptic ulcer, be because think that previously gastric ulcer and duodenal ulcer are because gastric acid and pepsin are formed to the mucosa autodigestion, in fact gastric acid and pepsin are the one of the main reasons of ulcer, also have other reasons can form Peptic Ulcers.Because the cause of disease and the clinical symptoms of gastric ulcer and duodenal ulcer have many similarities, it is gastric ulcer or duodenal ulcer that the doctor is difficult to distinguish sometimes, therefore often is diagnosed as peptic ulcer, or stomach, duodenal ulcer.If the clear and definite ulcer of energy is at stomach or duodenum, that just can directly be diagnosed as gastric ulcer or duodenal ulcer.
Gastritis is the inflammation of gastric mucosa, according to the order of severity of mucosa injury, gastritis can be divided into erosive gastritis and non-erosive gastritis, also can classify according to the position that stomach involves (as cardia, body of stomach, gastric antrum).According to the type of inflammatory cell, on the histology, gastritis can be further divided into acute gastritis and chronic gastritis.Acute gastritis shows as the neutrophil infiltration of cardia and body of stomach mucosa.Chronic gastritis often has atrophy (mucosa loss of function) to a certain degree and changes and give birth to, and often involves cardia, reduces with forfeiture of G cell and gastrin secretion, also can involve body of stomach, and the forfeiture with secreting acid gland causes gastric acid, the minimizing of pepsin and endogenous factors.
Reflux esophagitis and functional dyspepsia (FD) are common functional gastrointestinal disorders, and its sickness rate is higher, account for more than 1/3 of special outpatient clinic of digestion.Wherein, gastroesophageal reflux (GER) can be divided into physiological and pathologic, and physiological GER often occurs in when having meal daytime or after having meal, mainly is of short duration lower esophageal sphincter (LES) hypotension institute.Anti-reflux barrier function reduce, esophagus reduces the ability of cleaning up of anti-stream thing and (or) when gastric emptying is subjected to obstacle, physiological GER can develop into pathologic GER, cause gastric content even duodenal juice to blow back into esophagus through cardia, infringement esophagus mucosa, cause struvite changes such as hyperemia, erosion, and then develop into reflux esophagitis.Think at present in the pathogenesis of esophagitis, it is main paathogenic factor that the barrier function of the reduction of LES function, esophagus mucosa destroys, gastric acid or other harmful substances such as duodenal juice, bile, pancreatic juice then are the main components of infringement esophagus mucosa, thereby, it also is important virulence factor that gastric emptying causes the anti-duodenal juice that flows, bile etc. unusually, facilitates gastro oesophageal reflux disease (GORD) by above-mentioned multiple factor.
Patient's indigestion symptom of functional dyspepsia (FD) is obvious, and prolonged and repeated outbreak, even feels more serious than the patient of chronic gastritis, peptic ulcer, and the treatment difficulty is big, has a strong impact on patient's work and quality of life.Think that at present its morbidity is main relevant with gastrointestinal motility disorder, also there are problems such as gastric acid secretion increases, HP infection, Nervous and Mental Factors in part patient, so general first-selected short digestive tract power reinforcing medicine is gone up in treatment, and not positive to the treatment of the application of antacid and gastritis, peptic ulcer.
The inventor finds troxipide not only can be produced Synergistic with omeprazole effect in finishing invention " treatment digestion disease pharmaceutical composition and preparation method thereof " process (CN101513404A), and respectively with proton pump inhibitor, H 2The drug regimen of-receptor antagonist, gastric mucosa protectant and antacid also can be produced the effect of Synergistic.Particularly respectively with proton pump inhibitor, H 2The composite preparation of-receptor antagonist, gastric mucosa protectant and antacid; come gastroenteropathys such as therapeutic alliance gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux disease, functional dyspepsia, in particular for controlling single proton pump inhibitor or H 2-receptor antagonist is failed gastric ulcer, the duodenal ulcer stomach function regulating esophagus reflux disease of effectively treatment.
