CN102198131A - New compound preparation containing omeprazole - Google Patents
New compound preparation containing omeprazole Download PDFInfo
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- CN102198131A CN102198131A CN2010101307288A CN201010130728A CN102198131A CN 102198131 A CN102198131 A CN 102198131A CN 2010101307288 A CN2010101307288 A CN 2010101307288A CN 201010130728 A CN201010130728 A CN 201010130728A CN 102198131 A CN102198131 A CN 102198131A
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- omeprazole
- compound preparation
- preparation
- gastric
- gastric acid
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Abstract
The invention relates to a new compound preparation containing omeprazole, and the compound preparation is characterized by comprising omeprazole, dihydroxyaluminium aminoacetate, and pharmaceutical excipients. Wherein, dihydroxyaluminium aminoacetate has the direct effect of inhibiting gastric acid secretion and the function of preventing the degradation of omeprazole by gastric acid. Thus the preparation is reasonable in composition. When the preparation is taken, drug absorption is rapid, and a peak concentration can be reached rapidly, so that gastric acid can be effectively controlled. Compared with traditional omeprazole preparations added with sodium bicarbonate, the compound preparation provided in the invention has the characteristics of small dosage of gastric acid secretion inhibitor, lasting effect, no aerogenesis, and inabsorbability in the human body.
Description
Technical field
The present invention relates to field of medicaments, specifically, relate to a kind of new compound preparation that is prepared from through special process by omeprazole, dihydroxyaluminum aminoacetate and pharmaceutic adjuvant.
Background technology
Omeprazole (omeprazole, OME) act on the gastric mucosa parietal cell specifically, reduce the activity of the hydrogen potassium ATP enzyme in the parietal cell, thereby suppress basic gastric acid and stimulate the gastric acid secretion that causes, mainly be applicable to duodenal ulcer and Zollinger-Eillison syndrome, also can be used for gastric ulcer and reflux esophagitis.
Be deposited on after OME is oral in the gastric mucosa parietal cell, and specific effect suppresses its H-K-ATP enzyme (proton pump) activity in parietal cell, blocking-up gastric acid secretion end step, gastric acid inhibitory secretion.Research now, the best of taking medicine because of having a large amount of " active pump " to parallel with the OME absworption peak in the excitation period activation parietal cell after taking food, pressed down acid and acted on the strongest 30 minutes before the meal early morning.In the patient of OME treatment failure, have 75% to have " nocturnal acid breakthrough ", be evening 10 up at 5 o'clock next day gastric pH＜4 continue more than 60 minutes, the time of pH＞4 at night accounts for 51%, can bring up to 96% and add 20mgOME before sleeping, the gastric acid secretion amount is significantly reduced, be more conducive to gastric mucosa reparation and ulcer healing.
For the pharmacologically active after keeping OME to take, domestic listing product mostly is the stomach dissolution type preparation of enteric coated preparation or adding sodium bicarbonate at present.
Behind the OME enteric solubility preparation oral, target position changes, and onset time is slow, and because of the bioavailability difference of human body, the significance of difference of height is arranged; And the OME stomach dissolution type preparation of adding sodium bicarbonate is taken for a long time, and a large amount of retentions of metabolic alkalosis and sodium (causing hypokalemia) can take place, and is unfavorable to the patient that cardiorenal function is incomplete, and takes the preparation that contains sodium bicarbonate, and easily aerogenesis causes stomach discomfort.Therefore it is very necessary to seek a kind of OME compound preparation that can gastric solubleness can take and not contain carbonate again for a long time.
Summary of the invention
The present invention provides a kind of new compound preparation that is prepared from through special process by omeprazole, dihydroxyaluminum aminoacetate and pharmaceutic adjuvant to above-mentioned weak point.
The consumption of dihydroxyaluminum aminoacetate and with the ratio of omeprazole be key problem in technology of the present invention.Do not see research both at home and abroad for omeprazole/dihydroxyaluminum aminoacetate stomach dissolution type compound preparation.Reasonably the dose of dihydroxyaluminum aminoacetate can keep the suitable pH value of gastric, and this product of minute quantity is absorbed at the aluminum chloride that gastric is transformed into solubility, and from urine, drain, most of aluminium ion is combined into undissolved aluminum salt as phosphate, carbonate and soap at enteral, discharge from feces, can untoward reaction not arranged human body.This compound recipe has following advantage with sodium bicarbonate commonly used outside the dihydroxyaluminum aminoacetate subrogate country in a word: 1. antiacid effect is lasting; 2. astriction is arranged; 3. the mucous membrane protection effect is arranged; 4. do not produce CO
25. anacidity knock-on; 6. there is not alkalemia.
The compound preparation that omeprazole of the present invention is new takes following scheme to realize:
In the middle of the present invention, the dosage of the contained omeprazole of unit formulation: 5～40mg, containing dihydroxyaluminum aminoacetate dosage is 30～600mg; Omeprazole and dihydroxyaluminum aminoacetate best proportion are: 20mg/200～500mg and 40mg/200～500mg.
The consumption of the dihydroxyaluminum aminoacetate in the said components and with the ratio of omeprazole be key problem in technology of the present invention.After dihydroxyaluminum aminoacetate is taken, can keep the suitable pH value of gastric, this product of minute quantity is absorbed at the aluminum chloride that gastric is transformed into solubility, and from urine, drain, most of aluminium ion is combined into undissolved aluminum salt as phosphate, carbonate and soap at enteral, discharge from feces, can untoward reaction not arranged human body.
