CN105232502A - Orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and preparation method of orally disintegrating tablet - Google Patents
Orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and preparation method of orally disintegrating tablet Download PDFInfo
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- CN105232502A CN105232502A CN201510068373.7A CN201510068373A CN105232502A CN 105232502 A CN105232502 A CN 105232502A CN 201510068373 A CN201510068373 A CN 201510068373A CN 105232502 A CN105232502 A CN 105232502A
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- polacrilin potassium
- fluoxetine hydrochloride
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Abstract
The invention discloses an orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and a preparation method of the orally disintegrating tablet. The orally disintegrating tablet is characterized in that fluoxertine hydrochloride and polacrilin potassium are prepared into an ion exchange compound through a precipitation method, and the ion exchange compound is prepared into the orally disintegrating tablet through a wet granulation technology. Through the technology, the mouthfeel of the medicine can be obviously improved, and meanwhile, an organic solvent is added in the preparation process, so that the water content of the compound is low, the yield of the compound and the drying efficiency in the preparation process can be obviously improved, the occurrence of the sticking problem in the tabletting process is prevented, and the stability is improved.
Description
Technical field
The present invention relates to a kind of oral cavity disintegration tablet containing polacrilin potassium-fluoxetine Hydrochloride complex and preparation method thereof, be characterized in adopting polacrilin potassium to prepare ion exchange complexes as odor mask, 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 ", that is: " three-hypers " refers to high prevalence, high relapse rate and high mortality; Depression rate improves year by year, and treating depression has also become the focus problem of people.
Fluoxetine Hydrochloride is the reuptake inhibitor of a kind of selectivity five hydroxytryptamine for acute stage and maintaining treatment depression (MDD), acute stage and maintaining treatment obsession (OCD, the acute and treatment of chronic neuropathic disease of eating too much at one meal, the acute treatment of Panic disorder, companion or do not accompany agoraphobe, treatment associating fluoxetine and olanzapine, show effect, refractory depression, antidepressant drug relevant to I type bipolar affective disorder of acute depression make the compliance that oral cavity disintegration tablet can improve patient, 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 due to this raw material serious bitter taste, adopt conventional correctives cannot reach taste masking effect, this patent adopts polacrilin potassium as ion exchange resin, complex is formed with fluoxetine Hydrochloride, the bitterness covering medicine that can be fabulous, polacrilin potassium has the character of imbibition simultaneously, as disintegrating agent, can accelerate the disintegrate of medicine in mouth.There is no the patent disclosure adopting this kind of method to prepare Fluoxetine hydrochloride oral cavity disintegrating sheet at present.
The present invention adopts the sedimentation method, centrifuging, and spray drying method prepares clathrate, finally adopts wet granulation system prepare granule and obtain oral cavity disintegration tablet after tabletting, and the technique adopted is conventional production technique used, and preparation efficiency is high, easily realizes industrialization and produces.
Summary of the invention
The object of the invention is to prepare a kind of mouthfeel, disintegrate is better, and preparation process is simple, can realize the fluoxetine Hydrochloride oral cavity disintegration tablet that industrialization is produced.The present invention relates to a kind of oral cavity disintegration tablet containing polacrilin potassium-fluoxetine Hydrochloride complex and preparation method thereof, be characterized in that ion exchange complexes is prepared in employing, and adopt wet granulation technology to make oral cavity disintegration tablet, thus reach taste masking, improve disintegration rate, increase the effects such as yield.
The wet granulation technology that the present invention adopts, is joined by pharmaceutic adjuvant in the complex of the polacrilin potassium-fluoxetine Hydrochloride containing precipitation or centrifugal gained, stirs and granulate in wet granulator; Can also by centrifugal or precipitation gained polacrilin potassium-fluoxetine Hydrochloride complex drying after, mix with other adjuvants, adding binding agent or wetting agent, wet granulation machine stir granulate; Or by the complex of the polacrilin potassium-fluoxetine Hydrochloride of spraying dry gained, mix with other adjuvants, adding binding agent or wetting agent, stirring at wet granulation machine and granulate.
