CN104382870A - Compound containing polacrilin potassium-paroxetine - Google Patents
Compound containing polacrilin potassium-paroxetine Download PDFInfo
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- CN104382870A CN104382870A CN201410592262.1A CN201410592262A CN104382870A CN 104382870 A CN104382870 A CN 104382870A CN 201410592262 A CN201410592262 A CN 201410592262A CN 104382870 A CN104382870 A CN 104382870A
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- paroxetine
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- polacrilin potassium
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Abstract
The invention discloses an orally disintegrating tablet of a compound containing polacrilin potassium-paroxetine, and a preparation method of the orally disintegrating tablet. The orally disintegrating tablet is characterized in that an ion exchange compound is prepared from paroxetine hydrochloride and polacrilin potassium by adopting a precipitation method; and the orally disintegrating tablet is prepared by adopting a wet granulation process. Through the process, the taste of the medicine can be significantly improved, meanwhile, an organic solvent is added to the preparation process, so that the compound is low in moisture content, and is capable of effectively improving the yield of the compound and the drying efficiency in the preparation process, preventing the sticking problem in the tabletting process, and improving the stability.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to a kind of oral cavity disintegration tablet containing polacrilin potassium-paroxetine complex and preparation method thereof, be characterized in adopting the sedimentation method to prepare ion exchange complexes, and adopt wet granulation technology to make oral cavity disintegration tablet, thus reach taste masking, improve disintegration rate, increase yield, improve the effects such as stability.
Background technology
Depression is a kind of common mood disorders, can be caused by a variety of causes, low for main clinical characteristics with remarkable and lasting mental state, and mental state is low unbecoming with its situation, and having bradyphrenia, the symptoms such as action minimizing, can there is suicidal thought and behavior in severe patient.In addition, from the characteristics of incidence of depression, depression also has " three-hypers ", i.e. high prevalence, high relapse rate and high mortality; Along with depression rate improves year by year, the treatment of depression has also become the focus problem of people.
The features such as paroxetine is a kind of selectivity 5 hydroxytryptamine re uptake blocade, belongs to third generation antidepressants, and clinical proof has good effect, untoward reaction is lacked, and be applicable to depression in old age.Antidepressant drug makes the compliance that oral cavity disintegration tablet can improve patient, and it is particularly suitable for the more weak gerontal patient of function of deglutition.Domestic at present have marketed tablet, but there is no oral cavity disintegration tablet sale.But because the bitter numb taste of this raw material is serious, adopt conventional correctives cannot reach taste masking effect, this patent adopts polacrilin potassium as ion exchange resin, forms complex, make it have good mouthfeel with paroxetine.
Patent CN1853631A discloses a kind of oral cavity disintegration tablet adopting acrylic resin to carry out coating and taste masking.Patent CN10263129A discloses a kind of acrylic resin or polacrilin potassium of adopting to a kind of oral cavity disintegration tablet of medicine enclose, but and undeclared clathrate preparation method.Patent CN1140411A disclose a kind of polacrilin potassium and paroxetine are stirred in water after add the method that other adjuvants prepare paroxetine oral liquid, and prepare solid preparation, need the polacrilin potassium-paroxetine complex solidification that will be formed, the general method stirring rear sucking filtration that adopts is precipitated thing, dry again, but use the method to have following drawback: the composite particles 1, formed is very tiny, be very easy to form fine and close filter cake in filter process, need ceaselessly change and clean filter opening, sucking filtration efficiency is extremely low; Further, due to filter opening cleaning and replacing, cause complex to lose comparatively large, yield is lower, generally below 70%; 2, because polacrilin potassium itself is a kind of ion exchange resin, have the character of imbibition, and not easily dry after water suction, granulate if be used alone water, granule is not easily dried, and generally more than 5%, causes sticking in tableting processes, and bad stability.The present invention adopts the sedimentation method, and after prepared by clathrate, only need add organic solvent and leave standstill 12 ~ 24 hours, after leaving standstill, there is fine and close precipitate in visible lower floor, and upper solution is clarified, and removes supernatant, directly adds other excipient, can granulate, and dry.Simultaneously owing to adding organic solvent, solvent evaporation rate can be accelerated in drying course, make moisture content arrive less than 3% rapidly, prevent in sticking in the tableting processes caused because moisture is high and put procedure the problems such as bad stability.
