CN1660056A - Oral disintegration tablet of tramadol hydrochloride and preparation method - Google Patents
Oral disintegration tablet of tramadol hydrochloride and preparation method Download PDFInfo
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- CN1660056A CN1660056A CN 200410060369 CN200410060369A CN1660056A CN 1660056 A CN1660056 A CN 1660056A CN 200410060369 CN200410060369 CN 200410060369 CN 200410060369 A CN200410060369 A CN 200410060369A CN 1660056 A CN1660056 A CN 1660056A
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- tramadol hydrochloride
- oral cavity
- disintegration tablet
- tablet
- cavity disintegration
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Abstract
An orally disintegrating tablet of tramadol hydrochloride is prepared through preparing the dispersed solid from tramadol hydrochloride and dispersing solid carrier, mixing it with filler, disintegrant, flavouring and lubricant, stirring and tabletting.
Description
Technical field
The present invention relates to a kind of tramadol hydrochloride oral drug preparation, particularly tramadol hydrochloride oral cavity disintegration tablet and preparation method thereof.
Background technology
Tramadol hydrochloride, English name: Tramadol, Hydrochloride, chemical name is: methyl (±)-E-2[(=methylamino)]-1-(3-methoxyphenyl) Hexalin hydrochlorate, this product is white crystals or crystallinity powder; Odorless, bitter in the mouth; Have draw moist.It is very easily molten in water, and is easily molten in ethanol or chloroform, and slightly soluble in acetone is insoluble in ether.Its fusing point is 179-182 ℃.The molecular formula of this product is: C
16H
25NO
2HCl, molecular weight are 229.84, and its structural formula is as follows:
Tramadol hydrochloride is developed by the safe company of German Glan, at first in Germany's listing, is comprising many countries listing of China in 1977 at present, and this product is the potent analgesic of non-morphine class.Be mainly used in central nervous system's special receptor relevant with pain.Be usually used in clinically alleviating acute and chronic pain, can obtain satisfied analgesic effect aspect pain that causes in postoperative pain, pain of childbirth, wound pain, diagnostic exploration and the relaxing tumor pain.
The route of administration of tramadol hydrochloride is very wide, Orally-administrable, drop rectum with drug, and intramuscular injection or vein are slowly injected, or instil in the dilution posterior vein.At present, how tame production of units tramadol hydrochlorides such as China approved Shandong Xinhua, and by income national basic medical insurance medicine catalogue (Class B).Usually, the dosage form of this product comprises tablet, capsule, suppository, drop, injection etc.Oral administration solid tablet particularly, it is by tramadol hydrochloride 20mg, microcrystalline Cellulose 35mg, starch 23mg, Pulvis Talci 10mg, micropowder silica gel 1mg, magnesium stearate 1mg forms, and adopts powder direct compression, dry granulation tabletting or wet granule compression tablet.When the patient takes this medicine, must take, when taking, usually feel very inconvenient, even can meet accident, and for the patient who goes out, in that do not having can be inconvenient more under the situation of water for the patient of old man, child and dysphagia with boiled water.And this common oral tablet does not usually reach the effect of quick acting.
Summary of the invention
The object of the present invention is to provide a kind of tramadol hydrochloride oral cavity disintegration tablet and preparation method thereof, it can overcome the deficiency of prior art, can make patient's taking convenience, is not taken the restriction of water; Tablet places the oral cavity to meet saliva disintegrate rapidly, and the through port transmucosal absorbs rapidly, and is rapid-action to indication, early curative effect is obvious to reach the peak.And preparation technology is simple.
Oral cavity disintegration tablet (orally disintegrating tablee) is emerging in recent years a kind of oral cavity rapid release preparation, compare with conventional tablet, this dosage form need not also to need not to chew with water delivery service, medicine places mouth, after meeting the rapid disintegrate of saliva, in the oral cavity,, also can go into stomach, onset rapidly by means of swallowing act by mucosa absorption.