Up to the present, in the prior art, except that the inventor's CN101513404A patent of invention, do not see the compositions of the medicine of any use troxipide and other anti-peptic ulcer as yet.The inventor is in research process, and accident has been found the composite preparation of the medicine of troxipide and other anti-peptic ulcer, can produce the effect of Synergistic, and curative effect is better than single drug, and clinical use is had bigger meaning.Therefore, the inventor has finished the present invention for this reason.
Summary of the invention
The purpose of this invention is to provide and a kind ofly be better than that single drug, therapeutic effect are better, short treating period, composite preparation that effective percentage is high, the said composition preparation comprise troxipide respectively with the pharmaceutical composition and the pharmaceutic adjuvant of other anti-peptic ulcer.
The medicine of other anti-peptic ulcer promptly is proton pump inhibitor, H 2-receptor antagonist, gastric mucosa protectant and antacid.
Troxipide of the present invention respectively with the pharmaceutical composition of other anti-peptic ulcer, its active component troxipide is 1 with the drug weight ratio of other anti-peptic ulcer: 0.05-1: 50.
On the other hand, the troxipide that the present invention also provides treatment to go up effective dose is gone up the composite preparation of other medicament for resisting peptic ulcer of effective dose respectively with treatment, the said composition preparation is used for the treatment of the purposes in the medicine of gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux disease, functional dyspepsia.
In composite preparation of the present invention, troxipide is a novel defense factor and enhancement mode gastritis, gastric ulcer therapeutic agent.Be used for the treatment of gastric ulcer and can improve acute gastritis and the gastric mucosal lesion of chronic gastritis acute attack stage (rotten to the corn, hemorrhage, rubescent, edema) etc.Oral post-absorption and distribution are rapid, and the elimination half-life is longer, Tmax=2.33 ± 0.52h; Cmax=1.07 ± 0.36mg/L; AUC0 → int=9.38 ± 1.74h.mg/L; T 1/2=12.52 ± 3.69h.Physiological disposition meets linear kinetics.Mainly be distributed in small intestinal after the absorption, be followed successively by liver, kidney, lung, spleen etc.The bioavailability of its former liquid medicine solution is 99.6 ± 7.3% relatively.Its Its Mechanisms is shown it and proton pump inhibitor, H 2-receptor antagonist, gastric mucosa protectant and antacid are different, and gastric acid is alleviated in gastric acid secretion, protection gastric mucosa and neutralization does not have influence, but strengthen the defense factor of the anti-damage ability of gastric mucosa, promote the reparation at gastric ulcer position.Therefore, troxipide can be respectively and proton pump inhibitor, H 2-receptor antagonist, gastric mucosa protectant and antacid combination, and the effect that produces Synergistic.
When using troxipide of the present invention and come therapeutic alliance gastric ulcer, duodenal ulcer with the composite preparation of the medicine of other anti-peptic ulcer respectively, the medicine of other anti-peptic ulcer is secretion (proton pump inhibitor and the H of gastric acid inhibitory 2-receptor antagonist) or protection gastric mucosa (gastric mucosa protectant) or neutralization alleviate gastric acid (antacid); and troxipide is for strengthening the defense factor of the anti-damage ability of gastric mucosa; the reparation as early as possible of this ulcer spot will be promoted; the The combined medication will complement one another; Synergistic; strengthen the treatment gastric ulcer, duodenal ulcer is acute and the curative effect of chronic gastritis, gastroesophageal reflux disease, functional dyspepsia, curative effect obviously is better than single drug.
In composite preparation of the present invention, the active component troxipide may be mixed together with the medicine of other anti-peptic ulcer respectively, and adds pharmaceutic adjuvant, makes various peroral dosage forms, for example tablet, capsule, granule, suspensoid or oral liquid also can be made injection.And tablet can be conventional tablet, enteric coatel tablets, double-layer tablet, slow releasing tablet, dispersible tablet, oral cavity disintegration tablet, effervescent tablet, chewable tablet.Capsule can be conventional capsule, enteric coated capsule, slow releasing capsule, soft capsule.Injection can be to be injectable powder, lyophilized injectable powder and injection.Granule can be plain particles and effervescent granule.
Among the present invention, proton pump inhibitor can be that azoles, rabeprazole, Ai Suomeila azoles, Tenatoprazole, tenooprazole, rabmprazole, leminoprazole and Lan Minuola azoles and their pharmaceutical salts are drawn in lansoprazole, companion's holder.