Summary of the invention
The object of the invention is to prepare a kind of mouthfeel good, disintegrate is very fast, and preparation process is simple, and yield is higher, the paroxetine oral cavity disintegration tablet of good stability.The present invention relates to a kind of oral cavity disintegration tablet containing polacrilin potassium-paroxetine complex and preparation method thereof, be characterized in adopting the sedimentation method to prepare ion exchange complexes, and adopt wet granulation technology to make oral cavity disintegration tablet, thus reach taste masking, improve disintegration rate, increase yield, improve the effects such as stability.
The preparation method of complex is the sedimentation method, it is characterized in that, polacrilin potassium and paroxetine hydrochloride is fully disperseed in water, and the weight ratio of paroxetine and polacrilin potassium is 1:1 ~ 3, and solid-liquid ratio is 1:20 ~ 80; Form complex after stirring, then add organic solvent static after make it precipitate, then draw supernatant liquid, or first static, add organic solvent again after removing supernatant, obtain the complex containing certain proportion water and organic solvent.
Add organic solvent and comprise ethanol, methanol, acetone etc., wherein first-selected ethanol; The ratio of organic solvent and water is 1:5 ~ 10.
Adopt wet granulation technology in this technique, pharmaceutic adjuvant is joined in the complex containing the polacrilin potassium-paroxetine hydrochloride of organic solvent and water, stir in wet granulator and granulate, and at 40 ~ 70 DEG C, be dried to moisture content be 1 ~ 3%.The pharmaceutic adjuvant added comprises filler, disintegrating agent, lubricant, fluidizer correctives etc., and filler comprises lactose, mannitol, microcrystalline Cellulose etc., and disintegrating agent comprises polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, low substituted cellulose etc.; The pharmaceutic adjuvant ratio added is 50% ~ 80%.
Adopt oral cavity disintegration tablet prepared by this method, without bitter numb taste, good mouthfeel, disintegration time is within 20 seconds, yield is higher, is greater than 90%, and preparation efficiency is higher, in dry 2 hours, moisture content can reach less than 3%, prevents sticking in tableting processes, and increases the stability in put procedure.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, but be not limited to following embodiment.Wherein " % " refers to " % by weight ".
embodiment 1
In this embodiment, the ratio of paroxetine and polacrilin potassium is 1:1, and the ratio of polacrilin potassium and paroxetine solid and water is 1:50, and selected organic solvent is ethanol, and alcohol water ratio is 1:5.
Preparation technology: by the polacrilin potassium 100g of recipe quantity, paroxetine hydrochloride 114g, join in 10kg water and stir 1 hour, it is made fully to disperse, and form complex, add 2000L ethanol, static 12h, pump supernatant, 536g mannitol is added again in precipitate, 100g microcrystalline Cellulose, use wet granulator to stir to granulate, 24 mesh sieves are granulated, 50 DEG C of fluid bed dryings, after granulate, add 100g microcrystalline Cellulose again, 2g polyvinylpolypyrrolidone, 1g magnesium stearate, 1g silicon dioxide, 1g acesulfame potassium, mix homogeneously, according to paroxetine content in granule, the heavy also tabletting of conversion sheet, yield can arrive more than 90%, disintegration rate 15 ± 3s, mouthfeel is sweet and be with refrigerant sense.
embodiment 2
In this embodiment, the ratio of paroxetine and polacrilin potassium is 1:3, and the ratio of polacrilin potassium and paroxetine solid and water is 1:30.