Tramadol hydrochloride oral cavity disintegration tablet of the present invention is made up of tramadol hydrochloride, solid dispersion carrier, filler, disintegrating agent, correctives, lubricant.This tablet is by mass percentage:
Tramadol hydrochloride 5-40%, solid dispersion carrier 5-60%, filler 5-50%, disintegrating agent 3-35%, correctives 1-20%, lubricant 0-1%.
Described solid dispersion carrier may be selected to be: ethyl cellulose, and Polyethylene Glycol (PEG) (comprises PEG6000, PEG4000), polyvinylpyrrolidone (PVP), poloxamer, You Teqi (comprising Eudragit EC10cp, EudragitE100, Eudragit S100) and composition thereof.
Described filler may be selected to be: microcrystalline Cellulose (MCC), dextrin, lactose, starch and composition thereof.
Described disintegrating agent may be selected to be: low-substituted hydroxypropyl cellulose (L-HPC), crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na) and composition thereof.
Described correctives may be selected to be: mannitol, stevioside, natural or artificial sweeting agent such as A Siba is sweet.
Described lubricant may be selected to be: magnesium stearate, Stepanol MG, sodium lauryl sulphate, Pulvis Talci etc.
The preparation method of tramadol hydrochloride oral cavity disintegration tablet of the present invention is as follows:
At first, tramadol hydrochloride and solid dispersion carrier are prepared solid dispersion with fusion method or solvent method, then, press formula ratio again and remaining adjuvant filler, disintegrating agent, correctives and mix lubricant are even, adopt the powder direct compression, dry granulation tabletting or wet granule compression tablet, promptly.Be 10s-18min the disintegration of this tablet.
Technical characterstic of the present invention is: reach specification requirement by solid dispersion, correctives and disintegrating agent synergism.Select ethyl cellulose, Polyethylene Glycol (PEG6000 for use, PEG4000), polyvinylpyrrolidone (PVP), poloxamer, You Teqi (Eudragit EC10cp, Eudragit E100, Eudragit S100) and composition thereof prepare solid dispersion in advance for carrier, can cover the bitterness of some tramadol hydrochlorides earlier a little; Add natural or artificial sweeting agents such as correctives mannitol, lactose, stevioside, A Siba is sweet simultaneously and further cover the bitterness of tramadol hydrochloride; Filler and disintegrating agent are mixed into the skeleton that main adjuvant constitutes this tablet in the proper ratio simultaneously, make tablet rapidly even disintegrate in the oral cavity become tiny powder, and with swallowing into stomach, simultaneously, the medicine stripping reaches the effect of oral rapid onset.And this kind tablets is convenient, especially is fit to emergency treatment patient such as old man under part dysphagia or the special environment, the coma patient medication.
The present invention prepares solid dispersion in advance with tramadol hydrochloride and solid dispersion carrier, and then by prescription and residue adjuvant, filler, disintegrating agent, correctives, lubricant uniform mixing, adopt the powder direct compression, dry granulation tabletting or wet granule compression tablet, promptly.Not only preparation technology is simple for it, taking convenience, especially be fit to the medication of old man, child, emergency treatment patient, coma patient and dysphagia patients, and taking under the anhydrous situation such as field work, tourism, it is not taken the restriction of water, and, to indication absorb fast, rapid-action, reach the peak early, curative effect is obvious.
The specific embodiment
Further describe the specific embodiment of the present invention below in conjunction with embodiment
Embodiment 1
The present invention adopts following proportioning formulation to form.
Tramadol hydrochloride 5%, polyethylene glycol 6000 (PEG6000) 35%, starch 48%, low-substituted hydroxypropyl cellulose (L-HPC) 8%, stevioside 3.5%, magnesium stearate 0.5%.All on sale on the above-mentioned raw materials market, easily purchase.