Among the present invention, H 2-receptor antagonist can be cimetidine, ranitidine, famotidine, roxatidine and/or nizatidine.
Among the present invention, gastric mucosa protectant can be teprenone, bismuth citrate ranitidine, bismuth potassium citrate, bismuth aluminate, bismuth citrate, salicylic acid bismuth, Bismuth tartrate., colloidal bismmth pectin and/or sucralfate.
Among the present invention, antacid can be sodium bicarbonate, sodium carbonate, sodium citrate, sodium acetate, sodium tartrate, calcium bicarbonate, Citric acid calcium, hydrotalcite, aluminum carbonic acid, aluminium hydroxide, aluminum magnesium hydroxide, the coprecipitated thing of aluminium hydroxide/sodium bicarbonate, magnesium oxide, magnesium hydroxide, calcium carbonate, calcium lactate, calcium hydroxide, calcium gluconate, Citric acid calcium, calcium phosphate and/or Calcium d-tartrate.
Among the present invention, adjuvant is for being one or more compositions in filler, binding agent, lubricant, disintegrating agent, slow releasing agent, isoosmotic adjusting agent, the stabilizing agent.
Among the present invention, filler is for being but being not limited to lactose, fructose, glucose, sucrose, mannitol, aspartame, stevioside, saccharin sodium, microcrystalline Cellulose, sodium carboxymethyl cellulose, carbomer, sorbitol, xylitol, maltose alcohol, erythritol, starch and/or pregelatinized Starch.Preferred filler comprises lactose, microcrystalline Cellulose, fructose, glucose, sucrose, mannitol, aspartame, pre-gel starch or its mixture.
Among the present invention, binding agent is for being but being not limited to gelatin, arabic gum, guar gum, xanthan gum, hydroxypropyl emthylcellulose, polyvinylpyrrolidone, ethyl cellulose, dextrin, starch, Polyethylene Glycol, chitosan, maltodextrin, modified starch, pectin, carrageenan and poloxamer or its mixture etc., preferably polyethylene ketopyrrolidine, starch, poloxamer or its mixture.
Among the present invention, lubricant is for being but being not limited to magnesium stearate, stearic acid, calcium stearate, sodium stearyl fumarate, colloidality silicon dioxide and Talcum or its mixture; Preferred lubricant comprises magnesium stearate, stearic acid, Talcum or its mixture.
Among the present invention, disintegrating agent can be but be not limited to corn starch, crospolyvinylpyrrolidone, starch base sodium acetate, hydroxyethyl-cellulose, ethyl cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, amylum pregelatinisatum, microcrystalline Cellulose sodium, alginic acid, alginic acid sodium salt, compressibility sorbitol and carboxymethylcellulose calcium or its mixture; Preferred disintegrating agent comprises corn starch, sodium starch glycolate, hydroxyethyl-cellulose, carboxymethyl starch sodium, amylum pregelatinisatum, alginic acid, carboxymethylcellulose calcium or its mixture.
Among the present invention, coating materials can be but be not limited to hydroxypropyl methylcellulose, stomach dissolution type Opadry, enteric solubility Opadry, transparent type Opadry, acrylic resin, the strange L-100 of You Te, the strange S-100 of You Te, the strange L-100-55 of You Te, the strange L-30D-55 of You Te and the strange E-100 of You Te.Preferred coating materials comprises stomach dissolution type Opadry, enteric solubility Opadry, transparent type Opadry, acrylic resin, the strange L-100 of You Te, the strange S-100 of You Te.
Among the present invention, slow releasing agent can be but be not limited to hydroxypropyl methylcellulose, methylcellulose, cellulose acetate, ethyl cellulose, hydroxyethyl-cellulose, hydroxyl second formic acid cellulose acetate, stearic acid, tristerin, Brazil wax, octadecanol, Synthetic Spermacet, hexadecanol.Preferred slow releasing agent comprises hydroxypropyl methylcellulose, ethyl cellulose, tristerin.
