CN100542524C - A kind of Pharmaceutical composition that contains rasagiline - Google Patents
A kind of Pharmaceutical composition that contains rasagiline Download PDFInfo
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- CN100542524C CN100542524C CNB2006101134687A CN200610113468A CN100542524C CN 100542524 C CN100542524 C CN 100542524C CN B2006101134687 A CNB2006101134687 A CN B2006101134687A CN 200610113468 A CN200610113468 A CN 200610113468A CN 100542524 C CN100542524 C CN 100542524C
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- pharmaceutical composition
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- rasagiline
- oral administration
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Abstract
The invention discloses the medicinal compositions of a kind of oral administration solid, contain the organic acid of the rasagiline and the salt thereof of 0.5%～3% weight portion, the pentabasis alcohol that is lower than 60% weight portion and/or hexahydroxylic alcohols and 0.5～3% weight portion, be used for the treatment of parkinson.
Description
Technical field
The present invention relates to a kind of Pharmaceutical composition, the medicinal compositions of the parkinsonian rasagiline oral administration solid of particularly a kind of novel therapeutic.
Background technology
Parkinson is the second largest neural chronic disease after Alzheimer, parkinsonian morbidity mainly is because carrying out property of dopaminergic neuron degeneration in big substantia nigra-striatum system, causes due to the exhaustion of neurotransmitter dopamine in the striatal primary motor area territory.
The parkinsonian medicine of treatment has levodopa, DA receptor stimulating agent, MAO-B inhibitor, COMT inhibitor at present.Levodopa is the parkinsonian main force of treatment all the time since the sixties in 20th century, though levodopa has its superiority of not replacing, only is that the precursor as DA replenishes DA content, occurs severe complications easily.Have better safety with respect to the levodopa rasagiline, can improve motion and cognitive function, can be used for early stage parkinsonian's treatment separately.
EP0436492 discloses the application of rasagiline in aspect diseases such as treatment parkinson, dysmnesia, discloses rasagiline and has all played a role with dosage form administrations such as oral solid formulation, liquid preparation, emulsifiable paste, preparation capable of permeating skin.
WO9511016 discloses the application of rasagiline at aspects such as the degeneration of treatment cranial nerve, cerebral ischemia, cerebral trauma, neural division diseases, disclose among the embodiment and adopted breast, microcrystalline Cellulose, starch, carboxymethylstach sodium to prepare tablet, the prescription of dosage form such as liquid preparation, syrup is formed, but preparation stability is not good;
WO9718523 discloses a kind of stable pharmaceutical composition, contains the pentabasis alcohol and/or the hexahydroxylic alcohols that are at least 60% weight portion, also contains citric acid and magnesium stearate in its most preferred embodiment.But oral a large amount of mannitol can produce diarrhoea, anaphylaxis.Therefore, be necessary to overcome above-mentioned defective, a kind of new rasagiline pharmaceutical composition is provided
Summary of the invention
The purpose of this invention is to provide the medicinal compositions of the parkinsonian rasagiline oral administration solid of a kind of stable treatment, the mannitol consumption is less, and stability better.
The applicant is devoted to develop contains small amount of mannitol and stability preparation preferably, applicant's surprised discovery in a large amount of experimentations, opposite with the enlightenment of WO9718523 in instruction, when content is lower than the mannitol of 60% weight portion, the rasagiline oral solid formulation that can obtain to have good stability equally.
Pharmaceutical composition provided by the invention contains the organic acid of the pentabasis alcohol of the rasagiline of 0.5%～3% weight portion and salt thereof, 40%～60% weight portion and/or hexahydroxylic alcohols, 0.5～3% weight portion.
Pharmaceutical composition provided by the invention, pentabasis alcohol and/or hexahydroxylic alcohols as being fit to 40%～60% weight portion of the present invention are selected from a kind of and/or several mixture in mannitol, xylitol, sorbitol, the maltose alcohol.
Pharmaceutical composition provided by the invention is as suitable pentabasis alcohol of the present invention and/or hexahydroxylic alcohols most preferably mannitol, sorbitol.
Pharmaceutical composition provided by the invention is tablet, capsule or dispersible tablet form.
Pharmaceutical composition provided by the invention can be selected from stearic acid, citric acid or tartaric acid as suitable organic acid of the present invention.
Pharmaceutical composition provided by the invention is as suitable organic acid of the present invention stearic acid most preferably.
Pharmaceutical composition provided by the invention contains filler, binding agent, disintegrating agent, lubricant or correctives as suitable adjuvant of the present invention.
Pharmaceutical composition provided by the invention also can contain one or more mixture in starch, pregelatinized Starch, the microcrystalline Cellulose as being fit to filler of the present invention.
Pharmaceutical composition provided by the invention, can be selected from one or more mixture in polyvidone, sodium carboxymethyl cellulose, starch slurry, pregelatinized Starch, gelatin, xanthan gum, different concentration ethanol, the water as being fit to binding agent of the present invention, weight is 2%～20% weight portion.
Pharmaceutical composition provided by the invention can be selected from one or more mixture in polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, the hydroxypropyl cellulose as being fit to disintegrating agent of the present invention, and weight is 2%～10% weight portion.
Pharmaceutical composition provided by the invention, can be selected from one or more mixture in magnesium stearate, micropowder silica gel, the Pulvis Talci as being fit to lubricant of the present invention, weight is Pulvis Talci, the micropowder silica gel of 0.5%～3% weight portion, and weight is 0.2%～0.5% magnesium stearate.
Pharmaceutical composition provided by the invention can be selected from one or more mixture in aspartame, sucralose, stevioside, gelatin, xanthan gum, ethyl cellulose, acrylic resin, saccharin sodium, essence, cyclamate, essence, the Mentholum as being fit to correctives of the present invention.
