CN105213334A - A kind of vilazodone oral cavity disintegration tablet and preparation method thereof - Google Patents
A kind of vilazodone oral cavity disintegration tablet and preparation method thereof Download PDFInfo
- Publication number
- CN105213334A CN105213334A CN201510584625.1A CN201510584625A CN105213334A CN 105213334 A CN105213334 A CN 105213334A CN 201510584625 A CN201510584625 A CN 201510584625A CN 105213334 A CN105213334 A CN 105213334A
- Authority
- CN
- China
- Prior art keywords
- vilazodone
- oral cavity
- cavity disintegration
- disintegration tablet
- tablet according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of vilazodone oral cavity disintegration tablet, this oral cavity disintegration tablet has good mouthfeel, without the need to water when taking, entrance gets final product rapid disintegrate, be applicable to the dysphagia patients such as old man, mental patient to take, be also suitable for medication under the condition not easily obtaining water source in journey, wartime etc. simultaneously.Simultaneously because this product indication is severe adult's depressive disorder, good mouthfeel and take the Compliance that mode can improve patient simply, rapidly.In addition, the invention also discloses a kind of preparation method of vilazodone oral cavity disintegration tablet, adopt the method for the invention to prepare vilazodone Orally disintegrating blade technolgy simple, cost is low, the oral cavity disintegration tablet disintegrate prepared is fast, and onset is rapid, decreases patient consumes's sense of discomfort.
Description
Technical field
The present invention relates to a kind of antidepressant mental medicine oral cavity disintegration tablet and preparation method thereof, relate to a kind of vilazodone oral cavity disintegration tablet and preparation method particularly, belong to medical art.
Background technology
Depression is also known as depressive disorder, low for main clinical characteristics with remarkable and lasting mental state, is the main Types of mood disorders.Clinical visible mental state is low unbecoming with its situation, and the downhearted of emotion can from depressed to extremely grieved, and depression of feeling oneself inferior is even pessimistic and worldweary, can have suicidal attempt or behavior; Even occur numb; Some cases have obvious anxiety and mobility intense; The psychotic symptoms such as hallucination, vain hope can be there is in severe patient.Even each outbreak continues at least 2 weeks more than, elder's several years, majority of cases has the tendency of recurrent exerbation, and each outbreak great majority can be alleviated, and part can have residual symptoms or transfer to chronic.The report display that World Health Organization (WHO) issues, the whole world has suffers from depressive illness more than 3.5 hundred million people, the drop of cure rate and sickness rate causes patients with depression number to present the situation increased year by year, vilazodone is the medicine of first indolyl amine novel therapeutic severe adult depression, has selective serotonin reuptake inhibitor and 5-HT1A acceptor portion agonist dual function.
On January 21st, 2011, FDA ratifies the listing of vilazodone (Vilazodone) micromolecule oral tablet medicine, and commodity are called Viibryd.Vilazodone is obtained joint development weighed by TrovisPharmaceuticalsLLC company, forest laboratory (ForestLaboratories), ClinicalData, PGxHealth, is mainly used in treatment severe adult depression.Domesticly at present there is no this kind list marketing.
The dosage form of domestic granted antidepressant mental medicine has tablet, dispersible tablet, capsule, granule, injection etc. at present.Intravenous administration is for extremely inconvenient patient, and compliance is poor; The oral formulations such as tablet, capsule, granule, dispersible tablet, must use water delivery service when patient takes, be not suitable for the patient that old people, mental patient etc. exist dysphagia and take.And most of patients with depression needs Long-term taking medicine, therefore develop a kind ofly do not need with water delivery service, easily swallow, the preparation that can take whenever and wherever possible is very important.
Vilazodone oral cavity disintegration tablet of the present invention does not need with water delivery service, and saliva can make its disintegrate or dissolving, masks bad smell and the bitterness of medicine, improves the Long-term taking medicine compliance of patient.Due to oral cavity disintegration tablet rapid disintegrate in mouth, except major part enters except gastrointestinal tract with swallowing act, also some direct oral cavity mucosal absorption, reduces liver first-pass effect.In addition, oral cavity disintegration tablet arrives before gastrointestinal tract disintegrate also can be dispersed into tiny granule rapidly at medicine, in the gastrointestinal tract dispersion evenly, diffusional area is large, avoid medicine too high at gastrointestinal tract local concentration, cause gastrointestinal local irritation, untoward reaction reduces.The stripping rapidly of another diffusional area ambassador medicine energy, absorbs fast, rapid-action.The oral cavity disintegration tablet of visible antidepressant antipsychotics is compared other dosage forms and is had more advantage.
