CN101390857A - Medicine composition containing lansoprazole - Google Patents
Medicine composition containing lansoprazole Download PDFInfo
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- CN101390857A CN101390857A CN 200710122134 CN200710122134A CN101390857A CN 101390857 A CN101390857 A CN 101390857A CN 200710122134 CN200710122134 CN 200710122134 CN 200710122134 A CN200710122134 A CN 200710122134A CN 101390857 A CN101390857 A CN 101390857A
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- lansoprazole
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Abstract
Disclosed is a lansoprazole medicine combination, which contains alkaline substance which is not less than 10% by weight and used as stabilizer. The lansoprazole medicine combination is used for the treatment of peptic ulcer.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition, particularly a kind of pharmaceutical composition that contains lansoprazole.
Background technology
Lansoprazole is a kind of novel proton pump inhibitor; it is the benzimidazole substituent of exploitation after omeprazole; by the exploitation of Japanese Wu Tian company; it is mainly used in treatment gastric ulcer, duodenal ulcer, reflux esophagitis, assistant-Emhorn syndrome etc. clinically; its English name is Lansoprazole; chemical name is: (±)-2[[[3-methyl-4-(2,2, the 2-trifluoro ethoxy)-2-pyridine radicals] methyl] sulfinyl] benzimidazole.Its character is brownish white crystalline powder, is soluble in dimethyl formamide, dissolves in methanol, is insoluble in dehydrated alcohol, and ether is water-soluble hardly.
In recent years, main, smoking irregular by diet, drink, peptic ulcer rate that nervous, medicine irritation etc. causes increases gradually, brings great misery to the patient, the treatment of peptic ulcer more and more receives publicity clinically and payes attention to.
Peptic ulcer mainly refers to gastric ulcer and duodenal ulcer, and pathological changes is confined to stomach and 12 and refers to mucosa.Peptic ulcer is main because due to the gastric acid excessive secretion, thus mainly the gastric acid inhibitory secretion aspect treatment, the activity of the specific inhibition of lansoprazole energy H+-K+-ATP enzyme, this enzyme is the key enzyme that gastric acid generates.To basic gastric acid with by the irritability gastric acid secretion that stimulation causes inhibitory action is arranged.
The lansoprazole preparation is unstable under neutrality especially acid condition, and is destroyed easily in gastric acid, generally all adopts enteric material to carry out taking behind the coating in report, and disintegrate discharges in intestinal.Mainly disclose a kind of method that is fit to oral stabilizing pharmaceutical composition for preparing as EP0960620, comprise that the excretory substituted pyridylsulfinyl benzimidazole of gastric acid inhibitory mixes the mixture that forms with carrier.Wherein carrier mainly is the polymer that vinylpyrrolidone monomer is arranged, and utilizes said composition to prepare enteric coated capsule and tablet is more stable.And a kind of enteric coated preparation is disclosed among the EP10896694, and adopt enteric material to carry out coating, its casing play mainly is a hypromellose.Utilize the enteric coating parcel to make medicine stable really, also reached therapeutic effect, but increased technology difficulty.
Disclose a kind of compositions among the CN1116092, by comprising preparing as the benzimidazoles compound of lansoprazole class and the alkaline aqueous solution lyophilization of water miscible amide of antiulcer activity, production cost is higher.
Summary of the invention
The purpose of this invention is to provide a kind of stable pharmaceutical composition, said composition can be further used for preparing oral solid formulation.
The applicant is unexpected to find that lansoprazole can be stablized for a long time, in the preparation process, guarantee its stability, and certain alkaline environment must be provided in specific pH7-9 scope.Need to add certain weak base material, such material comprises inorganic base and organic base, and the example of inorganic base comprises the citrate of sodium or potassium, carbonate, bicarbonate, phosphate, sulfate, benzoate and anti-bad thrombosis salt, and calcium carbonate and magnesium carbonate; Organic base comprise amine, the instantiation of amine comprises N-methyl glucoside amine, guanine and arginine.
For convenience and improve patient's easy adaptability, most drug is sent with the form of unit dosage form, and with regard to solid drugs, these unit dosage forms generally are the forms of tablet and capsule, and in the present invention, dosage form is the form of capsule or tablet preferably; The form of tablet most preferably.
The applicant finds that alkaline matter is the best with one or both mixture of phosphate or carbonate.Selection is as stabilizing agent, preferably phosphoric acid hydrogen calcium in the phosphate.The applicant also finds, contains the alkaline matter during as filler that is no less than 10% weight, and preparation can keep good stable.
In the preparation of the Lansoprazole composition of wet method or non-slurry pelletizing, any granulating technique known in the art may be used to purpose of the present invention.