Preparation technology: take paroxetine hydrochloride 114g, polacrilin potassium 300g, joined in 2000g water, stir, it is made fully to disperse, form complex, supernatant is pumped after static, add 60ml ethanol again, add the microcrystalline Cellulose of 200g simultaneously, 356g mannitol, use wet granulator stirs, 24 mesh sieves are granulated, granulate after 50 DEG C of spraying dry, add 200g microcrystalline Cellulose again, 2g polyvinylpolypyrrolidone, 1g magnesium stearate, 1g silicon dioxide, 1g acesulfame potassium, mix homogeneously, according to paroxetine content in granule, the heavy also tabletting of conversion sheet, yield can arrive more than 90%, disintegration rate 15 ± 3s, mouthfeel is slightly sweet and be with refrigerant sense.
embodiment 3
In this embodiment, the ratio of paroxetine and polacrilin potassium is 1:2, and the ratio of polacrilin potassium and paroxetine solid and water is 1:60.
Preparation technology: take paroxetine hydrochloride 114g, polacrilin potassium 200g, joined in 1.8kg water, stir, it is made fully to disperse, form complex, supernatant is pumped after static, add 40ml ethanol again, add the microcrystalline Cellulose of 100g simultaneously, 446g lactose, use wet granulator stirs, 20 mesh sieves are granulated, granulate after 50 DEG C of oven dryings, add 100g microcrystalline Cellulose again, 2g low-substituted hydroxypropyl cellulose, 1g magnesium stearate, 1g acesulfame potassium, mix homogeneously, according to paroxetine content in granule, the heavy also tabletting of conversion sheet, yield can arrive more than 90%, disintegration rate 15 ± 3s, mouthfeel is slightly sweet and be with refrigerant sense.
embodiment 4
This embodiment prescription Central Plains supplementary product consumption is identical with embodiment 3, but preparation technology adopts suction method sediment separate out, does not add organic solvent.
Preparation technology: take paroxetine hydrochloride 114g, polacrilin potassium 200g, joined in 1.8kg water, stir, it is made fully to disperse, form complex, filter after removing liquid, dry, according to the amount of clathrate, according to prescription ratio conversion microcrystalline Cellulose, lactose, add wetting agent water again, use wet granulator stirs, 20 mesh sieves are granulated, granulate after 50 DEG C of oven dryings, add microcrystalline Cellulose again, low-substituted hydroxypropyl cellulose, magnesium stearate, sucralose, mix homogeneously, according to paroxetine content in granule, the heavy also tabletting of conversion sheet, disintegration rate 15 ± 3s, mouthfeel is slightly sweet, without bitter numb taste.
embodiment 5
Do not adopt polacrilin potassium to process raw material in this embodiment prescription, adopt common odor mask, the polacrilin potassium of 10% is changed into the polyvinylpolypyrrolidone of 10%, all the other adjuvants are identical with prescription one.
Preparation technology: by paroxetine hydrochloride 114g, adds 536g mannitol, 100g microcrystalline Cellulose, polyvinylpolypyrrolidone 100g; mix homogeneously, use wet granulator to stir and granulate, 24 mesh sieves are granulated; 50 DEG C of fluid bed dryings, after granulate, then add 100g microcrystalline Cellulose; 2g polyvinylpolypyrrolidone, 1g magnesium stearate, 1g silicon dioxide; 1g acesulfame potassium, mix homogeneously, according to paroxetine content in granule; heavy and the tabletting of conversion sheet, disintegration rate 40 ± 5s, mouthfeel is sweet and be with refrigerant sense.
embodiment 6
Investigate sample indices prepared by embodiment 1,2,3,4,5, comparing result is as follows:
From embodiment 1,2,3,4 result, after adopting polacrilin potassium to process raw material, four prescriptions are all without bitter numb taste, and disintegration rate is all within 20s, and dissolution reaches more than 90%, and related substance is all remarkable in required standard.And prescription 5 does not process raw material, adopt common odor mask, bitter numb taste is serious, and Orally disintegrating speed is far longer than all the other four prescriptions of practical polacrilin potassium, and preparation stability is compared with four prescriptions of employing polacrilin potassium process, obviously reduces.
