CN102942557A - Novel medicinal salt of dexlansoprazole - Google Patents
Novel medicinal salt of dexlansoprazole Download PDFInfo
- Publication number
- CN102942557A CN102942557A CN2012104868601A CN201210486860A CN102942557A CN 102942557 A CN102942557 A CN 102942557A CN 2012104868601 A CN2012104868601 A CN 2012104868601A CN 201210486860 A CN201210486860 A CN 201210486860A CN 102942557 A CN102942557 A CN 102942557A
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- China
- Prior art keywords
- lansoprazole
- ulcer
- dexlansoprazole
- magnesium
- medicinal salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- KLJYWVDAPALBKF-UHFFFAOYSA-N CC[N+]1(C)C2C(C)CC12 Chemical compound CC[N+]1(C)C2C(C)CC12 KLJYWVDAPALBKF-UHFFFAOYSA-N 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A novel medicinal salt of dexlansoprazole is represented as follows: x=0, 0.5, 1, 1.5, 2, 2.5 or 3; n=1, 2 or 3; and M= sodium, potassium, magnesium or zinc.
Description
Technical field
The present invention is the new pharmaceutical salts of R-lansoprazole, belongs to medical technical field.
Background technology
Lansoprazole is the medicine of novel gastric acid secretion inhibiting, it acts on the H+-K+-ATP enzyme of parietal cell, the H+ of parietal cell can not be transported in the stomach to be gone, so that the hydrochloric acid in gastric juice amount greatly reduces in the gastric juice, lansoprazole is because importing fluorine and the trifluoro ethoxy substituting group is arranged at 4 side chains of pyridine ring, make its bioavailability improve more than 30% than omeprazole, lipotropy also is better than omeprazole, therefore this product can promptly see through the parietal cell film and change sulfenic acid into and bring into play drug effect with inferior sulfonyl derivative under acidic conditions, the bacteriostatic activity of HP are risen to 4 times of omeprazole.Be used for clinically duodenal ulcer, stomach ulcer, reflux esophagitis, the treatment of Zuo-Ai (Zollinger-Ellison) syndrome (gastrinoma), evident in efficacy, helicobacter pylori there is restraining effect
R-lansoprazole is the enantiomorph of proton pump inhibitor lansoprazole, and its activity is higher than the R-lansoprazole of racemization, at present abroad listing, but bioavailability still is not very desirable, only has 48%.So how improving the bioavailability of R-lansoprazole and curative effect remains and needs further research.
Summary of the invention
The present invention is the new pharmaceutical salts of R-lansoprazole, and is as follows
x=0、0.5、1、1.5、2、2.5、3；
n=1、2、3；
M=sodium, potassium, magnesium, zinc.
The present invention also provides the preparation method of described compound.
The present invention also provides the pharmaceutical composition that comprises above-claimed cpd, and said composition contains the medicine acceptable carrier in case of necessity.Pharmaceutical composition of the present invention, can make any pharmaceutically useful formulation when making medicament, these formulations comprise: tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, suck agent, granule, powder, injection.Preparation of the present invention, oral dosage form preferably, as: granule, tablet, capsule, slow releasing tablet etc., more preferably tablet.
Can add the medicine acceptable carrier when being prepared into medicament, described medicine acceptable carrier can be: starch, sucrose, lactose, mannitol, silicon derivative, Mierocrystalline cellulose and derivative thereof, alginate, gelatin, polyvinylpyrrolidone, glycerine, POLYSORBATE 80, agar, calcium carbonate, Calcium hydrogen carbonate, tensio-active agent, polyoxyethylene glycol, cyclodextrin, beta-cyclodextrin, phospholipid material, kaolin, talcum powder, calcium stearate, Magnesium Stearate etc.
The present invention has also comprised and has stated the purposes of compound in preparation alimentary canal inflammation, digestive ulcer medicament.
Embodiment
Embodiment 1:
The preparation of R-lansoprazole sodium salt
Get R-lansoprazole 18.2g and be dissolved in the 60mL butanone, slowly drip the methanol solution (9.4mL) of 30% sodium methylate, reaction solution filters in stirred overnight at room temperature, solid butanone drip washing, and drying under reduced pressure obtains R-lansoprazole sodium 14.5g.