The current domestic patent about vilazodone preparation aspect is less, fast release solid oral formulations or oral cavity disintegration tablet Patents temporarily blank.
Summary of the invention
The object of the invention is to the problem mentioned for background technology, a kind of oral cavity disintegration tablet dosage form improving the antidepressant drug of the defect of prior art and preparation method thereof is provided, particularly a kind of vilazodone oral cavity disintegration tablet and preparation method thereof.
The technical scheme of the present invention realizing above-mentioned purpose is as follows:
The invention provides a kind of vilazodone oral cavity disintegration tablet, described vilazodone oral cavity disintegration tablet consists of the following composition: the vilazodone of 1-10%, the disintegrating agent of 5-30%, the filler of 10-80%, the correctives of 1-10%, the lubricant of 0.05-2%.
Above-mentioned correctives be selected from acesulfame potassium, aspartame, fruit essence, sucralose, stevioside one or more.
Above-mentioned filler is selected from mannitol, xylitol, lactose, microcrystalline Cellulose, starch, pregelatinized Starch
One or more.
Above-mentioned disintegrating agent is selected from cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, lowly gets
For one or more in hyprolose.
Above-mentioned lubricant is the one or many in magnesium stearate, stearic acid, silicon dioxide, sodium stearyl fumarate
Kind.
Correctives of the present invention is selected from acesulfame potassium, aspartame, fruit essence, preferred acesulfame potassium, A Si
Ba Tian.
Described filler is selected from mannitol, xylitol, lactose and microcrystalline Cellulose, preferred mannitol, xylose
One or more in alcohol and microcrystalline Cellulose.
Described disintegrating agent is selected from cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone.
Described lubricant is selected from magnesium stearate and silicon dioxide.
Above-described vilazodone oral cavity disintegration tablet, is characterized in that it is grouped into by the one-tenth of following percentage by weight: the filler of the vilazodone of 4-10%, the disintegrating agent of 8-20%, 40-80%, the correctives of 1-5%, the lubricant of 0.05-2%.
Above-described vilazodone oral cavity disintegration tablet, is characterized in that, described vilazodone oral cavity disintegration tablet is prepared from by following steps:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and filler, disintegrating agent, correctives equivalent are progressively increased and mix;
(3) in said mixture, lubricant is added, tabletting after mixing, sheet heavy 100-150mg, hardness 30-40N.
Above-mentioned vilazodone oral cavity disintegration tablet may be used for treatment severe adult depressive disorder, belongs to antipsychotics preparation.
Detailed description of the invention
Further illustrate the present invention by embodiment below, understand a kind of vilazodone oral cavity disintegration tablet and preparation method thereof further, but the present invention is not limited.
Following embodiment and comparative example compacting tablet, if not otherwise indicated, all suppress with the tablet machine of same model, and all by Hardness Control in the scope of 30-40N.
the preparation of embodiment 1 vilazodone oral cavity disintegration tablet (10mg)
| Label composition | Part by weight (%) |
| Vilazodone | 10 |
| Mannitol | 40 |
| Microcrystalline Cellulose | 31.5 |
| Polyvinylpolypyrrolidone | 8 |
| Cross-linking sodium carboxymethyl cellulose | 8 |
| Acesulfame potassium | 1 |
| Silicon dioxide | 1 |
| Magnesium stearate | 0.5 |
Preparation technology:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and the mannitol of recipe quantity, microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, acesulfame potassium equivalent are progressively increased and mix;
(3) in said mixture, silicon dioxide and magnesium stearate is added, tabletting after mixing, sheet heavy 100mg, hardness 30-40N.