Among the present invention, isoosmotic adjusting agent only is used for injection, and isoosmotic adjusting agent can be but be not limited to sodium chloride, sodium bicarbonate, sodium dihydrogen phosphate, calcium chloride, sodium lactate, calcium lactate, glucose and/or xylitol; Preferred isoosmotic adjusting agent comprises sodium chloride, sodium bicarbonate glucose.
Among the present invention, isoosmotic adjusting agent only is used for injection, and stabilizing agent can be but be not limited to the sodium salt of sodium salt, succinic acid and succinic acid of sodium salt, malonic acid, the malonic acid of sodium salt, ethylenediamine tetrapropionic acid, the ethylenediamine tetrapropionic acid of ethylenediaminetetraacetic acid, ethylenediaminetetraacetic acid; Preferred stabilizing agent comprises sodium salt, the ethylenediamine tetrapropionic acid of ethylenediaminetetraacetic acid, ethylenediaminetetraacetic acid, the sodium salt of ethylenediamine tetrapropionic acid.
The advantage of composite preparation of the present invention is to use conveniently, once take or shot administration simultaneously, and the effect of this administering drug combinations is better than individually dosed, obvious to effects such as treatment gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux disease, functional dyspepsias, be particularly useful for controlling single proton pump inhibitor or H 2-receptor antagonist or gastric mucosa protectant or antacid are failed the gastric ulcer, duodenal ulcer stomach function regulating esophagus reflux disease etc. of effectively treatment.
Below, explain the present invention in conjunction with specific embodiments.Following embodiment is used to further specify the present invention, but does not limit the scope of the invention.
Specific embodiments
Embodiment 1
Azoles sodium enteric tablet (every contains active component troxipide 100mg and draws azoles sodium 20mg with companion's holder) is drawn in troxipide companion holder, and its prescription is:
Concrete preparation method: the raw material and the adjuvant of above recipe quantity are crossed 80 mesh sieves respectively, standby.
The companion who crosses 80 mesh sieves is held in the palm the method mixing that draws azoles and microcrystalline Cellulose, lactose and crospovidone to adopt equivalent to progressively increase.With an amount of 5% starch slurry system soft material, granulate with 18 mesh sieves.Drying is 3 hours under 50 ℃.With 20 mesh sieve granulate.The magnesium stearate mixing, tabletting makes label, and is standby.
The strange L-100 of You Te, Pulvis Talci and the triethyl citrate of crossing 80 mesh sieves are added respectively in the ethanol of recipe quantity, stirred 45 minutes, make enteric coating liquid, standby.
Label is put into coating pan, 30 rev/mins of rotating speeds, the sheet bed tempertaure is controlled at 40-50 ℃, uses the enteric coating liquid spray coating.After having wrapped, under 50 ℃ of following dryings 1 hour, make ECT, standby.
Troxipide and the Opadry of crossing 80 mesh sieves are added respectively in the water of recipe quantity, stirred 45 minutes, make the medicine-feeding coating solution, standby.
ECT is put into coating pan, 30 rev/mins of rotating speeds, the sheet bed tempertaure is controlled at 40-50 ℃, uses medicine coating solution spray coating.After having wrapped, under 50 ℃ of following dryings 1 hour, make the medicine-feeding coated tablet, standby.
The Opadry of crossing 80 mesh sieves is added in the water of recipe quantity, stirred 45 minutes, make film coating liquid, standby.
The intestinal coated tablet of adding medicine to is put into coating pan, and 30 rev/mins of rotating speeds, sheet bed tempertaure are controlled at 40-50 ℃, with film coating liquid spray coating.After having wrapped, under 50 ℃ of following dryings 1 hour, check, packing, finished product.
Embodiment 2
Troxipide Lansoprazole sustained-release capsule (every contains active component troxipide 300mg and lansoprazole 30mg), its prescription is:
Figure BSA00000175510500071
Concrete preparation method: the HPMC-E6 of recipe quantity is added in the Aquacoat, be diluted with water to solid content and be 10% aqueous dispersion, stirred 30 minutes, make sustained release coating liquid, standby.
Celphere is put into coating pan, and 30 rev/mins of rotating speeds, sheet bed tempertaure are controlled at 45-55 ℃, with sustained release coating liquid spray coating, when the coating weightening finish is 8%, stop coating.With slow-release micro-pill under 50 ℃ of following dryings 1 hour, make the troxipide slow-release micro-pill, standby.
