CN101269074A - Pharmaceutical composition containing right-handed rebeprazole and preparation method thereof - Google Patents
Pharmaceutical composition containing right-handed rebeprazole and preparation method thereof Download PDFInfo
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- CN101269074A CN101269074A CNA2008101065169A CN200810106516A CN101269074A CN 101269074 A CN101269074 A CN 101269074A CN A2008101065169 A CNA2008101065169 A CN A2008101065169A CN 200810106516 A CN200810106516 A CN 200810106516A CN 101269074 A CN101269074 A CN 101269074A
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Abstract
The invention relates to a drug compound containing D-rabeprazole and the preparation method thereof. The drug compound is prepared by adopting D-rabeprazole as the main active ingredient and mixing with auxiliary ingredients acceptable in pharmacy. The drug compound can be made into any solid formulations, such as tablets, capsules, granules, dispersible tablets, chewable tablets, buccal tablets, effervescent tablets, effervescent granules and so on, wherein, the unit preparation content of D-rabeprazole is 2 to 40mg and 10 to 20mg is preferable. The drug compound of the invention containing D-rabeprazole can be used for treating various types of digestive tract diseases, in particular peptic ulcers.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition that contains dextral-rabeprazole and preparation method thereof, it is to be that main active is mixed formation with pharmaceutically acceptable adjuvant with the dextral-rabeprazole, belongs to medical technical field.
Background technology
The chemical structural formula of rabeprazole is as follows
In actual applications, we often adopt its pharmaceutical salts, and how common is sodium salt and potassium salt.RABEPRAZOLE SODIUM belongs to the medicine of secretion inhibitor, is the succedaneum of benzimidazole, no anticholinergic and anti-H2 histamine characteristic, but can be attached to the parietal cell surface by suppressing the secretion that the H+/K+-ATP enzyme comes gastric acid inhibitory.This enzyme system is counted as sour proton pump, so the generation that RABEPRAZOLE SODIUM blocks gastric acid as the proton pump inhibitor of gastric, this effect is a dosage correlation.Animal experiment confirmation RABEPRAZOLE SODIUM can be discharged from blood plasma and gastric mucosa after medication soon.
Rabeprazole comprises left-handed and two kinds of optical isomers of dextrorotation, and actual employed active component is the racemic mixture of two kinds of optical isomers.But experiment shows the pharmacological action of rabeprazole dextroisomer and wants obviously strong and laevoisomer and raceme thereof.Its dextroisomer minimum effective dose is little than raceme, and metabolic half life is long, can obviously improve the generation of curative effect and reduction toxicity.
Its dextroisomer structure is as follows
A pharmaceutical research shows: the effect of dextral-rabeprazole obviously is better than levo form and raceme in the ulcer rat model that acetic acid causes, experimental result is as (table 1)
Table 1 respectively organize rat ulcer index (mm2) and ulcer inhibition rate comparison (mean ± SD, n=15)
Also be at present the research of pharmacology and pharmacodynamics aspect, also not relevant for the research of preparation prescription for the research of dextral-rabeprazole.
Summary of the invention
The present invention relates to a kind of pharmaceutical composition that contains dextral-rabeprazole and preparation method thereof, it is to be that main active is mixed the compositions that forms with pharmaceutically acceptable adjuvant with the dextral-rabeprazole.Wherein dextral-rabeprazole comprises the acceptable slaine of itself and its or its hydrate.Said composition can be made various oral formulations as required, comprise any solid dosage formss such as tablet, capsule, granule, dispersible tablet, chewable tablet, buccal tablet, effervescent tablet, effervescent granule, wherein the unit formulation content of dextral-rabeprazole is 2-40mg, preferred 10-20mg.
Compositions of the present invention can be used for treating various digestive tract disease, in particular for peptic ulcer.
The specific embodiment
By following examples pharmaceutical composition that contains dextral-rabeprazole of the present invention and preparation method thereof is described further, but is not limited in this.
Embodiment 1 dextral-rabeprazole tablet
Prescription:
Preparation method:
Dextral-rabeprazole, microcrystalline Cellulose are crossed 80 mesh sieves respectively, and mix homogeneously joins 50% alcoholic solution in the mixed powder, the system soft material, 24 mesh sieves are granulated, drying, 20 mesh sieve granulate, add micropowder silica gel, CMS-Na, adopt suitable punch die compressed tablets behind the mix homogeneously, promptly.
If carry out coating for above-mentioned tablet, then obtain coated tablet, can be Film coated tablets, enteric coatel tablets etc.
Embodiment 2: the dextral-rabeprazole capsule
Prescription:
Preparation method:
Dextral-rabeprazole, starch are all crossed 80 mesh sieves, progressively increase behind the method mix homogeneously, add magnesium stearate according to equivalent, mix homogeneously, packing, promptly.
Used capsule shells can be conventional capsule, also can be enteric coated capsule.
Embodiment 3: the dextral-rabeprazole chewable tablet
Prescription:
Preparation method:
Supplementary materials such as dextral-rabeprazole, xylitol, mannitol are crossed 80 mesh sieves respectively, adopt equivalent incremental method mix homogeneously, add the 2%PVP-k30 alcoholic solution, the system soft material, 16 mesh sieves are granulated, drying, 20 mesh sieve granulate, the correctives, sweeting agent, the fluidizer mix homogeneously that add other, tabletting, promptly.