Embodiment 2:
The preparation of R-lansoprazole magnesium salts
Get the 0.24g MAGNESIUM METAL, join in the 18mL methyl alcohol, behind the adding catalytic amount methylene dichloride, stirring at room reaction to all MAGNESIUM METAL are converted into magnesium methylate.Above-mentioned suspension is joined among the methanol solution 150mL of 7.3g R-lansoprazole, after the stirring at room 30 minutes, filter, filtrate is poured in the 450mL methyl tertiary butyl ether, stirring at room is cooled to-10 ° of C and stirred 1 hour, filters the solid of separating out, methyl tertiary butyl ether is washed, and vacuum-drying obtains R-lansoprazole magnesium 6.1g.
Embodiment 3: effect experiment
1. experiment modeling:
Fasting feedwater 24h before 60 rat modelings, etherization in the cover+beaker cotton balls nose appends anesthesia, the tincture of iodine, alcohol routine disinfection, the xiphoid-process Ventral Midline 2～2.5cm that hits separates abdominal muscle, cuts off peritonaeum, gently move to stomach outside the abdomen, at the stomach facies ventralis, body of stomach and pyloric antrum intersection thrust 0.4～0.5mm under the serous coat with microsyringe is flat, inject 1O Glacial acetic acid 0.1mL, form papule, stomach is sent back to, sew up abdominal muscle, skin.
2. experimental technique:
30 rats are divided into 3 groups at random: blank model group, R-lansoprazole group, R-lansoprazole sodium group, R-lansoprazole magnesium group.Beginning administration in the 3rd day after the modeling, each group is all by 3mL/ (100g.d) gavage, and blank model group is to equal-volume physiological saline, and each organizes equal every day 1 time, totally 4 weeks.Modeling 3d (before the administration), l7d (administration l4d), 3ld (administration 28d) minute 3 batches of execution rats, cut off the abdominal cavity along ventrimeson, take out stomach, cut off along greater gastric curvature, clean with the ice normal saline flushing. gastric mucosa is flattened on flat board, with the maximum major diameter of vernier caliper measurement ulcer and vertical maximum wide footpath. ulcer index (uI) is measured major diameter and the widest footpath of ulcer with vernier callipers, multiply each other and calculate ulcer area as ulcer index, ulcer area: S=1/4 * DL * DS * π, DL refers to the ulcer major diameter in the formula, DS refers to the ulcer minor axis, and π gets 3.14.
3. experimental result:
Can find out that from the result each administration group all can effectively reduce ulcer area, wherein remarkable with R-lansoprazole sodium, the effect of magnesium salts group, prompting will can increase its availability and antiulcer curative effect behind the R-lansoprazole salify.
Each organize rat ulcer index (mm2) and ulcer inhibition rate comparison (
N=10)
Claims (4)
1. the new pharmaceutical salts of R-lansoprazole is as follows
x=0、0.5、1、1.5、2、2.5、3；
n=1、2、3；
M=sodium, potassium, magnesium, zinc.
2. the preparation method of the described compound of claim 1.
3. with the medicinal compositions of the described compound of claim 1.
4. the described arbitrary compound of claim 1-3 is characterized in that: the purposes in preparation alimentary canal inflammation, digestive ulcer medicament.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104868601A CN102942557A (en) | 2012-11-26 | 2012-11-26 | Novel medicinal salt of dexlansoprazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104868601A CN102942557A (en) | 2012-11-26 | 2012-11-26 | Novel medicinal salt of dexlansoprazole |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102942557A true CN102942557A (en) | 2013-02-27 |
Family
ID=47725573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012104868601A Pending CN102942557A (en) | 2012-11-26 | 2012-11-26 | Novel medicinal salt of dexlansoprazole |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102942557A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1306375A1 (en) * | 2000-08-04 | 2003-05-02 | Takeda Chemical Industries, Ltd. | Salts of benzimidazole compound and use thereof |
| CN101716176A (en) * | 2009-12-21 | 2010-06-02 | 扬子江药业集团上海海尼药业有限公司 | R-lansoprazole for injection and preparation method thereof |
-
2012
- 2012-11-26 CN CN2012104868601A patent/CN102942557A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1306375A1 (en) * | 2000-08-04 | 2003-05-02 | Takeda Chemical Industries, Ltd. | Salts of benzimidazole compound and use thereof |
| CN101716176A (en) * | 2009-12-21 | 2010-06-02 | 扬子江药业集团上海海尼药业有限公司 | R-lansoprazole for injection and preparation method thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20130227 |
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| WD01 | Invention patent application deemed withdrawn after publication |