CN101455629A - Oral solid preparation containing omeprazole - Google Patents
Oral solid preparation containing omeprazole Download PDFInfo
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- CN101455629A CN101455629A CNA2008101603462A CN200810160346A CN101455629A CN 101455629 A CN101455629 A CN 101455629A CN A2008101603462 A CNA2008101603462 A CN A2008101603462A CN 200810160346 A CN200810160346 A CN 200810160346A CN 101455629 A CN101455629 A CN 101455629A
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- omeprazole
- sodium bicarbonate
- oral solid
- tablet
- sodium
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Abstract
The present invention relates to an oral solid preparation which comprises omeprazole. The oral solid preparation is a stomach dissolved rapid release preparation which is composed of omeprazole, antacid sodium bicarbonate and medical supplementary materials. The sodium bicarbonate can increase pH value in the stomach. The omeprazole which is extraordinarily unstable to acid is not degraded by acid. Therefore the preparation according to the invention can quicken the onset time of omeprazole without being prepared into enteric-coated preparation. The dosage ratio between omeprazole and sodium bicarbonate can keep a reasonable medicine-taking dosage of sodium bicarbonate thereby keeping a proper pH value in the stomach and reducing the adverse effect of sodium bicarbonate.
Description
Technical field
The present invention relates to contain the oral solid formulation of omeprazole, the stomach dissolution type quick releasing formulation of forming by omeprazole, antacid sodium bicarbonate and pharmaceutic adjuvant.
Background technology
Omeprazole (omeprazole) is a benzimidazole proton pump inhibitors, can suppress parietal cell film inner proton pump (H
+, K
--ATP enzyme system), make the H in the cell wall
+Can not be transported in the gastric juice and go, thereby performance suppresses the effect of gastric secretion.It has been widely used in treating gastric ulcer, duodenal ulcer, reflux esophagitis, gastrinoma etc.
Omeprazole is alkalescence (Pka=4), and oral back is absorbed in small intestinal.Omeprazole is stabilizer pole under neutral and meta-alkalescence condition, and the half-life reaches 17 hours; Easily degraded under sour environment is when pH is then very unstable during near gastric acidity (pH=1), the half-life is about 2 minutes.
For the pharmacologically active after keeping omeprazole to take; the omeprazole of present domestic listing is enteric coated preparation mostly; generally be omeprazole to be made micropill carry out enteric coating again, or omeprazole packed in the enteric hollow capsule that the protection omeprazole exempts from stomach acids destroy.
Omeprazole enteric-coated preparation has delayed the initial inhibitory action of omeprazole to gastric acid, generally just reaches absworption peak at 2～4 hours blood drug level in oral back, and the back of taking medicine average onset time is 2..5～8 hour.
Dong Hengjin has measured the onset time (" the healthy people's of three kinds of omeprazole capsules bioavailability and to the influence of 24 hours pH value of gastric " of three kinds of enteric coated capsulees, the 38th the 8th phase of volume of " CHINESE JOURNAL OF INTERNAL MEDICINE " August in 1999: 533～536 pages), preceding 3 groups of experimenters, the 24 hourly average pH value of medication are 2.26; Take medicine back average onset time from being losec capsule (2.5 ± 0.5) hour, omeprazole capsule (6.1 ± 2.8) hour successively near slow order and omeprazole capsule (8.1 ± 0.1) hour, and statistical test shows that difference has highly significant between each group; The stomach inner pH value rate of climb is fast behind the oral 40mg losec capsule, and rising to pH value on average needs 2.5 hours more than 4.
Summary of the invention
The present invention is intended to sodium bicarbonate as acid inhibitor, and stomach inner pH value when improving the omeprazole stripping prepares a kind of stomach dissolution type quick releasing formulation of omeprazole.
In omeprazole stomach dissolution type quick releasing formulation of the present invention, the consumption of sodium bicarbonate and with the ratio of omeprazole be key problem in technology of the present invention.Reasonably the sodium bicarbonate dose can keep the suitable pH value of gastric, and reduces the untoward reaction that sodium bicarbonate causes.
The domestic research of not seeing for sodium bicarbonate consumption in omeprazole/sodium bicarbonate stomach dissolution type quick releasing formulation.Patent publication No. CN101120930A invents described omeprazole/sodium bicarbonate preparation and still is the enteric solubility preparation, can not solve omeprazole onset problem slowly.Invent in the described omeprazole quick-release preparation at patent publication No. CN101002769A, not the scope and the optimum thereof of the amount ranges of clear and definite sodium bicarbonate, sodium bicarbonate and omeprazole ratio.