The strange L-100 of You Te, Pulvis Talci and the triethyl citrate of crossing 80 mesh sieves are added respectively in the ethanol of recipe quantity, stirred 45 minutes, make enteric coating liquid, standby.
Celphere is put into coating pan, 30 rev/mins of rotating speeds, the sheet bed tempertaure is controlled at 45-55 ℃, uses the enteric coating liquid spray coating, when the coating weightening finish is 25%, stops coating.With enteric coated micropill under 50 ℃ of following dryings 1 hour, make the Lansoprazole intestine micropill, standby.
With troxipide slow-release micro-pill and Lansoprazole intestine micropill mix homogeneously, filled capsules, check, packing get finished product.
Embodiment 3
Troxipide bismuth potassium citrate double-layer tablet (every contains active component troxipide 100mg and bismuth potassium citrate 300mg), its prescription is:
Figure BSA00000175510500081
Concrete preparation method: the raw material and the adjuvant of above recipe quantity are crossed 80 mesh sieves respectively, standby.
With cross 80 mesh sieves troxipide, lactose, microcrystalline Cellulose and crospovidone mixing even.With an amount of 5% starch slurry system soft material, granulate with 18 mesh sieves.Drying is 3 hours under 50 ℃.With 20 mesh sieve granulate.Magnesium stearate, mixing makes troxipide layer granule, and is standby.
Bismuth potassium citrate, lactose, microcrystalline Cellulose and the crospovidone mixing of crossing 80 mesh sieves is even.With an amount of 5% starch slurry system soft material, granulate with 18 mesh sieves.Drying is 3 hours under 50 ℃.With 20 mesh sieve granulate.Magnesium stearate, mixing makes bismuth potassium citrate layer granule, and is standby.
Troxipide layer granule, bismuth potassium citrate layer granule are pressed into double-layer tablet.Check, packing get finished product.
Embodiment 4
Troxipide hydrotalcite capsule (every contains active component troxipide 100mg and hydrotalcite 500mg), its prescription is:
Composition The mg/ sheet
Troxipide ?100
Hydrotalcite ?500
Concrete preparation method: the raw material of above recipe quantity is crossed 80 mesh sieves respectively, standby.
Capsule is filled: will cross the troxipide and the hydrotalcite mix homogeneously of 80 mesh sieves, and filled capsules, check, packing get finished product.
Embodiment 5
Troxipide sodium bicarbonate particle (every bag contains active component troxipide 100mg and sodium bicarbonate 1100mg), its prescription is:
Composition The mg/ sheet
Troxipide ??100
Sodium bicarbonate ??1100
Lactose ??300
Mannitol ??200
Aspartame ??5
5% starch slurry In right amount
Concrete preparation method: the raw material and the adjuvant of above recipe quantity are crossed 80 mesh sieves respectively, standby.
With cross 80 mesh sieves troxipide, sodium bicarbonate, lactose, mannitol and aspartame mixing even.With an amount of 5% starch slurry system soft material, granulate with 8 mesh sieves.Drying is 3 hours under 50 ℃.With the screening of 8-60 mesh sieve, collect the granule of 8-60 mesh sieve, pack.Check, packing get finished product.
Embodiment 6
Troxipide aluminium hydroxide dry suspension (every bag contains active component troxipide 100mg and aluminium hydroxide 300mg), its prescription is:
Composition The mg/ sheet
Troxipide ?100
Aluminium hydroxide ?300
Mannitol ?200
Sodium carboxymethyl cellulose ?30
Aspartame ?5
Concrete preparation method: the raw material and the adjuvant of above recipe quantity are crossed 80 mesh sieves respectively, standby.
With cross 80 mesh sieves troxipide, aluminium hydroxide, mannitol, sodium carboxymethyl cellulose and aspartame mixing even, pack.Check, packing get finished product.