Even have been found that lansoprazole is than better curative effect is also arranged under the low dosage, in fact, by given patient is kept low dosage, might reduce side effect, still keep simultaneously efficacy of drugs, therefore need provide the lansoprazole that the low dosage form can be provided to the patient, for purposes of the present invention, by the final dosage that provides of lansoprazole preferably between 10mg and 120mg; More preferably between 30-50mg.
Compositions of the present invention also comprises the combination greater than the diluent or the diluent of about 30% weight.Wherein said diluent is meant lactose monohydrate, Lactis Anhydrous, microcrystalline Cellulose, mannitol, sorbitol.
The disintegrating agent that also comprises greater than about 5% weight of the present invention.Described disintegrating agent such as low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone and carboxymethyl starch sodium.
Can also add lubricant in the compositions of the present invention, other adjuvants such as fluidizer.Exist with tablet or capsule form;
Compositions of the present invention also can be added an amount of correctives and disintegrating agent and is prepared into oral cavity disintegration tablet, and described correctives comprises one or more mixture in sucralose, Ai Saimi, stevioside, the aspartame.Add filler such as sugar alcohols, starch, microcrystalline Cellulose during the pressing port cavity disintegrating tablet, lubricant such as magnesium stearate, Pulvis Talci, calcium stearate, hydrogenated vegetable oil and light silicic acid anhydride.
The specific embodiment
The present invention is further elaborated by following examples, but does not limit the scope of the invention.
Embodiment 1:
Preparation technology:
Lansoprazole was pulverized 100 mesh sieves, and mannitol, lactose, calcium hydrogen phosphate, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose are crossed 80 mesh sieves respectively, and magnesium stearate is crossed 60 orders.Mixing in the mixer granulator fast, add entry system soft material by recipe quantity, cross 18 mesh sieves, in 55 ℃ of baking ovens, after the drying, cross 24 mesh sieve granulate, add the magnesium stearate of recipe quantity, the mixing tabletting, every contains lansoprazole 30mg.
Embodiment 2:
Preparation technology:
Lansoprazole was pulverized 100 mesh sieves; mannitol, lactose, calcium hydrogen phosphate, microcrystalline Cellulose, polyvinylpolypyrrolidone are crossed 80 mesh sieves respectively; mixing in the mixer granulator fast, add entry system soft material by recipe quantity, cross 18 mesh sieves; in 55 ℃ of baking ovens after the drying; cross 24 mesh sieve granulate, obtain evenly full granule of color and luster, add the micropowder silica gel of recipe quantity; mixing incapsulates in the shell.Every contains lansoprazole 30mg.
Embodiment 3:
Preparation technology:
Lansoprazole was pulverized 100 mesh sieves; mannitol, lactose, calcium hydrogen phosphate, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose are crossed 80 mesh sieves respectively; mixing in the mixer granulator fast by recipe quantity; add entry system soft material, cross 18 mesh sieves, in 55 ℃ of baking ovens after the drying; cross 24 mesh sieve granulate; the magnesium stearate that adds recipe quantity, mixing, tabletting.Every contains lansoprazole 50mg
The comparative example 1:
Preparation technology:
Lansoprazole was pulverized 100 mesh sieves; lactose, corn starch, crystalline cellulose, hyprolose are crossed 80 mesh sieves respectively; mixing in the mixer granulator fast by recipe quantity; add entry system soft material, cross 18 mesh sieves, in 55 ℃ of baking ovens after the drying; cross 24 mesh sieve granulate; the magnesium stearate and the micropowder silica gel that add recipe quantity, mixing, tabletting.
The comparative example 2:
Preparation technology:
Lansoprazole was pulverized 100 mesh sieves; lactose, corn starch, hyprolose are crossed 80 mesh sieves respectively; mixing in the mixer granulator fast by recipe quantity; add entry system soft material, cross 18 mesh sieves, in 55 ℃ of baking ovens after the drying; cross 24 mesh sieve granulate; the magnesium stearate and the micropowder silica gel that add recipe quantity, mixing, fill capsule.
1: with the preparation produced among embodiment 1～3, the comparative example 1～2 in accelerated tests (40 ± 2 ℃ of temperature, humidity 75% ± 5%) related substance growth pattern is shown in table 1, the table 2 respectively and in the long-time stability experiment (25 ± 2 ℃ of temperature, humidity 60% ± 5%).
Table 1. accelerated tests result
| 1 month | 2 months | 3 months | 6 months | |
| Embodiment 1 | - | - | - | - |
| Embodiment 2 | - | - | - | - |
| Embodiment 3 | - | - | - | - |
| The comparative example 1 | - | - | + | + |
| The comparative example 2 | - | + | + | ++ |
Table 2. long-time stability experimental result
| 0 month | 3 months | 6 months | 9 months | 12 months | 18 months | |
| Embodiment 1 | - | - | - | - | - | - |
| Embodiment 2 | - | - | - | - | - | - |
| Embodiment 3 | - | - | - | - | - | - |
| The comparative example 1 | - | - | - | + | + | ++ |
| The comparative example 2 | - | - | + | + | ++ | ++ |
Annotate :-: the related substance growth was compared with 0 day and is no more than 0.05%; +: related substance increased with 0 day to be compared above 0.1%; ++: related substance increased with 0 day to be compared above 0.5%
Therefore, from the result shown in table 1～table 2 as can be seen, the Orally-administered solid composition that contains lansoprazole of the present invention is relatively stable, and other every assays also prove by the preparation of said composition preparation very stablely simultaneously, are a kind of good preparations therefore.
