CN102871978B - Levosulpiride tablets and preparation method thereof - Google Patents
Levosulpiride tablets and preparation method thereof Download PDFInfo
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- CN102871978B CN102871978B CN201210403060.9A CN201210403060A CN102871978B CN 102871978 B CN102871978 B CN 102871978B CN 201210403060 A CN201210403060 A CN 201210403060A CN 102871978 B CN102871978 B CN 102871978B
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Abstract
The invention provides levosulpiride tablets and a preparation method thereof. The levosulpiride tablets comprise levosulpiride, microcrystalline cellulose, crosslinking povidone and magnesium stearate, and have the advantages of simple prescription, high production efficiency, energy saving and cost saving; and the prepared tablets have the characteristics of quick disintegration and dissolution as well as good stability.
Description
Technical field
The present invention relates to pharmaceutical field, be specifically related to a kind of oral solid formulation.
Background technology
Relation between socio-psychological factors and gastrointestinal tract nervous system is very close, and stress can make gastric emptying change, and regulates the sensation of importing into of internal organs, causes functional dyspepsia (Functional dyspepsia, FD).Along with the quickening of modern society's rhythm of life and the aggravation of competition, people are subject to from surrounding pressure as more in family, work and society, and functional dyspepsia has become commonly encountered diseases, frequently-occurring disease clinically.The sickness rate of FD is about 20%-40%, in digestion special outpatient clinic, accounts for 60%-70%.FD patient has more state and the Mental Depression obstacle of anxiety compared with Healthy People, show as clinically the epigastric discomfort that continues or repeatedly show effect, with glutted, abdominal part flatulence after the meal, heating installation, early full, anorexia, feel sick, the symptom such as vomiting, heartburn, regurgitation, retrosternal pain, abnormal defecation, without part or whole body organic disease.
Levosulpiride (levosulpiride) is the levo-enantiomer of sulpiride; i.e. (S)-(-)-5-aminosulfonyl-N-[(1-ethyl-2-nafoxidine base) methyl]-2-methoxy benzamide; also can called after (S)-(-)-N-[methyl-(1-ethyl-2-pyrrolidinyl)]-2-methoxyl group-5-(amino-sulfonyl)-Benzoylamide is a kind of novel gastric motility new drug.Levosulpiride mainly plays a role by exciting 5-HT4 receptor and antagonism d2 dopamine receptor, main as anti-functional dyspepsia medicine clinically, also can be used as the medicine of psychosis, obstinate vomit, peptic ulcer, craniocerebral injury dizziness and headache.Compare with motilium, the activity of levosulpiride is high, and untoward reaction is low.
At present, at commercially available levosulpiride sheet (LEVOPRAID
?, Abbott) basis on, optimize prescription and preparation technology, enhance productivity, energy savings and production cost, be to need technical staff to put forth effort the technical problem solving.
Summary of the invention
On the one hand, the invention provides a kind of levosulpiride sheet, meter by weight, is comprised of the component of following content:
Wherein, the preferred 25-50 of levosulpiride, the preferred 80-120 of microcrystalline Cellulose, the preferred 10-30 of polyvinylpolypyrrolidone, the preferred 0.5-2 of magnesium stearate.
Preferably, the invention provides following 5 kinds of levosulpiride sheets:
| Levosulpiride sheet | 1 | 2 | 3 | 4 | 5 |
| Levosulpiride | 25?g | 5?g | 100?g | 50?g | 75?g |
| Microcrystalline Cellulose | 80?g | 50?g | 150?g | 120?g | 100?g |
| Polyvinylpolypyrrolidone | 10?g | 30?g | 50?g | 5?g | 20?g |
| Magnesium stearate | 0.5?g | 0.3?g | 5?g | 1.5?g | 2?g |
| Make | 1000 | 1000 | 1000 | 1000 | 1000 |
On the other hand, the invention still further relates to the preparation method of described levosulpiride sheet: levosulpiride, microcrystalline Cellulose, polyvinylpolypyrrolidone, magnesium stearate are mixed to tabletting.
Again on the one hand, the invention still further relates to the purposes of described levosulpiride sheet in the medicine of the anti-functional dyspepsia of preparation, psychosis, obstinate vomit, peptic ulcer, craniocerebral injury dizziness and headache.