Its preparation method is: take by weighing each composition by the ormal weight in the above-mentioned prescription.With the polyethylene glycol 6000 87.5mg heating and melting that takes by weighing, add the tramadol hydrochloride powder 12.5mg that pulverized 100 mesh sieves in advance earlier, stir, then the fused mass cryogenic quenching is solidified crushing screening.Add starch 120mg, low-substituted hydroxypropyl cellulose 20mg, stevioside 8.75mg, wet granulation adds magnesium stearate 1.25mg tabletting, promptly.Be 18min its disintegration, and taste is relatively more bitter.
Embodiment 2
The present invention adopts following proportioning formulation to form.
Tramadol hydrochloride 10%, Macrogol 4000 (PEG4000) 27.8%, starch 45%, low-substituted hydroxypropyl cellulose (L-HPC) 8.7%, stevioside 8%, magnesium stearate 0.5%.All on sale on the above-mentioned raw materials market, easily purchase.
Its preparation method is: take by weighing each composition by the ormal weight in the above-mentioned prescription.With the Macrogol 4000 69.5mg heating and melting that takes by weighing, add the tramadol hydrochloride powder 25mg that pulverized 100 mesh sieves in advance earlier, stir, then the fused mass cryogenic quenching is solidified crushing screening.Add starch 112.5mg, low-substituted hydroxypropyl cellulose 21.75mg, stevioside 20mg, wet granulation adds magnesium stearate 1.25mg tabletting, promptly.Be 16min its disintegration, and taste is relatively more bitter.
Embodiment 3
The present invention adopts following proportioning formulation to form.
Tramadol hydrochloride 15%, Macrogol 4000 (PEG4000) 38.8%, polyethylene glycol 6000 (PEG6000) 13.9%, microcrystalline Cellulose (MCC PH102) 12%, low-substituted hydroxypropyl cellulose (L-HPC) 8%, stevioside 12%, Pulvis Talci 0.3%.All on sale on the above-mentioned raw materials market, easily purchase.
Its preparation method is: take by weighing each composition by the ormal weight in the above-mentioned prescription.With Macrogol 4000 97mg and polyethylene glycol 6000 34.75mg, heating and melting adds the tramadol hydrochloride powder 37.5mg that pulverized 100 mesh sieves in advance, stirs, and then the fused mass cryogenic quenching is solidified crushing screening earlier.Add microcrystalline Cellulose (MCCpH102) 30mg, low-substituted hydroxypropyl cellulose 20mg, stevioside 30mg, wet granulation adds Pulvis Talci 0.75mg tabletting.Be 8min its disintegration, and taste is relatively more bitter.
Embodiment 4
The present invention adopts following proportioning formulation to form.
Tramadol hydrochloride 25%, You Teqi (Eudragit E100) 40%, microcrystalline Cellulose (MCC PH101) 12%, low-substituted hydroxypropyl cellulose (L-HPC) 8%, crospolyvinylpyrrolidone (PVPP) 8%, starch 4%, stevioside 2%, Pulvis Talci 1%.All on sale on the above-mentioned raw materials market, easily purchase.
Its preparation method is: take by weighing each composition by the ormal weight in the above-mentioned prescription.Earlier You Teqi (Eudragit E100) 100mg is heated fusion with dehydrated alcohol in 50 ℃ of water-baths, add tramadol hydrochloride 62.5mg dissolving, rotary evaporation removes and desolvates to drying crushing screening under the vacuum condition.Add microcrystalline Cellulose (MCCPH101) 30mg, low-substituted hydroxypropyl cellulose (L-HPC) 20mg, crospolyvinylpyrrolidone 20mg, starch 10mg, stevioside 5mg, Pulvis Talci 2.5mg, mix homogeneously powder direct compression.Be 3min its disintegration, and bitterness alleviates.
Embodiment 5
The present invention adopts following proportioning formulation to form.
Tramadol hydrochloride 12.8%, You Teqi (Eudragit S100) 13.9%, low-substituted hydroxypropyl cellulose (L-HPC) 12%, carboxymethyl starch sodium (CMS-Na) 10%, dextrin 38.8%, A Siba is sweet 12%, sodium lauryl sulphate 0.5%.All on sale on the above-mentioned raw materials market, easily purchase.