The preparation method of complex is the sedimentation method, centrifuging or spray drying method, wherein the feature of the sedimentation method is, polacrilin potassium and fluoxetine Hydrochloride are fully disperseed in water, complex is formed after stirring, add organic solvent again or directly static after make it precipitate, then draw supernatant liquid and obtain polacrilin potassium-fluoxetine complex; Organic solvent comprises ethanol, methanol, acetone, preferred alcohol, and the ratio of itself and water is 1:5 ~ 20.The feature of centrifuging is, polacrilin potassium and fluoxetine Hydrochloride is fully disperseed in water, and forms complex, then after centrifugal, remove supernatant, obtain polacrilin potassium-fluoxetine Hydrochloride complex.The feature of spray drying method is, polacrilin potassium and fluoxetine Hydrochloride is fully disperseed in water, and forms complex, more spray-driedly obtains polacrilin potassium-fluoxetine Hydrochloride complex.Wherein the weight ratio of fluoxetine Hydrochloride and polacrilin potassium is 1:1 ~ 3, and solid-liquid ratio is 1:20 ~ 80, preferred 1:40 ~ 60.
Adopt wet granulation technology in this technique, pharmaceutic adjuvant is joined in the complex containing the polacrilin potassium-fluoxetine 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.; Correctives includes but not limited to sucralose, acesulfame potassium, strawberry essence etc.; The pharmaceutic adjuvant ratio added is 40% ~ 85%.
Adopt oral cavity disintegration tablet prepared by this method, without bitter numb taste, good mouthfeel, disintegration time is within 20 seconds, and yield is higher, and technique is simply efficient, easily realizes industrialization and produces.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described in further detail, but be not limited to following enforcement
Example.Wherein " % " refers to " % by weight ".
Embodiment 1
In this embodiment, the ratio of fluoxetine Hydrochloride and polacrilin potassium is 1:0.5, and the ratio of polacrilin potassium and fluoxetine Hydrochloride solid and water is 1:50, and selected organic solvent is ethanol, and alcohol water ratio is 1:5, adopts the sedimentation method and add organic solvent to prepare complex.
Preparation technology: by the polacrilin potassium 50g of recipe quantity, fluoxetine Hydrochloride 100g, join in 7.5kg water and stir 1 hour, it is made fully to disperse, and form complex, add 2000L ethanol, static 12h, pump supernatant, 550g mannitol is added again in precipitate, 150g microcrystalline Cellulose, use wet granulator to stir to granulate, 24 mesh sieves are granulated, 50 DEG C of fluid bed dryings, 20min, moisture is reduced to less than 3%, after granulate, add 100g microcrystalline Cellulose again, 20g polyvinylpolypyrrolidone, 10g magnesium stearate, 10g silicon dioxide, 10g acesulfame potassium, mix homogeneously, according to fluoxetine Hydrochloride 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, but aftertaste is slightly bitter.In preparation process, add organic solvent, make complex moisture low, the drying efficiency in complex yield and preparation process can be significantly improved.
Embodiment 2
In this embodiment, the ratio of fluoxetine Hydrochloride and polacrilin potassium is 1:3, and the ratio of polacrilin potassium and fluoxetine Hydrochloride solid and water is 1:30, adopts centrifuging to prepare complex.
Preparation technology: take fluoxetine Hydrochloride 100g, polacrilin potassium 300g, joined in 12kg water, stir, it is made fully to disperse, form complex, after off-line, remove supernatant, add the microcrystalline Cellulose of 100g again, 370g mannitol, use wet granulator stirs, 24 mesh sieves are granulated, granulate after 50 DEG C of spraying dry, add the microcrystalline Cellulose of 100g again, 10g magnesium stearate, 10g silicon dioxide, 10g acesulfame potassium, mix homogeneously, according to fluoxetine Hydrochloride 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 fluoxetine Hydrochloride and polacrilin potassium is 1:2, and the ratio of polacrilin potassium and fluoxetine Hydrochloride solid and water is 1:60.