The present invention can make oral formulations commonly used.The used pharmaceutic adjuvant of the present invention comprises adjuvant commonly used such as starch, dextrin, lactose, sucrose, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose, cross-linking sodium carboxymethyl cellulose, mannitol, magnesium stearate etc.
The specific embodiment
Form by the following examples further specifies the present invention, but this should be interpreted as restriction of the present invention.The technology that all genus foregoing of the present invention is realized all belongs to scope of the present invention.
Embodiment one
Specification (1): omeprazole 20g, dihydroxyaluminum aminoacetate 500g, sucrose 500g, mannitol 100g, sodium carboxymethyl cellulose 10g;
Specification (2): omeprazole 40g, dihydroxyaluminum aminoacetate 500g, sucrose 500g, mannitol 100g, sodium carboxymethyl cellulose 10g;
Preparation method: take by weighing the supplementary material of recipe quantity according to preparation (1) and (2), cross 100 mesh sieves respectively, mix homogeneously, 1000 bags of packing promptly get dry suspension.
Instructions of taking, treatment duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome (gastrinoma), stress ulcer are taken a specification (1) dry suspension, each 1 bag every day; The treatment gastric ulcer is taken a specification (2) dry suspension every day, each 1 bag.
Embodiment two
Specification (1): omeprazole 20g, dihydroxyaluminum aminoacetate 300g, microcrystalline Cellulose 100g,, magnesium stearate 2g.
Specification (2): omeprazole 40g, dihydroxyaluminum aminoacetate 300g, microcrystalline Cellulose 100g,, magnesium stearate 2g.
Preparation method: take by weighing the supplementary material of recipe quantity according to preparation (1) and (2), cross 100 mesh sieves respectively, mix homogeneously, dry granulation, granulate adds magnesium stearate, tabletting, both tablet.
Instructions of taking, treatment duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome (gastrinoma), stress ulcer are taken (1) 1 of specification every day; The treatment gastric ulcer is taken (2) 1 of specifications every day.
Embodiment three
Specification (1): omeprazole 20g, dihydroxyaluminum aminoacetate 250g, starch 100g,, magnesium stearate 1g.
Specification (2): omeprazole 40g, dihydroxyaluminum aminoacetate 250g, starch 100g,, magnesium stearate 1g.
Preparation method: according to the recipe quantity of preparation (1) and (2), accurately take by weighing respectively, cross 100 mesh sieves, fully mixing; Granulate, granulate adds magnesium stearate, and the dress capsule had both got capsule.
Instructions of taking, treatment duodenal ulcer, reflux esophagitis, Zollinger-Ellison Syndrome (gastrinoma), stress ulcer are taken (1) 1 of specification every day; The treatment gastric ulcer is taken (2) 1 of specifications every day.
The preparation of omeprazole is more clinically at present, the compound preparation of U.S.'s listing in 2004 omeprazole and sodium bicarbonate, and the many families of domestic appearance are imitated.This product and its formation complementation can be satisfied the demand of different patients to omeprazole.
Claims (4)
1. compound preparation of being made up of omeprazole, dihydroxyaluminum aminoacetate and pharmaceutic adjuvant, wherein: the dosage of the contained omeprazole of unit formulation: 5 ~ 40mg, containing dihydroxyaluminum aminoacetate dosage is 30 ~ 600mg.
2. compound preparation according to claim 1, omeprazole and dihydroxyaluminum aminoacetate best proportion are: 20mg/200mg ~ 500mg and 40mg/200mg ~ 500mg.
3. compound preparation according to claim 1 is characterized in that making up routinely technology with pharmaceutically pharmaceutic adjuvant makes various oral formulations.
4. according to the omeprazole compound preparation of claim 1-3, said preparation has selectivity gastric acid secretion is had obvious inhibitory action, is applicable to gastric and duodenal ulcers, gastrointestinal disease such as reflux esophagitis, gastrinoma, stress ulcer, gastric ulcer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010101307288A CN102198131A (en) | 2010-03-24 | 2010-03-24 | New compound preparation containing omeprazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2010101307288A CN102198131A (en) | 2010-03-24 | 2010-03-24 | New compound preparation containing omeprazole |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102198131A true CN102198131A (en) | 2011-09-28 |
Family
ID=44659289
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2010101307288A Pending CN102198131A (en) | 2010-03-24 | 2010-03-24 | New compound preparation containing omeprazole |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102198131A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2173506C (en) * | 1993-10-12 | 2006-05-09 | Tomohisa Matsushita | Enteric granule-containing tablets |
| CN101002939A (en) * | 2007-01-12 | 2007-07-25 | 广东华南药业有限公司 | Medicine composition for treating diseases relating to gastric acid |
-
2010
- 2010-03-24 CN CN2010101307288A patent/CN102198131A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2173506C (en) * | 1993-10-12 | 2006-05-09 | Tomohisa Matsushita | Enteric granule-containing tablets |
| CN101002939A (en) * | 2007-01-12 | 2007-07-25 | 广东华南药业有限公司 | Medicine composition for treating diseases relating to gastric acid |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20110928 |