Its preparation method is: take by weighing each composition by the ormal weight in the above-mentioned prescription.With You Teqi (Eudragit S100) 34.75mg, dissolve in stirring at room earlier, add tramadol hydrochloride 32mg dissolving, constantly boil off solvent to dry, crushing screening with dehydrated alcohol.Add low-substituted hydroxypropyl cellulose 30mg, carboxymethyl starch sodium 25mg, dextrin 97mg, the sweet 30mg of A Siba, sodium lauryl sulphate 1.25mg, mix homogeneously, powder direct compression.Be 8min its disintegration, and bitterness alleviates.
Embodiment 6
The present invention adopts following proportioning formulation to form.
Tramadol hydrochloride 40%, Macrogol 4000 (PEG4000) 23.5%, polyethylene glycol 6000 (PEG6000) 11.8%, microcrystalline Cellulose (MCCPH102) 14.2%, stevioside 6%, low-substituted hydroxypropyl cellulose (L-HPC) 4%, Pulvis Talci 0.5%.All on sale on the above-mentioned raw materials market, easily purchase.
Its preparation method is: take by weighing each composition by the ormal weight in the above-mentioned prescription.Earlier with Macrogol 4000 (PEG4000) 58.75mg and polyethylene glycol 6000 (PEG6000) 29.5mg heating and melting, add the tramadol hydrochloride powder 100mg that pulverized 100 mesh sieves in advance, stir, then the melts cryogenic quenching is solidified, powder sieves, and adds microcrystalline Cellulose (MCCPH102) 35.5mg, low-substituted hydroxypropyl cellulose (L-HPC10mg), stevioside 15mg, wet granulation adds Pulvis Talci 1.25mg tabletting.Be 4min its disintegration, and bitterness is arranged slightly.
Claims (7)
1, a kind of tramadol hydrochloride oral cavity disintegration tablet, by tramadol hydrochloride, the solid dispersion carrier, filler, disintegrating agent, correctives, lubricant are formed, and this tablet is by mass percentage:
Tramadol hydrochloride 5-40%, solid dispersion carrier 5-60%, filler 5-50%, disintegrating agent 3-35%, correctives 1-20%, lubricant 0-1%.
2, tramadol hydrochloride oral cavity disintegration tablet as claimed in claim 1, wherein said solid dispersion carrier is ethyl cellulose or Polyethylene Glycol (PEG) or polyvinylpyrrolidone or poloxamer or You Teqi and composition thereof, said Polyethylene Glycol comprises, PEG6000 and PEG4000, said You Teqi comprises Eudragit EC10cp, Eudragit E100, Eudragit S100.
3, tramadol hydrochloride oral cavity disintegration tablet as claimed in claim 1, wherein said filler are microcrystalline Cellulose or dextrin or lactose or starch and mixture.
4, tramadol hydrochloride oral cavity disintegration tablet as claimed in claim 1, wherein said disintegrating agent be low-substituted hydroxypropyl cellulose or XLPE ketopyrrolidine or carboxymethyl starch receive and composition thereof.
5, tramadol hydrochloride oral cavity disintegration tablet as claimed in claim 1, wherein said correctives are natural or artificial sweeting agents such as mannitol or lactose or stevioside or A Siba be sweet.
6, such as claim 1 the tramadol hydrochloride oral cavity disintegration tablet of art, wherein said lubricant is magnesium stearate or Stepanol MG or sodium lauryl sulphate or Pulvis Talci.
7, the preparation method of tramadol hydrochloride oral cavity disintegration tablet as claimed in claim 1 comprises following processing step:
At first tramadol hydrochloride and solid dispersion carrier are prepared into solid dispersion by formula ratio with fusion method or solvent method, press formula ratio and filler, disintegrating agent, correctives, lubricant uniform mixing then.Adopt the powder direct compression, dry granulation tabletting or wet granule compression tablet, promptly.