the preparation of embodiment 2 vilazodone oral cavity disintegration tablet (20mg)
| Label composition | Part by weight (%) |
| Vilazodone | 20 |
| Mannitol | 40 |
| Microcrystalline Cellulose | 30.5 |
| Polyvinylpolypyrrolidone | 8 |
| Cross-linking sodium carboxymethyl cellulose | 8 |
| Acesulfame potassium | 2 |
| Silicon dioxide | 1 |
| Magnesium stearate | 0.5 |
Preparation technology:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and the mannitol of recipe quantity, microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, acesulfame potassium equivalent are progressively increased and mix;
(3) in said mixture, silicon dioxide and magnesium stearate is added, tabletting after mixing, sheet heavy 110mg, hardness 30-40N.
the preparation of embodiment 3 vilazodone oral cavity disintegration tablet (10mg)
| Label composition | Part by weight (%) |
| Vilazodone | 10 |
| Wood dew alcohol | 42 |
| Microcrystalline Cellulose | 31 |
| Polyvinylpolypyrrolidone | 6 |
| Cross-linking sodium carboxymethyl cellulose | 8 |
| Acesulfame potassium | 1 |
| Aspartame | 0.5 |
| Silicon dioxide | 1 |
| Magnesium stearate | 0.5 |
Preparation technology:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and the wood of recipe quantity are revealed alcohol, microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, acesulfame potassium, aspartame equivalent progressively increases and mix;
(3) in said mixture, silicon dioxide and magnesium stearate is added, tabletting after mixing, sheet heavy 100mg, hardness 30-40N.
the preparation of embodiment 4 vilazodone oral cavity disintegration tablet (20mg)
| Label composition | Part by weight (%) |
| Vilazodone | 20 |
| Wood dew alcohol | 40 |
| Microcrystalline Cellulose | 34 |
| Polyvinylpolypyrrolidone | 6 |
| Cross-linking sodium carboxymethyl cellulose | 6 |
| Acesulfame potassium | 2 |
| Aspartame | 0.5 |
| Silicon dioxide | 1 |
| Magnesium stearate | 0.5 |
Preparation technology:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and the wood of recipe quantity are revealed alcohol, microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, acesulfame potassium, aspartame equivalent progressively increases and mix;
(3) in said mixture, silicon dioxide and magnesium stearate is added, tabletting after mixing, sheet heavy 110mg, hardness 30-40N.
the preparation of embodiment 5 vilazodone oral cavity disintegration tablet (10mg)
| Label composition | Part by weight (%) |
| Vilazodone | 10 |
| Mannitol | 50 |
| Microcrystalline Cellulose | 25 |
| Polyvinylpolypyrrolidone | 6 |
| Cross-linking sodium carboxymethyl cellulose | 6 |
| Acesulfame potassium | 1 |
| Aspartame | 0.5 |
| Silicon dioxide | 1 |
| Magnesium stearate | 0.5 |
Preparation technology:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and the mannitol of recipe quantity, microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, acesulfame potassium, aspartame equivalent are progressively increased and mix;
(3) in said mixture, silicon dioxide and magnesium stearate is added, tabletting after mixing, sheet heavy 100mg, hardness 30-40N.
the preparation of embodiment 6 vilazodone oral cavity disintegration tablet (20mg)
| Label composition | Part by weight (%) |
| Vilazodone | 20 |
| Mannitol | 50 |
| Microcrystalline Cellulose | 30 |
| Polyvinylpolypyrrolidone | 6 |
| Cross-linking sodium carboxymethyl cellulose | 6 |
| Acesulfame potassium | 1 |
| Aspartame | 0.5 |
| Silicon dioxide | 1 |
| Magnesium stearate | 0.5 |
Preparation technology:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and the mannitol of recipe quantity, microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, acesulfame potassium, aspartame equivalent are progressively increased and mix;
(3) in said mixture, silicon dioxide and magnesium stearate is added, tabletting after mixing, sheet heavy 115mg, hardness 30-40N.
test example 1: the disintegration of oral cavity disintegration tablet checks
Get 2ml water (37 DEG C) and be placed in 5ml test tube, add vilazodone oral cavity disintegration tablet, start timing, being shattered into independently fine particle, stopping to all collapsing, record disintegration time, the not dynamic test tube of disintegrating procedue, gets 6 at every turn and detects, get its meansigma methods.