Wherein prescription 1,2,3 adopts the sedimentation method to prepare clathrate, and adds organic solvent, and prescription 4 adopts suction method to prepare, pure water phase, does not all add organic solvent before and after preparation.Prescription 4 and other three prescriptions compare, and yield obviously lowers, and granule water content is greater than 5%, 0 day related substance and other three prescriptions substantially as broad as long, but accelerate after January single assorted and always assortedly increase obviously, stability is obviously not as other three prescriptions.Contrast known, oral cavity disintegration tablet containing polacrilin potassium-paroxetine complex described in the present invention and preparation method thereof, can effectively taste masking, improve disintegration rate, increase yield, the effects such as raising stability.
Claims (8)
1. contain a pharmaceutical composition for medicinal active ingredient polacrilin potassium and paroxetine and pharmaceutically acceptable pharmaceutic adjuvant, wherein added pharmaceutic adjuvant ratio is 50% ~ 80%; Its preparation method comprises the employing sedimentation method and paroxetine and polacrilin potassium is made ion exchange complexes, then adds organic solvent and other pharmaceutic adjuvant, adopts wet granulation technology to make oral cavity disintegration tablet.
2. ion exchange complexes according to claim 1, is characterized in that the weight ratio of paroxetine and polacrilin potassium is 1:1 ~ 3.
3. according to claim 1, the preparation method of complex is the sedimentation method, it is characterized in that, polacrilin potassium and paroxetine are fully disperseed in water, and form complex, add organic solvent deposit again, or first precipitate and remove supernatant afterwards and add organic solvent again, obtain the solid sediment containing certain proportion water and organic solvent.
4. according to claim 3, polacrilin potassium and paroxetine are fully disperseed in water, wherein solid-liquid ratio is 1:20 ~ 80; The ratio adding organic solvent and water is 1:5 ~ 20.
5. according to claim 3, the organic solvent added comprises ethanol, methanol, acetone.
6. according to claim 5, the first-selected ethanol of organic solvent.
7. according to claim 1, the present invention adopts wet granulation technology, is itself and pharmaceutic adjuvant to be joined in the complex containing the polacrilin potassium-paroxetine of organic solvent and water, stirs and granulate in wet granulator.
8. according to claim 7, the pharmaceutic adjuvant added includes but not limited to filler, disintegrating agent, lubricant, fluidizer, correctives; Wherein filler includes but not limited to that lactose, mannitol, microcrystalline Cellulose, disintegrating agent include but not limited to polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, low substituted cellulose, and correctives includes but not limited to sucralose, acesulfame potassium, strawberry essence.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201410592262.1A CN104382870A (en) | 2014-10-30 | 2014-10-30 | Compound containing polacrilin potassium-paroxetine |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410592262.1A CN104382870A (en) | 2014-10-30 | 2014-10-30 | Compound containing polacrilin potassium-paroxetine |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1140411A (en) * | 1994-02-03 | 1997-01-15 | 史密丝克莱恩比彻姆有限公司 | Oral liquid compositions contg. paroxetine resinate |
| WO2001058449A1 (en) * | 2000-02-11 | 2001-08-16 | Smithkline Beecham Plc | Water dispersible formulation of paroxetine |
| CN102525966A (en) * | 2010-12-13 | 2012-07-04 | 江苏万全特创医药生物技术有限公司 | Tablet containing paroxetine and preparation method thereof |
| CN102631329A (en) * | 2012-04-12 | 2012-08-15 | 无锡万全医药技术有限公司 | Oral paroxetine disintegrating tablet and preparation process thereof |
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2014
- 2014-10-30 CN CN201410592262.1A patent/CN104382870A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1140411A (en) * | 1994-02-03 | 1997-01-15 | 史密丝克莱恩比彻姆有限公司 | Oral liquid compositions contg. paroxetine resinate |
| WO2001058449A1 (en) * | 2000-02-11 | 2001-08-16 | Smithkline Beecham Plc | Water dispersible formulation of paroxetine |
| CN102525966A (en) * | 2010-12-13 | 2012-07-04 | 江苏万全特创医药生物技术有限公司 | Tablet containing paroxetine and preparation method thereof |
| CN102631329A (en) * | 2012-04-12 | 2012-08-15 | 无锡万全医药技术有限公司 | Oral paroxetine disintegrating tablet and preparation process thereof |
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Application publication date: 20150304 |