2: the inhibitory action of ulcer
Be fixed in the ferrum cage rat is single, make its fasting can't help water 48 hours.Take above-mentioned prescription sample after 1 hour, with the surgical thread ligation of its stomachus pyloricus,, flowed out to prevent gastric juice the position ligation of stomach cardia with surgical thread the dissection back with rat execution in 19 hours after the ligation.Take off stomach then, the place cuts off stomach along greater gastric curvature, and water washes away behind the impurity on Weishang with investigating its damaged surfaces degree (use anatomic microscope), and calculates ulcer index (UI) agent ulcer inhibition rate according to following formula.
Ulcer inhibition rate=[(matched group UI-medication group UI)/blank group UI] * 100%
Table 3. prescription suppresses and ulcer suppression ratio result gastric acid secretion
| The gastric acid secretion suppression ratio | Ulcer inhibition rate | |
| Embodiment 1 | 33 | 82 |
| Embodiment 2 | 30 | 90 |
| Embodiment 3 | 35 | 88 |
| The comparative example 1 | 19 | 34 |
| The comparative example 2 | 13 | 27 |
As can be seen from Table 3, the suppression ratio of 1～3 pair of gastric acid of embodiment is stronger, and behind the adding alkaline conditioner, it is more stable to write out a prescription, and is reduced greatly by the stomach acids destroy rate, effectively the secretion of gastric acid inhibitory.
Claims (6)
1, a kind of pharmaceutical composition that comprises lansoprazole or its officinal salt, contain be no less than 10% weight alkaline matter as filler.
2, pharmaceutical composition as claimed in claim 1, wherein said alkaline matter are one or both mixture of phosphate or carbonate.
3, pharmaceutical composition as claimed in claim 2, wherein said phosphate are calcium hydrogen phosphate.
4, pharmaceutical composition as claimed in claim 1 wherein also comprises the combination greater than the diluent or the diluent of 30% weight.
5, pharmaceutical composition as claimed in claim 4, wherein said diluent is selected from lactose monohydrate, Lactis Anhydrous, microcrystalline Cellulose or mannitol.
6, pharmaceutical composition as claimed in claim 1 wherein also contains lubricant, and fluidizer exists with tablet or capsule form.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710122134 CN101390857A (en) | 2007-09-21 | 2007-09-21 | Medicine composition containing lansoprazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710122134 CN101390857A (en) | 2007-09-21 | 2007-09-21 | Medicine composition containing lansoprazole |
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| Publication Number | Publication Date |
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| CN101390857A true CN101390857A (en) | 2009-03-25 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200710122134 Pending CN101390857A (en) | 2007-09-21 | 2007-09-21 | Medicine composition containing lansoprazole |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102198109A (en) * | 2011-05-20 | 2011-09-28 | 广东帅广医药有限公司 | Lansoprazole medicine composition tablet and preparation method thereof |
| CN101716159B (en) * | 2009-11-20 | 2012-01-04 | 上海新亚药业闵行有限公司 | Stable lansoprazole tablet and preparation method thereof |
| CN102772387A (en) * | 2012-08-09 | 2012-11-14 | 广东帅广医药有限公司 | Lansoprazole composition enteric capsule and preparation method thereof |
| CN106236735A (en) * | 2016-07-28 | 2016-12-21 | 南京正宽医药科技有限公司 | A kind of lansoprazole intestine dissolving capsule treating gastric ulcer and preparation method thereof |
-
2007
- 2007-09-21 CN CN 200710122134 patent/CN101390857A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101716159B (en) * | 2009-11-20 | 2012-01-04 | 上海新亚药业闵行有限公司 | Stable lansoprazole tablet and preparation method thereof |
| CN102198109A (en) * | 2011-05-20 | 2011-09-28 | 广东帅广医药有限公司 | Lansoprazole medicine composition tablet and preparation method thereof |
| CN102772387A (en) * | 2012-08-09 | 2012-11-14 | 广东帅广医药有限公司 | Lansoprazole composition enteric capsule and preparation method thereof |
| CN106236735A (en) * | 2016-07-28 | 2016-12-21 | 南京正宽医药科技有限公司 | A kind of lansoprazole intestine dissolving capsule treating gastric ulcer and preparation method thereof |
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Application publication date: 20090325 |