Embodiment 7
Azoles sodium (every bottle contains active component troxipide 100mg and draws azoles sodium 20mg with companion's holder) is drawn in injection troxipide companion holder, and its prescription is:
Composition The mg/ sheet
Troxipide ?100
Azoles sodium is drawn in companion's holder ?20
Mannitol ?100
Sodium ethylene diamine tetracetate ?1
Sodium chloride ?10
Sodium hydroxide In right amount
Concrete its preparation method is: the troxipide, the companion's holder that take by weighing recipe quantity draw azoles sodium, mannitol and sodium ethylene diamine tetracetate, sodium chloride that it is dissolved in the proper amount of water for injection, and the control temperature stirs about 50 ℃ and makes its dissolving; The sodium hydroxide solution that adds 0.1mol/L is regulated pH value and is about 11.5, adds the active carbon of 0.1% (W/V) again, be incubated 20 minutes, coarse filtration is taken off charcoal, adds to the full amount of water for injection, mixing is measured content and pH value, qualified after, with 0.22 μ m filtering with microporous membrane, fill false add plug is put lyophilization in the freeze drying box under 100 grades of environment, the tamponade outlet, roll lid, after the assay was approved the lamp inspection decals.
Embodiment 8
The clinical effectiveness evaluation that the azoles enteric coatel tablets are drawn in troxipide companion holder
Take embodiment 1 product, 2 times on the one oral this product are treated single omeprazole enteric-coated capsules or ranitidine capsule and are failed the effectively gastroesophageal reflux disease of treatment, according to clinical observation, total effective rate is 89.5%, and the sick healing rate that decreases of gastroscope check mucous membrane of esophagus is respectively 84.2%; 2 times on the one oral this product, the treatment functional dyspepsia, according to clinical observation, total effective rate is 92.4%.
Embodiment 9
The clinical effectiveness evaluation of troxipide bismuth potassium citrate double-layer tablet
Take embodiment 3 products, 3 times on the one oral this product are treated single bismuth potassium citrate capsule and are failed the effectively duodenal ulcer of treatment, and according to clinical observation, total effective rate is 91.6%; 3 times on the one oral this product are treated single bismuth potassium citrate and are failed the effectively acute gastritis of treatment, according to clinical observation, and total effective rate 91.7%.
Embodiment 10
The capsular clinical effectiveness evaluation of troxipide hydrotalcite
Take embodiment 4 products, 3 times on the one oral this product are treated single hydrotalcite sheet and are failed the effectively gastric ulcer of treatment, and according to clinical observation, total cure rate is 91.4%.3 times on the one oral this product are treated single hydrotalcite sheet and are failed the effectively duodenal ulcer of treatment, and according to clinical observation, total cure rate is 93.7%.

Claims (16)

1. the compositions of a medicament for resisting peptic ulcer, it is characterized in that: comprise troxipide respectively with the medicine of other anti-peptic ulcer and the compositions of acceptable accessories, the medicine of described other anti-peptic ulcer is: proton pump inhibitor (PPI), H 2-receptor antagonist, gastric mucosa protectant and antacid, the weight ratio of the medicine of the ulcer of troxipide and other anti-digestion is 1: 0.05-1: 50.
2. the compositions of medicament for resisting peptic ulcer as claimed in claim 1, it is characterized in that: described proton pump inhibitor is: azoles, rabeprazole, Ai Suomeila azoles, Tenatoprazole, tenooprazole, rabmprazole, leminoprazole and/or Lan Minuola azoles and their pharmaceutical salts are drawn in lansoprazole, companion's holder.
3. the compositions of medicament for resisting peptic ulcer as claimed in claim 1, it is characterized in that: described H2-receptor antagonist is: cimetidine, ranitidine, famotidine, roxatidine and/or nizatidine and their pharmaceutical salts.
4. the pharmaceutical composition of the anti-digestive ulcer of troxipide as claimed in claim 1 is characterized in that: described gastric mucosa protectant is: teprenone, bismuth citrate ranitidine, bismuth potassium citrate, bismuth aluminate, bismuth citrate, salicylic acid bismuth, Bismuth tartrate., colloidal bismmth pectin and/or or sucralfate.