Sodium bicarbonate is a weakly basic drugs, and its oral formulations is mainly used in hyperchlorhydria at present clinically, the gastric acid that neutralization is superfluous.Sodium bicarbonate is soluble in water, in and the gastric acid effect fast, can alleviate stimulation and the corrosion of gastric acid to ulcer surface, alleviate the pylorospasm pain due to the hyperchlorhydria, peracid ulcer is had temporary transient analgesic effect, and using at the Peptic Ulcers outbreak initial stage has symptomatic treatment usefulness faster; Under its oral formulations is obeyed when acute gastritis, chronic gastritis acute attack play pain or before the pain.
But sodium bicarbonate also can stimulate pylorus secretion gastrin simultaneously, and prolonged application can cause the Secondary cases gastroxia, and consumption is big to reduce pepsin activity even complete deactivation indirectly; And sodium bicarbonate can increase intragastric pressure, causes symptoms such as abdominal distention, heating installation, stomach discomfort, and because flatulence stimulates ulcer surface, serious ulcer is had the danger of bringing out perforation.Therefore, the dose of sodium bicarbonate should have certain restriction.The sodium bicarbonate sheet of China's approval listing, its oral dose are each 0.3～1 grams, and every day 3 times, use must not be above 7 days continuously.
In the present invention, the dosage of the contained omeprazole of unit formulation is 5～40mg, the dosage that contains sodium bicarbonate is 550～1680mg, omeprazole/sodium bicarbonate best proportion be: 20mg/1100mg～20mg/1680mg and 40mg/1100mg～40mg/1680mg.When taking preparation of the present invention, can not only convert dose (can not replace 1 preparation that contain omeprazole 40mg) with 2 preparations that contain omeprazole 20mg by the amount of the contained omeprazole of unit formulation, and should be according to take the dose that the sodium bicarbonate amount is not higher than the principle conversion omeprazole of 1680mg at every turn.
The present invention can be made into following stomach dissolution type dosage form: hard capsule, tablet, dispersible tablet, oral cavity disintegration tablet, chewable tablet, buccal tablet, effervescent tablet, granule, dry suspension, powder, used adjuvant comprises dextrin, hypromellose, PVP, starch, sodium carboxymethyl cellulose, lactose, xylitol, mannitol, sucrose, microcrystalline Cellulose, carboxymethyl starch sodium, xanthan gum, magnesium stearate, micropowder silica gel, Pulvis Talci, essence, sucralose, saccharin sodium, stevioside etc.
The present invention 1 hour ante cibum oral after, the peak time of omeprazole is about 30min, stomach inner pH value rises within 30min, onset time is far above omeprazole enteric-coated preparation.
The specific embodiment
The specific embodiment of form is described further foregoing of the present invention by the following examples, but this should be interpreted as that the above-mentioned subject area of the present invention closely is limited to following examples.Allly belong to the technology that foregoing of the present invention realizes and all belong to scope of the present invention.
Embodiment one
Specification (1): omeprazole 10g, sodium bicarbonate 550g, microcrystalline Cellulose 34g, magnesium stearate 6g;
Specification (2): omeprazole 20g, sodium bicarbonate 550g, microcrystalline Cellulose 24g, magnesium stearate 6g;
Preparation method: according to the recipe quantity of preparation (1) and (2), omeprazole, sodium bicarbonate, microcrystalline Cellulose and magnesium stearate are crossed 100 mesh sieves respectively, mix homogeneously carries out the capsule fill, makes 1000 hard capsules.
Instructions of taking: treatment duodenal ulcer, gastroesophageal reflux disease, gastroesophageal reflux disease, erosive esophagitis, take a specification (1) capsule every day, each 2; The treatment gastric ulcer is taken a specification (2) capsule every day, each 2.
Embodiment two
Specification (1): omeprazole 20g, sodium bicarbonate 1680g, sodium carboxymethyl cellulose 600g, hypromellose 700g, essence 8g, saccharin sodium 8g, magnesium stearate 8g;
Specification (2): omeprazole 40g, sodium bicarbonate 1680g, sodium carboxymethyl cellulose 600g, hypromellose 700g, essence 8g, saccharin sodium 8g, magnesium stearate 8g.
Preparation method: according to the recipe quantity of preparation (1) and (2), omeprazole, sodium bicarbonate, microcrystalline Cellulose and magnesium stearate are crossed 100 mesh sieves respectively, mix homogeneously is made 1000 bags of dry suspension.
Instructions of taking: treatment duodenal ulcer, gastroesophageal reflux disease, gastroesophageal reflux disease, erosive esophagitis, take a specification (1) dry suspension every day, each 1 bag; Treatment gastric ulcer and prevention critical patient gastrorrhagia are taken a specification (2) dry suspension every day, each 1 bag.
