CN102631329A - Oral paroxetine disintegrating tablet and preparation process thereof - Google Patents
Oral paroxetine disintegrating tablet and preparation process thereof Download PDFInfo
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- CN102631329A CN102631329A CN2012101056823A CN201210105682A CN102631329A CN 102631329 A CN102631329 A CN 102631329A CN 2012101056823 A CN2012101056823 A CN 2012101056823A CN 201210105682 A CN201210105682 A CN 201210105682A CN 102631329 A CN102631329 A CN 102631329A
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- paroxetine
- stripping
- oral tablet
- quick disintegrate
- ability
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Abstract
The invention relates to an oral paroxetine solid preparation capable of being rapidly disintegrated and dissolved and a preparation process thereof. The solid preparation has the characteristics of maintaining favorable taste in the condition of using a covering process and a taste masking agent, and rapidly expanding and dispersing in water to dissolve the paroxetine out, thus the dissolution rate and biological availability of the preparation are greatly enhanced, and the therapeutic effect can be more efficiently and rapidly achieved.
Description
Technical field
The present invention relates to a kind of pharmaceutical products and preparation technology, is paroxetine oral tablet of the quick disintegrate of a kind of ability, stripping and preparation method thereof.
Background technology
Depression is a kind of common mood disorders, can be caused by a variety of causes, and low with remarkable and persistent mental state is main clinical characteristics, and mental state is low unbecoming with its situation, and suicidal thought and behavior can appear in severe patient.Most cases have the tendency of outbreak repeatedly, and the great majority that at every turn show effect can be alleviated, and part can have residual symptom or transfer to chronic.
Depression has at least 10% patient maniac access can occur, and should be diagnosed as the two-phase obstacle this moment.Our depression of often saying is meant serious symptom depression (major depression) clinically in fact in addition, has 16% people influenced by it in certain period throughout one's life among the crowd.Suffer from depression except paying serious emotion and social costs, economic cost also is huge.According to World Health Organization's statistics, depression has become the world's the 4th big illness, expects the year two thousand twenty, possibly become the second largest disease that is only second to coronary heart disease.
Paroxetine is a kind of selectivity 5-HT reuptake inhibitor, during common dose, other mediators is not had obvious influence.Absorb the concentration that improves 5-HT in the nerve synapse gap again through what stop 5-HT, thereby produce antidepressant effect.Can absorb fully after oral, food and medicine all do not influence its absorption.First pass effect is arranged, only 1% be present in body circulation after the administration, plasma protein binding rate is 93%, can be distributed in each histoorgan of whole body, also can pass through mammary gland secretion.Mainly through liver metabolism, generate the uridylic acid chemical compound, after kidney excretes, fraction is discharged from feces through bile secretion.
Experiment shows, these article are fit to the patients with depression of treatment with anxiety neurosis, acts on sooner than tricyclic antidepressants antidepressant, and curative effect is better than imipramine.Be applicable to the various melancholias of treatment.Comprise depression and reactive depression with anxiety, with or without the panic disorder of agoraphobia, and obsession.
Along with the prolongation of human average life and the decline of age growth swallow, the oral tablet administering mode becomes the problem that people pay close attention to.According to estimates, there is 50% people that swallow tablet and capsule are had any problem approximately, influenced the compliance of Drug therapy.In department of pediatrics and old medicine and pharmacology field; To in water, dissolving or suspend, can chew or can in mouth, very big demand being arranged rapid dissolved solid preparation, need not the oral quick dispersible preparation that water and swallowing act just can disperse or dissolve rapidly and just can address this problem.This dosage form can be dispersed or dissolved in saliva rapidly after putting into mouth, but medicine oral or the absorption of intraesophageal mucosa, bioavailability is higher than ordinary preparation, and the side effect that is caused by first pass metabolism also can alleviate.