The specific embodiment
Below the present invention is described in further detail, but not only be confined to following embodiment.
Embodiment 1:
Preparation technology:
1. supplementary material is pulverized, sieved, standby.
2. the rasagiline mesilate, mannitol, microcrystalline Cellulose, starch that takes by weighing recipe quantity be by the equivalent principle mix homogeneously that progressively increases, solid mixture.
3. granulate drying, granulate with adding starch slurry in the solid mixture.
4. calculated yield adds micropowder silica gel, Pulvis Talci, stearic acid, mixes, and is encapsulated.
Embodiment 2:
Preparation technology:
1. supplementary material is pulverized, sieved, standby.
2. the rasagiline mesilate, sorbitol, microcrystalline Cellulose, pre-paying starch, starch that takes by weighing recipe quantity be by the equivalent principle mix homogeneously that progressively increases, solid mixture.
3. granulate drying, granulate with adding starch slurry in the solid mixture.
4. calculated yield adds micropowder silica gel, Pulvis Talci, citric acid, mixes tabletting.
Embodiment 3:
Preparation technology
1. supplementary material is pulverized, sieved, standby.
2. the rasagiline mesilate, mannitol, microcrystalline Cellulose, carboxymethylstach sodium that takes by weighing recipe quantity be by the equivalent principle mix homogeneously that progressively increases, solid mixture.
3. 50% alcohol granulation, drying, granulate will be added in the solid mixture.
4. calculated yield adds essence, sucralose, Mentholum, magnesium stearate, citric acid, mixing, tabletting.
Embodiment 4:
Preparation technology
5. supplementary material is pulverized, sieved, standby.
6. the rasagiline mesilate, sorbitol, microcrystalline Cellulose, cross-linked carboxymethyl cellulose sodium that takes by weighing recipe quantity be by the equivalent principle mix homogeneously that progressively increases, solid mixture.
7. 50% alcohol granulation, drying, granulate will be added in the solid mixture.
8. calculated yield adds Fructus Citri tangerinae powdered flavor, aspartame, Pulvis Talci, stearic acid, mixing, tabletting.
Embodiment 5:
Preparation technology:
1. supplementary material is pulverized, sieved, standby.
2. the rasagiline mesilate, lactose, mannitol that takes by weighing recipe quantity be by the equivalent principle mix homogeneously that progressively increases, solid mixture.
3. granulate drying, granulate with adding water in the solid mixture.
4. calculated yield adds magnesium stearate, tartaric acid, mixes, and is encapsulated.
Embodiment 6: the accelerated stability according to the sample of embodiment 2 preparation the results are shown in following table:
Embodiment 7: the long-time stability according to the sample of embodiment 2 preparation the results are shown in Table:
Contain in the prescription that preparation that the pentabasis alcohol of 40%～60% weight portion and/or hexahydroxylic alcohols, 0.5%～3.0% weight portion organic acid make quickened six months and long-term 18 months stability better.
Claims (6)
1. medicinal compositions of oral administration solid, contain 0.5%～3% weight portion rasagiline mesilate, be not less than 40% and be lower than the mannitol of 60% weight portion or citric acid, stearic acid or the tartaric acid of sorbitol and 0.5～3% weight portion, described compositions is a tablet.
2. Pharmaceutical composition according to claim 1 is characterized in that containing filler, binding agent, disintegrating agent, lubricant and correctives.
3. Pharmaceutical composition according to claim 2 is characterized in that containing 0.5%～4% parts by weight of micro silica gel powder or Pulvis Talci.
4. medicinal compositions of oral administration solid, it is a tablet form, the ratio of each component is:
5. medicinal compositions of oral administration solid, it is a tablet form, the ratio of each component is:
6. medicinal compositions of oral administration solid, it is a tablet form, the ratio of each component is:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006101134687A CN100542524C (en) | 2006-09-29 | 2006-09-29 | A kind of Pharmaceutical composition that contains rasagiline |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006101134687A CN100542524C (en) | 2006-09-29 | 2006-09-29 | A kind of Pharmaceutical composition that contains rasagiline |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101152153A CN101152153A (en) | 2008-04-02 |
| CN100542524C true CN100542524C (en) | 2009-09-23 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006101134687A Expired - Fee Related CN100542524C (en) | 2006-09-29 | 2006-09-29 | A kind of Pharmaceutical composition that contains rasagiline |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100542524C (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100189790A1 (en) * | 2009-01-23 | 2010-07-29 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline formulation |
| EP2403485A2 (en) * | 2009-03-05 | 2012-01-11 | Sandoz AG | Pharmaceutical composition containing rasagiline mesylate |
| CN102048717B (en) † | 2009-10-29 | 2014-02-19 | 重庆医药工业研究院有限责任公司 | Stable rasagiline composition |
| CN103315983B (en) * | 2012-12-20 | 2015-06-03 | 上海中西制药有限公司 | Rasagiline preparation and preparation method thereof |
| CN115400090A (en) * | 2022-10-09 | 2022-11-29 | 北京新领先医药科技发展有限公司 | Orally disintegrating tablet composition of rasagiline and preparation method thereof |
-
2006
- 2006-09-29 CN CNB2006101134687A patent/CN100542524C/en not_active Expired - Fee Related
Non-Patent Citations (2)
| Title |
|---|
| 甘露醇在化工中的开发应用. 梁智，罗鸣.化学中间体，第3-4期. 2002 |
| 甘露醇在化工中的开发应用. 梁智，罗鸣.化学中间体，第3-4期. 2002 * |
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| Publication number | Publication date |
|---|---|
| CN101152153A (en) | 2008-04-02 |
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