Preparation technology: take fluoxetine Hydrochloride 100g, polacrilin potassium 200g, joined in 1.8kg water, stir, it is made fully to disperse, form complex, spray drying method is used to make composite powder suspendible liquid again, add the microcrystalline Cellulose of 100g again, 460g lactose, after using wet granulator mix homogeneously, add appropriate 30% ethanol and stir granulation, oscillating granulator is crossed 20 mesh sieves and is granulated, granulate after 50 DEG C of oven dryings, add 100g microcrystalline Cellulose again, 20g low-substituted hydroxypropyl cellulose, 10g magnesium stearate, 10g sucralose, mix homogeneously, according to fluoxetine Hydrochloride 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
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 fluoxetine Hydrochloride 100g, adds 550g 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; 20g polyvinylpolypyrrolidone, 10g magnesium stearate, 10g silicon dioxide; 10g acesulfame potassium, mix homogeneously, according to fluoxetine Hydrochloride content in granule; the heavy also tabletting of conversion sheet, disintegration rate 40 ± 5s, mouthfeel bitterness is heavier.
Embodiment 5
Do not adopt polacrilin potassium to process raw material in this embodiment prescription, adopt acrylic resin as odor mask, all the other adjuvants are identical with prescription two.
Preparation technology: fluoxetine Hydrochloride and acrylic resin are dispersed in after stirring in the alcoholic solution of 50%; be dried rear pulverizing again, then add the microcrystalline Cellulose of 100g, 370g mannitol; use wet granulator stirs; 24 mesh sieves are granulated, granulate after 50 DEG C of spraying dry, then add 100g microcrystalline Cellulose; 10g magnesium stearate; 10g silicon dioxide, 10g acesulfame potassium, mix homogeneously.According to fluoxetine Hydrochloride content in granule, the heavy and tabletting of conversion sheet, disintegration rate 55 ± 5s, mouthfeel is sweet and be with refrigerant sense, and aftertaste is more bitter.
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 prescription mouthfeels are all good, and without bitterness, and disintegration rate is all within 20s.And prescription 5 does not process raw material, adopt Common flavoring agents, bitter numb taste is serious, and Orally disintegrating speed is far longer than all the other four prescriptions of practical polacrilin potassium.And prescription 6 uses conventional odor mask acrylic resin to process raw material, although be significantly increased compared with Common flavoring agents in mouthfeel, but aftertaste is slightly bitter, and the prescription project of disintegration time and use polacrilin potassium, significant prolongation, close to 1 minute, and due to acrylic resin water insoluble, must organic solvent be added in preparation process, be unfavorable for environmental protection.And the solid mass that dry rear formation is harder, just can granulate after needing pulverizing, complex process, preparation efficiency is lower.
Contrast known, oral cavity disintegration tablet containing polacrilin potassium-fluoxetine Hydrochloride complex described in the present invention and preparation method thereof, can effectively taste masking, improve the effects such as disintegration rate, and preparation is simple, efficiency is higher, is easy to industrialization production.
Claims (10)
1. one kind contains oral cavity disintegration tablet of polacrilin potassium and fluoxetine Hydrochloride complex and preparation method thereof, and its feature comprises makes ion exchange complexes by fluoxetine Hydrochloride and polacrilin potassium, then adds other pharmaceutic adjuvant, adopts wet granulation technology to make oral cavity disintegration tablet; Wherein the weight ratio of fluoxetine Hydrochloride and polacrilin potassium is 1:1 ~ 3, and the pharmaceutic adjuvant ratio added is 40% ~ 85%, and the preparation method of complex is natural sedimentation method, centrifugal or spray drying method.
2. the oral cavity disintegration tablet containing polacrilin potassium and fluoxetine Hydrochloride complex according to claim 1, it is characterized in that, the sedimentation method are fully disperseed in water polacrilin potassium and fluoxetine Hydrochloride, and form complex, again through precipitation, or after adding organic solvent deposit, remove supernatant, obtain polacrilin potassium-fluoxetine Hydrochloride complex; Centrifuging is fully disperseed in water polacrilin potassium and fluoxetine Hydrochloride, and form complex, then after centrifugal, remove supernatant, obtain polacrilin potassium-fluoxetine complex; Spray drying method is fully disperseed in water polacrilin potassium and fluoxetine Hydrochloride, and form complex, more spray-driedly obtain polacrilin potassium--fluoxetine Hydrochloride complex.