In the FDA listing Orally disintegrating flake products, preparation process has been taked two kinds of methods basically: freeze-drying (Zydis method) and direct compression process (Orasolv method).Wherein Zydis method and common freeze drying process, for example powder pin freeze-dry process is different, mainly is that principal agent and adjuvant quantitatively are divided in the fixed mold, and lyophilizing is anhydrated, and makes the solid preparation of high porosity.This method is a Britain R.P.Scherer house journal, and each drugmaker takes the mode of consigned processing to carry out the oral cavity disintegration tablet preparation by Scherer company; And the Orasolv method also is to take to become the granule taste masking with gelatin, microcrystalline Cellulose parcel principal agent earlier, adds the mannitol of more amount, and other adds a small amount of effervescent, disintegrating agent, correctives and lubricant, forms with less pressure direct compression.Cima company has this patent technology, and each drugmaker adopts the mode of consigned processing to be processed by Cima company.Present above two kinds of methods Orally disintegrating piece preparation method that is comparative maturities, but its particularity is all arranged, to process conditions and equipment requirements than higher.The solid solution technology is to adopt two kinds of solvents; With first kind of solvent carrier mass is dissolved fully, freezing back adds second kind of solvent, and first kind of solvent exchange come out; Adopt appropriate method to vapor away second kind of solvent then; Obtain the carrier framework of high porosity, after certain method was solidified, direct compression promptly got.Yet, adopt tabletting behind the wet granulation usually, but find that after deliberation wet granulation technology can influence disintegration rate to the existing national conditions of China.The present invention uses clathrate process, can remedy the shortcoming of wet granulation, has guaranteed good disintegrate and stripping simultaneously.
CN1074922C discloses " liquid oral compositions that contains the paroxetine resinate "; Wherein mentioned a kind of taken liquid medicine composition that contains paroxetine-Amberlite IRP-88 coordination compound, had acceptable bioavailability and can be good at covering the bitterness of active component paroxetine.Use acrylic resin or polacrilin resin that the active component paroxetine is carried out enclose to reach the effect of taste masking among the present invention; Process the oral cavity rapid disintegration tablet; Can be dispersed or dissolved in saliva rapidly after putting into mouth; But medicine oral or intraesophageal mucosa absorb, and bioavailability is higher than ordinary preparation, and the side effect that is caused by first pass metabolism also can alleviate.
Summary of the invention
The oral cavity rapid disintegration tablet that the purpose of this invention is to provide a kind of paroxetine is to be applicable to gerontal patient, dysphagia person and taking medicine under the situation of hydropenia, the inconvenience of avoiding tablet and granule to use.
The oral cavity rapid disintegration tablet of the paroxetine that the present invention relates to; The preparation of employing pressing; For reaching the effect that the effect that utilizes saliva in the oral cavity is a disintegratable; Adopt pharmaceutics technological selection prescription, make it can be in the oral cavity not reach disintegrate fast in time of 1 minute, be preferably less than 30 seconds with saliva.In the external slaking test appearance, should disintegrate in 30 seconds, be preferably less than 20 seconds.The invention has the advantages that rapid disintegration tablet disintegrate stripping fast, thereby improve the dissolution rate and the bioavailability of medicine, more effectively bring into play the curative effect effect.
The rapid disintegration tablet that the present invention relates to, active component are paroxetine.
The mixture that contains multiple excipient among the present invention plays respectively and keeps sheet weight, sheet shape, disintegrate, bonding, moistening, flavored action.
The paroxetine oral tablet of the quick disintegrate of the ability that the present invention relates to, stripping is characterized in that using the inclusion agents enclose to reach the effect to the active component taste masking.
The inclusion agents that the present invention relates to is characterized in that inclusion agents can be selected from one or more in acrylic resin and the polacrilin resin.
The paroxetine oral tablet of the quick disintegrate of ability of the present invention, stripping is characterized in that diluent can be selected from one or more in xylitol, the mannitol.
The paroxetine oral tablet of the quick disintegrate of ability of the present invention, stripping is characterized in that disintegrating agent can be selected from receiving one or more of microcrystalline Cellulose, polyvinylpolypyrrolidone, hydroxypropyl cellulose, cross-linked carboxymethyl cellulose.Meet the hundred times that to expand rapidly behind the water, reach the effect that tablet bursts apart.The adding method of disintegrating agent has interior addition, outer addition, inside and outside addition, is preferably inside and outside addition.
The paroxetine oral tablet of the quick disintegrate of ability of the present invention, stripping is characterized in that binding agent can be selected from one or more in starch, the pregelatinized Starch.
The paroxetine oral tablet of the quick disintegrate of ability of the present invention, stripping is characterized in that disintegrating agent can be selected from one or more in magnesium stearate, silicon dioxide, the Pulvis Talci.
The paroxetine oral tablet of the quick disintegrate of ability of the present invention, stripping is characterized in that correctives can be selected from one or more in steviosin, sucralose, acesulfame potassium, the citric acid.
Tablet of the present invention has suitable hardness, can tolerate the various processing under the routine operation condition and its character is not produced significantly influence.Usually hardness is between 30-70 newton.