5. the compositions of medicament for resisting peptic ulcer as claimed in claim 1, it is characterized in that: described antacid is: sodium bicarbonate, sodium carbonate, sodium citrate, sodium acetate, sodium tartrate, calcium bicarbonate, Citric acid calcium, hydrotalcite, aluminum carbonic acid, aluminium hydroxide, aluminum magnesium hydroxide, the coprecipitated thing of aluminium hydroxide/sodium bicarbonate, magnesium oxide, magnesium hydroxide, calcium carbonate, calcium lactate, calcium hydroxide, calcium gluconate, Citric acid calcium, calcium phosphate and/or Calcium d-tartrate.
6. the compositions of medicament for resisting peptic ulcer as claimed in claim 1, it is characterized in that: described adjuvant is pharmaceutical carrier that can be compatible, and this pharmaceutical carrier is one or more compositions in filler, binding agent, lubricant, disintegrating agent, coating materials, slow releasing agent, isoosmotic adjusting agent, the stabilizing agent.
7. the compositions of medicament for resisting peptic ulcer as claimed in claim 6 is characterized in that: described filler be selected from as in next group material one or more: lactose, fructose, glucose, sucrose, mannitol, aspartame, stevioside, saccharin sodium, microcrystalline Cellulose, sodium carboxymethyl cellulose, carbomer, sorbitol, xylitol, maltose alcohol, erythritol, starch and pregelatinized Starch.
8. the compositions of medicament for resisting peptic ulcer as claimed in claim 6 is characterized in that: described binding agent be selected from as in next group material one or more: gelatin, arabic gum, guar gum, xanthan gum, hydroxypropyl emthylcellulose, polyvinylpyrrolidone, ethyl cellulose, dextrin, starch, Polyethylene Glycol, chitosan, maltodextrin, modified starch, pectin, carrageenan and poloxamer.
9. the pharmaceutical composition of the anti-digestive ulcer of troxipide as claimed in claim 6 is characterized in that: described lubricant be the choosing be taken from as next the group material in one or more: magnesium stearate, stearic acid, calcium stearate, sodium stearyl fumarate, colloidality silicon dioxide and Pulvis Talci.
10. the compositions of medicament for resisting peptic ulcer as claimed in claim 6 is characterized in that: described disintegrating agent be choosing be taken from as in next group material one or more: corn starch, crospolyvinylpyrrolidone, sodium starch glycolate, hydroxyethyl-cellulose, ethyl cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose, amylum pregelatinisatum, microcrystalline Cellulose sodium, alginic acid, alginic acid sodium salt, compressibility sorbitol and carboxymethylcellulose calcium.
11. the compositions of medicament for resisting peptic ulcer as claimed in claim 6 is characterized in that: described coating materials be the choosing be taken from as next the group material in one or more: hydroxypropyl methylcellulose, stomach dissolution type Opadry, enteric solubility Opadry, transparent type Opadry, acrylic resin, the strange L-100 of You Te, the strange S-100 of You Te, the strange L-100-55 of You Te, the strange L-30D-55 of You Te and the strange E-100 of You Te.
12. the compositions of medicament for resisting peptic ulcer as claimed in claim 6 is characterized in that: described slow releasing agent be selected from as next the group material in one or more: hydroxypropyl methylcellulose, methylcellulose, cellulose acetate, ethyl cellulose, hydroxyethyl-cellulose, hydroxyl second formic acid cellulose acetate, stearic acid, tristerin, Brazil wax, octadecanol, Synthetic Spermacet, hexadecanol.
13. the compositions of medicament for resisting peptic ulcer as claimed in claim 6, it is characterized in that: described grade is oozed adjustment and only is used for injection, isoosmotic adjusting agent be selected from as next the group material in one or more: sodium chloride, sodium bicarbonate, sodium dihydrogen phosphate, calcium chloride, sodium lactate, calcium lactate, glucose and xylitol.
14. the compositions of medicament for resisting peptic ulcer as claimed in claim 6, it is characterized in that: described stabilizing agent only is used for injection, and stabilizing agent is selected from as one or more the material of next group in the material: the sodium salt of the sodium salt of the sodium salt of the sodium salt of ethylenediaminetetraacetic acid, ethylenediaminetetraacetic acid, ethylenediamine tetrapropionic acid, ethylenediamine tetrapropionic acid, malonic acid, malonic acid, succinic acid and succinic acid.