Beneficial effect of the present invention is: 1) prescription is simple, only contains three kinds of adjuvants; 2) preparation technology is simple, can adopt direct mixed pressuring plate, has save the steps such as wet granulation, dry, granulate, enhances productivity approximately 1 times, and has saved cost and the energy; 3) impurity content is low, better quality, and drug safety is higher, is better than commercially available product; 4) stripping is rapid, is better than commercially available product; 5) good stability, under high humidity (RH92.5%, 10 days), high temperature (60 ℃, 10 days) and illumination (4500Lx, 10 days) condition, impurity content low (< 0.10%), and under the acceleration environment of 40 ℃ of high temperature, relative humidity RH75%, in 6 months, keep stable, be better than commercially available product.
The dosage of levosulpiride sheet of the present invention need to be determined according to clinician's judgement, and for example, daily dose can be 75mg～200mg.
The specific embodiment
The specific embodiment only, for further explaining and describing the present invention, should not be interpreted as any limitation of the invention.
Embodiment 1～5 levosulpiride sheet
The prescription of levosulpiride sheet sees the following form:
Preparation technology: by the raw material blending of recipe quantity, tabletting, obtains.
The stripping comparative study of experimental example 1 levosulpiride sheet and commercially available prod
Get levosulpiride sheet and commercially available prod LEVOPRAID that embodiment 1～5 makes
?according to two appendix XC first methods of < < Chinese Pharmacopoeia > > version in 2010, measure dissolution, the 0.1mol/L hydrochloric acid solution 1000ml of take is solvent, rotating speed is 50 turn/min, operation in accordance with the law, through certain hour, get the 0.1mol/L hydrochloric acid solution that solution 5ml(adds same volume simultaneously in stripping rotor), filter, precision measures subsequent filtrate, according to high performance liquid chromatography, (with octadecylsilane chemically bonded silica, be filler, 0.05mol/L phosphate buffer (the pH3.5)-acetonitrile (90:10) of take is mobile phase, flow velocity is 1ml per minute, detection wavelength is 220nm.Number of theoretical plate is pressed levosulpiride peak and is calculated, and should be not less than 2000.The separating degree of levosulpiride and adjacent impurity peaks is all up to specification.Get dissolution subsequent filtrate as need testing solution; It is appropriate that precision takes levosulpiride reference substance, adds mobile phase dilution and make the solution that contains 25 μ g in every 1ml, in contrast product solution.Precision measures need testing solution and reference substance solution 10 μ l, and injection liquid chromatography, records chromatogram, by external standard method, with calculated by peak area, measures the accumulation stripping percentage rate of tablet.Result is as follows:
The cumulative leaching rate % of commercially available prod sees the following form:
| Time | 3min | 5min | 10min | 15min | 30min | 45min |
| Cumulative leaching rate % | 91.2 | 97.1 | 96.9 | 97.5 | 96.3 | 96.5 |
The cumulative leaching rate % of levosulpiride sheet prepared by embodiment 1-5 sees the following form:
| Embodiment | 1 | 2 | 3 | 4 | 5 |
| 1min | 70.8 | 72.8 | 65.1 | 56.8 | 52.2 |
| 2min | 88.9 | 89.2 | 88.6 | 86.4 | 89.6 |
| 3min | 99.4 | 98.3 | 99.7 | 96.3 | 98.5 |
| 4min | 99.6 | 98.8 | 99.3 | 99.7 | 99.5 |
| 5min | 99.7 | 99.5 | 99.2 | 99.9 | 100.2 |
| 10min | 99.2 | 99.9 | 99.8 | 99.5 | 100.3 |
The stability study (25 ℃, RH75%, without packing) of experimental example 2 levosulpiride sheets under super-humid conditions
High wet test is carried out in levosulpiride sheet and commercially available prod that embodiment 1～5 is made, according to the high performance liquid chromatography of two sulpiride determination of foreign matters of < < Chinese Pharmacopoeia > > version in 2010, measure impurity and content, adopt experimental example 1 method to measure dissolution (be 5 minutes sample time), result is as follows:
The stability study (Lx4500, without packing) of experimental example 3 levosulpiride sheets under strong illumination condition
Exposure experiments to light is carried out in levosulpiride sheet and commercially available prod that embodiment 1～5 is made, by standard, detects, and result is as follows:
The stability study (60 ℃, without packing) of experimental example 4 levosulpiride sheets under hot conditions
Hot test is carried out in levosulpiride sheet and commercially available prod that embodiment 1～5 is made, according to the high performance liquid chromatography of two sulpiride determination of foreign matters of < < Chinese Pharmacopoeia > > version in 2010, measure impurity and content, adopt experimental example 1 method to measure dissolution (be 3 minutes sample time), result is as follows:
The stability study of experimental example 5 levosulpiride sheets under acceleration environment (40 ℃, RH75%)
The levosulpiride sheet that embodiment 1～5 is made and commercially available levosulpiride sheet carry out accelerated test, the high performance liquid chromatography checking according to two sulpiride related substances of < < Chinese Pharmacopoeia > > version in 2010, measure impurity and content, adopt experimental example 1 method to measure dissolution (be 3 minutes sample time), result is as follows:
Experimental example 1～5 shows, compared with prior art, the present invention has the following advantages: 1) can complete stripping in 3 minutes, and stripping is rapider, and onset is faster; 2) impurity content lower (being about 0.05%), is about 1/3 of commercially available product (0.16%); 3) under high humidity, high temperature, illumination, place 10 days, and accelerated test 6 months, product stripping etc. has no significant change, and impurity is no more than 0.10%, and quality is more stable, and clinical efficacy and safety expection can be better.
Claims (7)
1. a levosulpiride sheet, counts by weight, composed as follows:
2. a levosulpiride sheet, the prescription of every 1000 is as follows:
3. a levosulpiride sheet, the prescription of every 1000 is as follows:
4. a levosulpiride sheet, the prescription of every 1000 is as follows:
5. a levosulpiride sheet, the prescription of every 1000 is as follows:
6. a levosulpiride sheet, the prescription of every 1000 is as follows:
7. a preparation method for the arbitrary described levosulpiride sheet of claim 1-6, comprises the levosulpiride of recipe quantity, polyvinylpolypyrrolidone, microcrystalline Cellulose, magnesium stearate is mixed, tabletting.
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| CN201210403060.9A CN102871978B (en) | 2012-10-19 | 2012-10-19 | Levosulpiride tablets and preparation method thereof |
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| CN201210403060.9A CN102871978B (en) | 2012-10-19 | 2012-10-19 | Levosulpiride tablets and preparation method thereof |
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| CN102871978A CN102871978A (en) | 2013-01-16 |
| CN102871978B true CN102871978B (en) | 2014-04-09 |
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| CN113332276A (en) * | 2021-06-01 | 2021-09-03 | 大桐制药（中国）有限责任公司 | Production method of sulpiride preparation |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1723892A (en) * | 2005-07-15 | 2006-01-25 | 任巧玲 | Sulpride dispersion tablets prepn. method |
| CN1836651A (en) * | 2006-04-27 | 2006-09-27 | 上海和臣医药工程有限公司 | Levogyration sulpiride injection and its preparation method |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AU3667899A (en) * | 1998-04-29 | 1999-11-16 | American Home Products Corporation | Antipsychotic indolyl derivatives |
| CN100477985C (en) * | 2005-12-06 | 2009-04-15 | 福寿堂制药有限公司 | Dispersible tablet for clearing away heat of brain and heart and preparation process thereof |
| CN100457100C (en) * | 2005-12-23 | 2009-02-04 | 北京科信必成医药科技发展有限公司 | Metoclopramide oral cavity disintegrating tablet and its production method |
| CA2738114A1 (en) * | 2008-09-22 | 2010-04-08 | Rubicon Research Private Limited | Compositions exhibiting delayed transit through the gastrointestinal tract |
| US20110052700A1 (en) * | 2009-08-31 | 2011-03-03 | Depomed, Inc. | Gastric retentive pharmaceutical compositions for immediate and extended release of levosulpiride |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1723892A (en) * | 2005-07-15 | 2006-01-25 | 任巧玲 | Sulpride dispersion tablets prepn. method |
| CN1836651A (en) * | 2006-04-27 | 2006-09-27 | 上海和臣医药工程有限公司 | Levogyration sulpiride injection and its preparation method |
Non-Patent Citations (1)
| Title |
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| 高剑锋，等.舒必利分散片的制备及质量控制.《中国药房》.2007,第18卷(第1期),第52页左栏第2-3段. * |
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