Embodiment 4: the dextral-rabeprazole dispersible tablet
Prescription
Preparation method:
Supplementary materials such as dextral-rabeprazole, microcrystalline Cellulose are crossed 80 mesh sieves respectively, adopt equivalent incremental method mix homogeneously, standby; Add 75% alcoholic solution, the system soft material, 16 mesh sieves are granulated, drying, 20 mesh sieve granulate add other correctives orange flavor, sweeting agent stevioside, fluidizer micropowder silica gel, mix homogeneously such as disintegrating agent PPVP, L-HPC, tabletting, promptly.
Embodiment 5: the dextral-rabeprazole effervescent tablet
Prescription
Preparation method:
Dextral-rabeprazole is crossed 80 mesh sieves, mix homogeneously; Get half mixed powder amount, with the citric acid mix homogeneously, with 50% alcoholic solution system soft material, 18 orders are granulated, drying, 16 order granulate; Get the surplus mixed powder again, mix with sodium carbonate, sodium bicarbonate, the same method is granulated; Two kinds of granules of gained mix, and add other adjuvant, and as mix homogeneously such as PEG6000, orange flavor, acesulfame potassium, sodium chloride, tabletting promptly.
Embodiment 6: the dextral-rabeprazole granule
Prescription
Preparation method:
Dextral-rabeprazole, mannitol, sorbitol were waited 80 mesh sieves, mix homogeneously; With the 75% alcoholic solution system soft material of 5%PVPk-30,16 orders are granulated, drying, and 12 order granulate add other adjuvant, and as mix homogeneously such as orange flavor, acesulfame potassiums, packing is promptly.
Embodiment 7
7.1. experimental technique: effect experiment
Go into to organize patient's 116 examples, male 72 examples, women 44 examples, age 22-54 year, average 36 years old.Upper abdominal pain 88 examples wherein, hunger property pain 42 examples, abdominal distention 79 examples, acid regurgitation 64 examples, singultus 53 examples, 46 examples of feeling sick are vomitted 38 examples, melena 32 examples, course of disease elder is 2 years, weak point person is 3 months.Have 83 examples to find all that through endoscopy ulcer exists among the 116 routine patients, the ulcer diameter accounts for the above person of 67%, 2～3cm at 1cm with interior person and takes second place; Form is ellipse garden, lamellar and map shape and changes; Visible gastric mucosa congestion, edema, erosion under the mirror; Periphery neatly or is put in order, and mostly is fester, and minority is a circumferential ridges, the dark ulcer of concavity.116 routine patients are divided into A group 54 examples at random and B organizes 62 examples.A group rabeprazole 20mg, the B group is used dextral-rabeprazole 20mg, is early decoction being taken at a draught before the meal, and the treatment phase is 7w; Afterwards for consolidating and the prevention of recurrence phase.The 8th～10w dose reduces by half; Administration is 1 time next day of the 10th～13w.
7.2 experimental result:
Curative effect determinate standard: ulcer is pressed Sakita endoscopic classification method by stages.Gastroscope check and pathological examination, ulcer are just calculated recovery from illness reaching complete epithelization.Total symptom is decided to be the disappearance that has two or more ulcer symptoms and sign at least or obviously alleviates notes down: as stomachache, abdominal distention, feel sick, vomiting, acid regurgitation, heating installation, poor appetite.Symptom and sign were obviously alleviated by complete obiteration in 0 fen in 1 minute, 2 fens basic alleviations, and no significant change in 3 fens is kept the score.The results are shown in Table 2
Table 2 liang group therapeutic outcome (%)
Claims (6)
1. the present invention relates to a kind of pharmaceutical composition that contains dextral-rabeprazole, it is characterized in that, is to be that main active is mixed the compositions that forms with pharmaceutically acceptable adjuvant with the dextral-rabeprazole.
2. the described compositions of claim 1 is characterized in that, dextral-rabeprazole comprises the acceptable slaine of itself and its or its hydrate.
3. the described compositions of claim 1 is characterized in that, can make oral formulations.
4. the described compositions of claim 3 is characterized in that, oral formulations comprises any solid dosage formss such as tablet, capsule, granule, dispersible tablet, chewable tablet, buccal tablet, effervescent tablet, effervescent granule.
5. the described compositions of claim 1 is characterized in that, the unit formulation content of dextral-rabeprazole is 2-40mg, preferred 10-20mg.
6. the described compositions of claim 1 is used for the treatment of digestive tract disease, is preferred for peptic ulcer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008101065169A CN101269074A (en) | 2008-05-14 | 2008-05-14 | Pharmaceutical composition containing right-handed rebeprazole and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2008101065169A CN101269074A (en) | 2008-05-14 | 2008-05-14 | Pharmaceutical composition containing right-handed rebeprazole and preparation method thereof |
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| CN101269074A true CN101269074A (en) | 2008-09-24 |
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| CNA2008101065169A Pending CN101269074A (en) | 2008-05-14 | 2008-05-14 | Pharmaceutical composition containing right-handed rebeprazole and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101836984A (en) * | 2009-03-17 | 2010-09-22 | 北京利乐生制药科技有限公司 | Dextral-rabeprazole-magnesium-containing pharmaceutical preparation and preparation method thereof |
-
2008
- 2008-05-14 CN CNA2008101065169A patent/CN101269074A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101836984A (en) * | 2009-03-17 | 2010-09-22 | 北京利乐生制药科技有限公司 | Dextral-rabeprazole-magnesium-containing pharmaceutical preparation and preparation method thereof |
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Open date: 20080924 |