test example 2: tablet friability inspection
Carry out according to method under " tablet friability inspection technique " item in Chinese Pharmacopoeia 2010 editions two annex XG, calculate less loss weight (%), and observe whether there are the abnormal conditions such as fracture, be full of cracks and/or pulverizing.
test example 3: Orally disintegrating test and mouthfeel inspection
Choose healthy volunteer 6, oral cavity disintegration tablet is placed on lingual surface and starts timing, to all collapsing stopping timing of scattering in the oral cavity, record disintegration time, and experience the sensation in slice, thin piece oral cavity after being placed in mouth to complete disintegrate.
Table 1 vilazodone oral cavity disintegration tablet result of the test
Know that the vilazodone oral cavity disintegration tablet disintegrate adopting prescription of the present invention and preparation method to prepare is rapid by upper table, slice, thin piece hardness is qualified, mouthfeel is good, without grittiness, and do not need special producing condition, there is production cost low, carry, store, transport and take feature easily, improve patient consumes's compliance, there is higher actual application value.
Claims (12)
1. a vilazodone oral cavity disintegration tablet, is characterized in that described vilazodone oral cavity disintegration tablet is by following one-tenth
Be grouped into: the vilazodone of 1-10%, the disintegrating agent of 5-30%, the filler of 10-80%, the correctives of 1-10%, the lubricant of 0.05-2%.
2. vilazodone oral cavity disintegration tablet according to claim 1, is characterized in that described correctives is for peace
Match honey, aspartame, fruit essence, sucralose, one or more in stevioside.
3. vilazodone oral cavity disintegration tablet according to claim 1, is characterized in that described filler is sweet
Dew alcohol, xylitol, lactose, microcrystalline Cellulose, starch, one or more in pregelatinized Starch.
4. vilazodone oral cavity disintegration tablet according to claim 1, is characterized in that described disintegrating agent is for handing over
Connection sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, one in low-substituted hydroxypropyl cellulose or
Multiple.
5. vilazodone oral cavity disintegration tablet according to claim 1, is characterized in that described lubricant is hard
One or more in fatty acid magnesium, stearic acid, silicon dioxide, sodium stearyl fumarate.
6. vilazodone oral cavity disintegration tablet according to claim 2, is characterized in that described correctives is selected from
Acesulfame potassium, aspartame, fruit essence, preferred acesulfame potassium, aspartame.
7. vilazodone oral cavity disintegration tablet according to claim 3, is characterized in that described filler is selected from
Mannitol, xylitol, lactose and microcrystalline Cellulose, in preferred mannitol, xylitol and microcrystalline Cellulose one
Kind or multiple.
8. vilazodone oral cavity disintegration tablet according to claim 4, is characterized in that described disintegrating agent is selected from
Cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone.
9. vilazodone oral cavity disintegration tablet according to claim 5, is characterized in that described lubricant is selected from
Magnesium stearate and silicon dioxide.
10. vilazodone oral cavity disintegration tablet according to claim 1, is characterized in that it is by following weight hundred
The one-tenth of proportion by subtraction is grouped into: the filler of the vilazodone of 4-10%, the disintegrating agent of 8-20%, 40-80%, the correctives of 1-5%, the lubricant of 0.05-2%.
11. vilazodone oral cavity disintegration tablets according to claim 1, is characterized in that, described vilazodone oral cavity disintegration tablet is prepared from by following steps:
(1) vilazodone raw material pulverizing is crossed 100 mesh sieves;
(2) raw material after pulverizing and filler, disintegrating agent, correctives equivalent are progressively increased and mix;
(3) in said mixture, lubricant is added, tabletting after mixing, sheet heavy 100-150mg, hardness 30-40N.