Tablet of the present invention can be through following method or other suitable method preparations.With inclusion agents the active component paroxetine is carried out enclose; The paroxetine clathrate is crossed 100 mesh sieves and various excipient is crossed 80 mesh sieves, behind the recipe quantity precision weighing, with paroxetine clathrate and correctives, filler, 1/2 minute the disintegrating agent equivalent method mix homogeneously that progressively increases; Add wetting agent; Process soft material, must do granule after the uniform temperature drying, add other 1/2 part disintegrating agent and lubricant mixing again after the granulate tabletting promptly get.
The specific embodiment
Below in conjunction with embodiment further explain the present invention, but do not limit the present invention.
Embodiment 1
Paroxetine is dissolved in the alcoholic solution of acrylic resin, all after the dissolving, 60 ℃ revolve steaming 4 hours, get the paroxetine clathrate:
Preparation technology:
Paroxetine clathrate in the prescription is crossed 100 orders cross 80 orders respectively with all excipient.
With paroxetine clathrate, mannitol, 1/2 polyvinylpolypyrrolidone and 1/2 microcrystalline Cellulose according to the equivalent method mix homogeneously that progressively increases.
Add the starch slurry for preparing, the system soft material, 18 mesh sieves push the granulation of sieving.
Wet grain placed under the 50 degree conditions freeze-day with constant temperature 3 hours.
Dried granule 24 mesh sieve granulate add the residue adjuvant, mixing.
Rotary tablet machine is prepared into 1000 tablets of tablets with following characteristic:
Average sheet heavily is between the 255-265mg; Hardness is between the 30-70 newton;
Average disintegration time was less than 1 minute in the oral cavity, and disintegration time was less than 30 seconds in disintegration tester.
Taste in the oral cavity, free from extraneous odour, no grittiness.
Investigate dissolution according to solubility inspection technique in two appendix of Pharmacopoeia of the People's Republic of China version in 2010,20 minutes dissolution is greater than 95%.
Embodiment 2
Paroxetine is dissolved in the alcoholic solution of acrylic resin, all after the dissolving, 60 ℃ revolve steaming 4 hours, get the paroxetine clathrate:
Preparation technology:
Embodiment 2 is identical with method for preparing and the detection method of embodiment 1.
Average sheet heavily is between the 257-266mg; Hardness is 30-50 newton, and the intraoral disintegration time, disintegration time was less than 30 seconds in disintegration tester less than 1 minute.
Taste in the oral cavity, free from extraneous odour, no grittiness.20 minutes dissolution is greater than 90%.
Embodiment 3
Paroxetine is dissolved in the alcoholic solution of polacrilin potassium, all after the dissolving, 60 ℃ revolve steaming 4 hours, get the paroxetine clathrate:
Preparation technology:
Embodiment 3 is identical with method for preparing and the detection method of embodiment 1.
Average sheet heavily is between the 255-264mg; Hardness is 30-50 newton, and the intraoral disintegration time, disintegration time was less than 30 seconds in disintegration tester less than 1 minute.
Taste in the oral cavity, free from extraneous odour, no grittiness.20 minutes dissolution is greater than 90%.
The present invention describes through above description and instance, more than is described as nonrestrictively, does not limit claim scope of the present invention.
Claims (9)
1. the paroxetine oral tablet of the quick disintegrate of ability, stripping is characterized in that said preparation can keep good mouthfeel under the condition of using inclusion agents enclose and odor mask, and the dispersion of in water, can expanding rapidly, makes the rapid stripping of paroxetine.Weight proportion is following:
2. the paroxetine oral tablet of the quick disintegrate of ability according to claim 1, stripping is characterized in that using the inclusion agents enclose to reach the effect to the active component taste masking.
3. inclusion agents according to claim 2 is characterized in that inclusion agents can be selected from one or more in acrylic resin, the polacrilin resin.
4. the paroxetine oral tablet of the quick disintegrate of ability according to claim 1, stripping is characterized in that diluent can be selected from one or more in xylitol, the mannitol.
5. the paroxetine oral tablet of the quick disintegrate of ability according to claim 1, stripping is characterized in that disintegrating agent can be selected from one or more in microcrystalline Cellulose, polyvinylpolypyrrolidone, the hydroxypropyl methylcellulose.
6. the paroxetine oral tablet of the quick disintegrate of ability according to claim 1, stripping is characterized in that binding agent can be selected from one or more in starch, the pregelatinized Starch.
7. the paroxetine oral tablet of the quick disintegrate of ability according to claim 1, stripping is characterized in that disintegrating agent can be selected from one or more in magnesium stearate, silicon dioxide, the Pulvis Talci.