3. the oral cavity disintegration tablet containing polacrilin potassium and fluoxetine Hydrochloride complex according to claim 2, it is characterized in that: polacrilin potassium and fluoxetine Hydrochloride are fully disperseed in water, wherein solid-liquid ratio is 1:20 ~ 80.
4. the oral cavity disintegration tablet containing polacrilin potassium and fluoxetine Hydrochloride complex according to claim 3, is characterized in that: the solid-liquid ratio that polacrilin potassium and fluoxetine Hydrochloride fully disperse in water is 1:40 ~ 60.
5. the oral cavity disintegration tablet containing polacrilin potassium and fluoxetine Hydrochloride complex according to claim 2, is characterized in that: the organic solvent added in the sedimentation method comprises ethanol, methanol, acetone, and the ratio of itself and water is 1:5 ~ 20.
6. the oral cavity disintegration tablet containing polacrilin potassium and fluoxetine Hydrochloride complex according to claim 5, is characterized in that: the organic solvent added is ethanol.
7. contain the oral cavity disintegration tablet of polacrilin potassium and fluoxetine Hydrochloride complex according to claim 1; it is characterized in that: the present invention adopts wet granulation technology; be pharmaceutic adjuvant is joined in the complex of the polacrilin potassium-fluoxetine Hydrochloride containing precipitation or centrifugal gained, stir in wet granulator and granulate.
8. contain the oral cavity disintegration tablet of polacrilin potassium and fluoxetine Hydrochloride complex according to claim 1; it is characterized in that: the present invention adopts wet granulation technology; can also by centrifugal or precipitation gained polacrilin potassium-fluoxetine Hydrochloride complex drying after; mix with other adjuvants; adding binding agent or wetting agent, stirring at wet granulation machine and granulate.
9. contain the oral cavity disintegration tablet of polacrilin potassium and fluoxetine Hydrochloride complex according to claim 1; it is characterized in that: the present invention adopts wet granulation technology; by the complex of the polacrilin potassium-fluoxetine Hydrochloride of spraying dry gained; mix with other adjuvants; adding binding agent or wetting agent, stirring at wet granulation machine and granulate.
10. contain the oral cavity disintegration tablet of polacrilin potassium and fluoxetine Hydrochloride complex according to claim 1, it is characterized in that: the pharmaceutic adjuvant added includes but not limited to filler, disintegrating agent, lubricant, fluidizer, correctives, filler includes but not limited to lactose, mannitol, microcrystalline Cellulose, disintegrating agent includes but not limited to polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, low substituted cellulose; Correctives includes but not limited to sucralose, acesulfame potassium, strawberry essence.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510068373.7A CN105232502A (en) | 2015-02-10 | 2015-02-10 | Orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and preparation method of orally disintegrating tablet |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510068373.7A CN105232502A (en) | 2015-02-10 | 2015-02-10 | Orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and preparation method of orally disintegrating tablet |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005065640A1 (en) * | 2004-01-06 | 2005-07-21 | Panacea Biotec Ltd. | Compositions of buccal dosage forms for extended drug release and the process of preparing such compositions |
| CN1981746A (en) * | 2005-12-13 | 2007-06-20 | 量子高科（北京）研究院有限公司 | Fluoxetine hydrochloride oral disintegrant tablets and their production |
| CN102430122A (en) * | 2005-12-13 | 2012-05-02 | 量子高科（北京）研究院有限公司 | Fluoxertine hydrochloride orally disintegrating tablet 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 |
-
2015
- 2015-02-10 CN CN201510068373.7A patent/CN105232502A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005065640A1 (en) * | 2004-01-06 | 2005-07-21 | Panacea Biotec Ltd. | Compositions of buccal dosage forms for extended drug release and the process of preparing such compositions |
| CN1981746A (en) * | 2005-12-13 | 2007-06-20 | 量子高科（北京）研究院有限公司 | Fluoxetine hydrochloride oral disintegrant tablets and their production |
| CN102430122A (en) * | 2005-12-13 | 2012-05-02 | 量子高科（北京）研究院有限公司 | Fluoxertine hydrochloride orally disintegrating tablet 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: 20160113 |
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