12. vilazodone oral cavity disintegration tablets according to claim 1 may be used for treatment severe adult depressive disorder, belong to antipsychotics preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510584625.1A CN105213334A (en) | 2015-09-15 | 2015-09-15 | A kind of vilazodone oral cavity disintegration tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510584625.1A CN105213334A (en) | 2015-09-15 | 2015-09-15 | A kind of vilazodone oral cavity disintegration tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105213334A true CN105213334A (en) | 2016-01-06 |
Family
ID=54982856
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510584625.1A Pending CN105213334A (en) | 2015-09-15 | 2015-09-15 | A kind of vilazodone oral cavity disintegration tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105213334A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106580895A (en) * | 2016-12-07 | 2017-04-26 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
| CN106667939A (en) * | 2017-02-14 | 2017-05-17 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride and preparation method thereof |
| CN110604723A (en) * | 2018-06-14 | 2019-12-24 | 北京万全德众医药生物技术有限公司 | Vilazodone hydrochloride orally disintegrating tablet and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103893180A (en) * | 2012-12-30 | 2014-07-02 | 北京科源创欣科技有限公司 | Pharmaceutical composition for treating insomnia |
-
2015
- 2015-09-15 CN CN201510584625.1A patent/CN105213334A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103893180A (en) * | 2012-12-30 | 2014-07-02 | 北京科源创欣科技有限公司 | Pharmaceutical composition for treating insomnia |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106580895A (en) * | 2016-12-07 | 2017-04-26 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
| CN106667939A (en) * | 2017-02-14 | 2017-05-17 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride and preparation method thereof |
| CN110604723A (en) * | 2018-06-14 | 2019-12-24 | 北京万全德众医药生物技术有限公司 | Vilazodone hydrochloride orally disintegrating tablet and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Sharma | Formulation development and evaluation of fast disintegrating tablets of salbutamol sulphate for respiratory disorders | |
| ES2393640T3 (en) | Orodisintegrable tablets | |
| CN103536568B (en) | A kind of oral cavity disintegration tablet containing Lurasidone and preparation method thereof | |
| TW201815384A (en) | Tablet comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)-benzaldehyde | |
| CN102740893B (en) | Dry-coated orally disintegrating tablet | |
| CN105228595B (en) | Deglutible N-acetylcystein tablet | |
| JPWO2011019043A1 (en) | Intraoral quick disintegrating tablet containing two or more kinds of particles | |
| Sharma et al. | Formulation development and evaluation of fast disintegrating tablets of salbutamol sulphate, cetirizine hydrochloride in combined pharmaceutical dosage form: a new era in novel drug delivery for pediatrics and geriatrics | |
| JP2014507475A (en) | Methods and compositions for treating depression using cyclobenzaprine | |
| Jha et al. | Formulation and evaluation of melt-in-mouth tablets of haloperidol | |
| CN107789328B (en) | Orally disintegrating tablet containing donepezil hydrochloride and preparation method thereof | |
| CN105213334A (en) | A kind of vilazodone oral cavity disintegration tablet and preparation method thereof | |
| Sharma et al. | Formulation development and evaluation of fast disintegrating tablet of cetirizine hydrochloride: a novel drug delivery for pediatrics and geriatrics | |
| JP7036856B2 (en) | Orally disintegrating tablet | |
| WO2023193745A1 (en) | Dextromethorphan-quinidine orally disintegrating tablet and use thereof | |
| Husain et al. | Development, optimization and characterization of hydrocolloid based mouth dissolving film of Telmisartan for the treatment of hypertension | |
| CN104224758A (en) | Levocetirizine hydrochloride oral instant film and preparation method thereof | |
| CN108261399A (en) | Olanzapine oral disnitegration tablet and preparation method thereof | |
| Rangole et al. | Formulation and in-vitro evaluation of rapidly disintegrating tablets using hydrochlorothiazide as a model drug | |
| CN109589314A (en) | Preparation method containing hydrobromic acid Vortioxetine oral disintegrating tablet | |
| CN116687870A (en) | Orally disintegrating tablet and preparation method thereof | |
| CN106038501A (en) | Escitalopram oxalate oral disintegrating tablet and preparation method thereof | |
| CN104622824A (en) | Aripiprazole orally disintegrating tablet and preparation method thereof | |
| AU2012238330B1 (en) | Fast Dissolving Solid Dosage Form | |
| Sahoo et al. | Designing of orodispersible tablet of diethyl carbamazine citrate for the treatment of filariasis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160106 |
|
| WD01 | Invention patent application deemed withdrawn after publication |