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| Application Number | Priority Date | Filing Date | Title |
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| CNB2004100603698A CN100348180C (en) | 2004-12-24 | 2004-12-24 | Oral disintegration tablet of tramadol hydrochloride and preparation method |
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|---|---|---|---|
| CNB2004100603698A CN100348180C (en) | 2004-12-24 | 2004-12-24 | Oral disintegration tablet of tramadol hydrochloride and preparation method |
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| CN1660056A true CN1660056A (en) | 2005-08-31 |
| CN100348180C CN100348180C (en) | 2007-11-14 |
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| CNB2004100603698A Expired - Fee Related CN100348180C (en) | 2004-12-24 | 2004-12-24 | Oral disintegration tablet of tramadol hydrochloride and preparation method |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102072901A (en) * | 2010-10-22 | 2011-05-25 | 杭州天迈生物科技有限公司 | Quick detection troche for sulfite in food |
| CN102451164A (en) * | 2010-10-22 | 2012-05-16 | 量子高科（北京）研究院有限公司 | Analgesic oral cavity disintegrating tablet and preparation method thereof |
| CN103385860A (en) * | 2013-06-29 | 2013-11-13 | 北京万全德众医药生物技术有限公司 | Fexofenadine hydrochloride orally disintegrating tablets and preparation method thereof |
| CN103462916A (en) * | 2013-09-12 | 2013-12-25 | 山东天力药业有限公司 | Vitamin C chewable tablet and preparation method thereof |
| TWI449542B (en) * | 2006-03-30 | 2014-08-21 | Nippon Zoki Pharmaceutical Co | Solid pharmaceutical preparation |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2120451T7 (en) * | 1991-09-06 | 2009-11-05 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | COMPOSITION THAT INCLUDES A TRAMADOL AND ACETAMINOPHENE COMPOUND, AND ITS USE. |
| US5645858A (en) * | 1994-10-06 | 1997-07-08 | Ortho Pharmaceutical Corporation | Multilayered controlled release pharmaceutical dosage form |
| ATE284211T1 (en) * | 1997-11-06 | 2004-12-15 | Lannacher Heilmittel | ORAL RETARD PREPARATION CONTAINING TRAMADOL AND METHOD FOR THE PRODUCTION THEREOF |
| CN1528273A (en) * | 2003-10-21 | 2004-09-15 | 宇 周 | Analgesic tramadol hydrochloride oral disintegrating tablet and preparing method thereof |
-
2004
- 2004-12-24 CN CNB2004100603698A patent/CN100348180C/en not_active Expired - Fee Related
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI449542B (en) * | 2006-03-30 | 2014-08-21 | Nippon Zoki Pharmaceutical Co | Solid pharmaceutical preparation |
| CN102072901A (en) * | 2010-10-22 | 2011-05-25 | 杭州天迈生物科技有限公司 | Quick detection troche for sulfite in food |
| CN102451164A (en) * | 2010-10-22 | 2012-05-16 | 量子高科（北京）研究院有限公司 | Analgesic oral cavity disintegrating tablet and preparation method thereof |
| CN102451164B (en) * | 2010-10-22 | 2015-11-25 | 量子高科（北京）研究院有限公司 | A kind of analgesic oral cavity disintegrating tablet and preparation method thereof |
| CN103385860A (en) * | 2013-06-29 | 2013-11-13 | 北京万全德众医药生物技术有限公司 | Fexofenadine hydrochloride orally disintegrating tablets and preparation method thereof |
| CN103462916A (en) * | 2013-09-12 | 2013-12-25 | 山东天力药业有限公司 | Vitamin C chewable tablet and preparation method thereof |
| CN103462916B (en) * | 2013-09-12 | 2016-03-02 | 山东天力药业有限公司 | A kind of Chewable C and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN100348180C (en) | 2007-11-14 |
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