Embodiment three
Specification (1): omeprazole 20g, sodium bicarbonate 1680g, dextrin 600g, essence 8g, saccharin sodium 8g, magnesium stearate 8g;
Specification (2): omeprazole 40g, sodium bicarbonate 1680g, dextrin 600g, essence 8g, saccharin sodium 8g, magnesium stearate 8g.
Preparation method: according to the recipe quantity of preparation (1) and (2), omeprazole, sodium bicarbonate, microcrystalline Cellulose and magnesium stearate are crossed 100 mesh sieves respectively, mix homogeneously is that adhesive is granulated with the alcoholic solution, 70 ℃ of oven dry, and granulate is made 1000 bags of granules.
Instructions of taking: treatment duodenal ulcer, gastroesophageal reflux disease, gastroesophageal reflux disease, erosive esophagitis, take a specification (1) granule every day, each 1 bag; Treatment gastric ulcer and prevention critical patient gastrorrhagia are taken a specification (2) granule every day, each 1 bag.
Claims (5)
1, a kind of oral solid formulation that contains omeprazole is made up of omeprazole, sodium bicarbonate and pharmaceutic adjuvant.It is characterized in that: the dosage of the contained omeprazole of unit formulation is 5～40mg, and the dosage that contains sodium bicarbonate is 550～1680mg.
2, according to the described oral solid formulation of claim 1, omeprazole/sodium bicarbonate best proportion be: 20mg/1100mg～20mg/1680mg and 40mg/1100mg～40mg/1680mg.
3,, it is characterized in that can be made into following stomach dissolution type fast dissolving dosage form: hard capsule, tablet, dispersible tablet, oral cavity disintegration tablet, chewable tablet, buccal tablet, effervescent tablet, granule, dry suspension, powder according to the described oral solid formulation of claim 1.
4, according to the described oral solid formulation of claim 1, it is characterized in that: used adjuvant comprises dextrin, hypromellose, PVP, starch, sodium carboxymethyl cellulose, lactose, xylitol, mannitol, sucrose, microcrystalline Cellulose, carboxymethyl starch sodium, xanthan gum, magnesium stearate, micropowder silica gel, Pulvis Talci, essence, sucralose, saccharin sodium, stevioside etc.
5, according to the described oral solid formulation of claim 1, it is characterized in that when taking, can not only converting dose (can not replace 1 preparation that contain omeprazole 40mg) with 2 preparations that contain omeprazole 20mg by the amount of the contained omeprazole of unit formulation, and should be according to take the dose that the sodium bicarbonate amount is not higher than the principle conversion omeprazole of 1680mg at every turn.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101603462A CN101455629A (en) | 2008-11-17 | 2008-11-17 | Oral solid preparation containing omeprazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101603462A CN101455629A (en) | 2008-11-17 | 2008-11-17 | Oral solid preparation containing omeprazole |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101455629A true CN101455629A (en) | 2009-06-17 |
Family
ID=40766928
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008101603462A Pending CN101455629A (en) | 2008-11-17 | 2008-11-17 | Oral solid preparation containing omeprazole |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101455629A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101816641A (en) * | 2010-03-11 | 2010-09-01 | 沈阳亿灵医药科技有限公司 | Omeprazole quick-release solid preparation and preparation method thereof |
| CN102641286A (en) * | 2012-03-12 | 2012-08-22 | 南京海纳医药科技有限公司 | Compound omeprazole dry suspension and preparation method thereof |
| CN102688196A (en) * | 2012-05-21 | 2012-09-26 | 杭州华东医药集团生物工程研究所有限公司 | Omeprazole pellets and preparation method thereof |
| CN115444832A (en) * | 2021-06-09 | 2022-12-09 | 长春澜江医药科技有限公司 | Pharmaceutical composition containing omeprazole magnesium and preparation thereof |
-
2008
- 2008-11-17 CN CNA2008101603462A patent/CN101455629A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101816641A (en) * | 2010-03-11 | 2010-09-01 | 沈阳亿灵医药科技有限公司 | Omeprazole quick-release solid preparation and preparation method thereof |
| CN101816641B (en) * | 2010-03-11 | 2012-04-04 | 沈阳亿灵医药科技有限公司 | Omeprazole quick-release solid preparation and preparation method thereof |
| CN102641286A (en) * | 2012-03-12 | 2012-08-22 | 南京海纳医药科技有限公司 | Compound omeprazole dry suspension and preparation method thereof |
| CN102688196A (en) * | 2012-05-21 | 2012-09-26 | 杭州华东医药集团生物工程研究所有限公司 | Omeprazole pellets and preparation method thereof |
| CN115444832A (en) * | 2021-06-09 | 2022-12-09 | 长春澜江医药科技有限公司 | Pharmaceutical composition containing omeprazole magnesium and preparation thereof |
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Open date: 20090617 |