15. the compositions of medicament for resisting peptic ulcer as claimed in claim 1 is characterized in that: the said composition preparation can be made following dosage form: tablet, enteric coatel tablets, double-layer tablet, slow releasing tablet, dispersible tablet, oral cavity disintegration tablet, effervescent tablet, chewable tablet, capsule, enteric coated capsule, slow releasing capsule, soft capsule, granule, effervescent granule, dry suspension, oral liquid and injection.
16. the compositions of medicament for resisting peptic ulcer as claimed in claim 1 is characterized in that: the said composition preparation is used for the treatment of the application of gastric ulcer, duodenal ulcer, acute and chronic gastritis, gastroesophageal reflux disease and functional dyspepsia disease medicament.
CN 201010206305 2010-06-23 2010-06-23 Composite of peptic ulcer resisting medicaments and preparation method thereof Pending CN101869709A (en)

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Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102552257A (en) * 2010-12-21 2012-07-11 北大方正集团有限公司 Compound preparation containing ranitidine hydrochloride and troxipide and application thereof
CN102885851A (en) * 2012-10-12 2013-01-23 西安新通药物研究有限公司 Drug for treating diarrhea
CN104146155A (en) * 2014-08-08 2014-11-19 北京英惠尔生物技术有限公司 Coating material as well as preparation method and application thereof
CN106038585A (en) * 2016-05-27 2016-10-26 郑州思辩科技有限公司 Colloidal bismuth pectin tablets and preparation method thereof
CN106420801A (en) * 2016-12-08 2017-02-22 董振龙 Oral liquid preparation containing sodium bicarbonate for quickly relieving gastroesophageal reflux clinical symptoms
US20170095507A1 (en) * 2014-08-17 2017-04-06 Shanxi Zhendong Ante Biopharmaceutical Co., Ltd. Dispersion preparation containing colloidal bismuth pectin and preparing method therefor
CN113082188A (en) * 2021-04-28 2021-07-09 重庆市畜牧科学院 Preparation method of veterinary drug for resisting gastrointestinal inflammation
CN114344327A (en) * 2021-12-24 2022-04-15 大连大学 Application of pH response gastric mucosa protective agent
CN116459222A (en) * 2023-04-20 2023-07-21 山东中医药大学附属医院 Pivelum bromide composition, preparation and application thereof

Citations (1)

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CN101513404A (en) * 2009-04-02 2009-08-26 广西方略药业集团有限公司 Medicament compound for treating digestive disease and the method for preparing the same

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101513404A (en) * 2009-04-02 2009-08-26 广西方略药业集团有限公司 Medicament compound for treating digestive disease and the method for preparing the same

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102552257A (en) * 2010-12-21 2012-07-11 北大方正集团有限公司 Compound preparation containing ranitidine hydrochloride and troxipide and application thereof
CN102885851A (en) * 2012-10-12 2013-01-23 西安新通药物研究有限公司 Drug for treating diarrhea
CN104146155A (en) * 2014-08-08 2014-11-19 北京英惠尔生物技术有限公司 Coating material as well as preparation method and application thereof
US20170095507A1 (en) * 2014-08-17 2017-04-06 Shanxi Zhendong Ante Biopharmaceutical Co., Ltd. Dispersion preparation containing colloidal bismuth pectin and preparing method therefor
CN106038585A (en) * 2016-05-27 2016-10-26 郑州思辩科技有限公司 Colloidal bismuth pectin tablets and preparation method thereof
CN106420801A (en) * 2016-12-08 2017-02-22 董振龙 Oral liquid preparation containing sodium bicarbonate for quickly relieving gastroesophageal reflux clinical symptoms
CN113082188A (en) * 2021-04-28 2021-07-09 重庆市畜牧科学院 Preparation method of veterinary drug for resisting gastrointestinal inflammation
CN114344327A (en) * 2021-12-24 2022-04-15 大连大学 Application of pH response gastric mucosa protective agent
CN116459222A (en) * 2023-04-20 2023-07-21 山东中医药大学附属医院 Pivelum bromide composition, preparation and application thereof

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Application publication date: 20101027