8. the paroxetine oral tablet of the quick disintegrate of ability according to claim 1, stripping is characterized in that correctives can be selected from one or more in steviosin, sucralose, acesulfame potassium, the citric acid.
9. according to claim 1; The paroxetine oral tablet of the quick disintegrate of this ability, stripping is characterized in that with inclusion agents the active component paroxetine being carried out enclose, and the paroxetine clathrate is crossed 100 mesh sieves and various excipient is crossed 80 mesh sieves; Behind the recipe quantity precision weighing; With paroxetine clathrate and correctives, filler, 1/2 minute the disintegrating agent equivalent method mix homogeneously that progressively increases, add wetting agent, process soft material; Must do granule after the uniform temperature drying, add other 1/2 portion of disintegrating agent and lubricant mixing again after the granulate tabletting promptly get.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012101056823A CN102631329A (en) | 2012-04-12 | 2012-04-12 | Oral paroxetine disintegrating tablet and preparation process thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012101056823A CN102631329A (en) | 2012-04-12 | 2012-04-12 | Oral paroxetine disintegrating tablet and preparation process thereof |
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| CN102631329A true CN102631329A (en) | 2012-08-15 |
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| CN2012101056823A Pending CN102631329A (en) | 2012-04-12 | 2012-04-12 | Oral paroxetine disintegrating tablet and preparation process thereof |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104382870A (en) * | 2014-10-30 | 2015-03-04 | 万全万特制药江苏有限公司 | Compound containing polacrilin potassium-paroxetine |
| CN105232502A (en) * | 2015-02-10 | 2016-01-13 | 万全万特制药江苏有限公司 | Orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and preparation method of orally disintegrating tablet |
| CN107157945A (en) * | 2017-06-02 | 2017-09-15 | 云南省药物研究所 | A kind of tablet of new opioid activator hydrochloride and preparation method thereof |
| CN108938580A (en) * | 2017-05-26 | 2018-12-07 | 万全万特制药江苏有限公司 | Paroxetine hydrochloride oral disintegrating tablet |
| CN111643474A (en) * | 2020-07-20 | 2020-09-11 | 华益药业科技(安徽)有限公司 | Preparation process of paroxetine film coated tablet |
| CN112137970A (en) * | 2019-06-28 | 2020-12-29 | 北京万全德众医药生物技术有限公司 | Paroxetine hydrochloride orally disintegrating tablet and preparation process thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001058449A1 (en) * | 2000-02-11 | 2001-08-16 | Smithkline Beecham Plc | Water dispersible formulation of paroxetine |
| CN1853631A (en) * | 2005-04-27 | 2006-11-01 | 上海秀新臣邦医药科技有限公司 | Fast disintegrant containing paroxetine |
-
2012
- 2012-04-12 CN CN2012101056823A patent/CN102631329A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001058449A1 (en) * | 2000-02-11 | 2001-08-16 | Smithkline Beecham Plc | Water dispersible formulation of paroxetine |
| CN1853631A (en) * | 2005-04-27 | 2006-11-01 | 上海秀新臣邦医药科技有限公司 | Fast disintegrant containing paroxetine |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104382870A (en) * | 2014-10-30 | 2015-03-04 | 万全万特制药江苏有限公司 | Compound containing polacrilin potassium-paroxetine |
| CN105232502A (en) * | 2015-02-10 | 2016-01-13 | 万全万特制药江苏有限公司 | Orally disintegrating tablet containing polacrilin potassium-fluoxertine hydrochloride compound and preparation method of orally disintegrating tablet |
| CN108938580A (en) * | 2017-05-26 | 2018-12-07 | 万全万特制药江苏有限公司 | Paroxetine hydrochloride oral disintegrating tablet |
| CN108938580B (en) * | 2017-05-26 | 2022-09-27 | 万全万特制药江苏有限公司 | Paroxetine hydrochloride oral disintegrating tablet |
| CN107157945A (en) * | 2017-06-02 | 2017-09-15 | 云南省药物研究所 | A kind of tablet of new opioid activator hydrochloride and preparation method thereof |
| CN107157945B (en) * | 2017-06-02 | 2021-03-12 | 云南省药物研究所 | Novel opium delta receptor stimulant hydrochloride tablet and preparation method thereof |
| CN112137970A (en) * | 2019-06-28 | 2020-12-29 | 北京万全德众医药生物技术有限公司 | Paroxetine hydrochloride orally disintegrating tablet and preparation process thereof |
| CN111643474A (en) * | 2020-07-20 | 2020-09-11 | 华益药业科技(安徽)有限公司 | Preparation process of paroxetine film coated tablet |
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