CN106860410A - A kind of escitalopram oxalate oral disintegrating tablet and preparation method thereof - Google Patents
A kind of escitalopram oxalate oral disintegrating tablet and preparation method thereof Download PDFInfo
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- CN106860410A CN106860410A CN201710159207.7A CN201710159207A CN106860410A CN 106860410 A CN106860410 A CN 106860410A CN 201710159207 A CN201710159207 A CN 201710159207A CN 106860410 A CN106860410 A CN 106860410A
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- China
- Prior art keywords
- escitalopram oxalate
- disintegrating tablet
- oral disintegrating
- filler
- disintegrant
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
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- Animal Behavior & Ethology (AREA)
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Abstract
The invention discloses a kind of preparation method of escitalopram oxalate oral disintegrating tablet, belong to medicine new technical field.The piece is with escitalopram oxalate as main component, using dry granulation technology, comprising filler, disintegrant, flavouring, lubricant.This invention simplifies technique, improve the mobility and compact property in product preparation process, it is ensured that the good outward appearance of product, disintegration and dissolution.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, and in particular to a kind of preparation method of escitalopram oxalate oral disintegrating tablet.Should
Piece is clinically used to treat depression.
Background technology
FOREST LABS companies of the U.S. early have been developed that escitalopram oxalate piece, by Denmark H. LundbeckA/S
Production listing, trade name Lexapro（Lexapro）, formulation is conventional tablet, and specification is 10mg, for treat depressive disorder,
Have or without the panic disorder of square disease, existing original domestic at present grinds listing.In addition, copying also has occurred in the market
Medicine, formulation is tablet, and at home and abroad market oral disintegrating tablet formulation does not occur.
The chemical name of escitalopram oxalate is S（+）-1-（3- dimethylamine propyls）-1-（4- difluorophenyls）-1,3-
Dihydroisobenzofuran -5- eyeball oxalates, chemical mechanical formula is
。
Escitalopram is the list-S- enantiomers of two hydrogenated phthalein derivative Citaloprams.Escitalopram resists
The mechanism of depressive illness effect may with suppress central nervous system neurons to the reuptake of 5-HT, so as to strengthen maincenter 5- hydroxyl colors
The function of amine energy nerve is relevant.Clinically hinder for treatment depressive disorder, panic disorder, social anxiety disorder, generalized anxiety disorder
Hindering has remarkable result.
According to WHO Report, current depression is global the fourth-largest Disease Spectrum, is also to cause patient's function
Disabled one of the main reasons, about 1/7 people can be subjected to depression puzzlement in certain stage of life.Expect 2020
Year, depression is only second to the second largest disease of cardiovascular disease by turning into.Prevention and treatment for depression are very urgent, but greatly
The gloomy pain of some patientss mood, it is difficult to concentrate one's energy and right mind, has resentment to medication, causes aggravation.Mouthful
Disintegrating tablet can improve the compliance of patient and energy quick acting for conventional tablet, it is ensured that timely symptom management.
Chinese patent CN106038501A discloses one kind and uses half dry type on escitalopram oxalate oral disintegrating tablet
The invention of grain tablet forming technique, advantage is to be disintegrated that rapid, mouthfeel is excellent, and disintegrant selected by two kinds of techniques is different, flavouring auxiliary material
Nuance, dry granulation process operating process is more convenient easily-controllable, and the finished product content uniformity is more preferable.
The content of the invention
The invention provides a kind of preparation method of escitalopram oxalate oral disintegrating tablet, its feature is：
（1）Simple and easy to apply using dry granulation process, process facilitates easily-controllable, meets existing preparation technique, convenient big production；
（2）The compliance of patient's medication is improved, and it is rapid-action, facilitate depressive patient to take.
The inventive technique scheme for meeting These characteristics is as follows：The escitalopram oxalate of 5-15% is bulk drug, is equipped with
The filler of 20-90%, the disintegrant of 5-20%, the flavouring of 0.5-5%, the lubricant of 0.05-5%.
Above-mentioned filler is one or more in mannitol, lactose, microcrystalline cellulose, starch, particularly preferred sweet dew
Alcohol and microcrystalline cellulose.
Above-mentioned disintegrant is Ac-Di-Sol, PVPP, low-substituted hydroxypropyl cellulose, carboxymethyl shallow lake
One or more in powder sodium, particularly preferred low-substituted hydroxypropyl cellulose.
Above-mentioned flavouring is one or more in menthol, acesulfame potassium, fruit essence, Sucralose, Steviosin, special
Not preferred menthol, Steviosin, green apple essence.
Above-mentioned lubricant is one or more in silica, talcum powder, magnesium stearate, stearic acid, particularly preferably
Silica, magnesium stearate.
The characteristics of above-described escitalopram oxalate oral disintegrating tablet is：The escitalopram oxalate of 5-15% is
Bulk drug, is equipped with filler, the disintegrant of 5-20%, the flavouring of 0.5-5%, the lubricant of 0.05-5% of 20-90%, using dry
Method granulation technique.Specific preparation process is as follows：
（1）Escitalopram oxalate is crossed into 40 mesh sieves, it is standby；Additional filler and disintegrant are separately dried to moisture and are less than
3%, it is standby；The broken mesh sieve of mistake 60 of levigation is made blend to additional filler altogether with flavouring, standby；
（2）After by escitalopram oxalate and silica premix, by mixed powder and interior plus filler, interior mix with disintegrant
Adding magnesium stearate to mix after even must mix powder 1；
（3）Mixed powder 1 is pelletized with dry granulating machine, with 30 mesh sieve whole grains, it is ensured that the grain amount of 30 mesh sieves can be passed through>80%；
（4）Blend, additional disintegrant are added in particle and mix lubricant is uniform must mix powder 2；
（5）By the φ flat stampings of 6mm of mixed powder 2, hardness 20-30N.
Specific embodiment：
The present invention is further illustrated with embodiment below, a kind of escitalopram oxalate oral disintegrating tablet and its system is further appreciated that
Preparation Method, but the present invention is not limited except as.
Following embodiment and the tablet of comparative example's compacting, if not otherwise indicated, with the tablet press machine of same model
Suppressed.
Embodiment 1
Preparation process：（1）Escitalopram oxalate was crushed into 40 mesh sieves；Mannitol crushed 100 mesh sieves, standby；
（2）By escitalopram oxalate, microcrystalline cellulose PH101, mannitol and low-substituted hydroxypropyl cellulose, silica
It is well mixed,（3）With the flat stampings of ф 6, piece weight 100mg, hardness 20-30N.
Embodiment 2
Preparation process：（1）Escitalopram oxalate was crushed into 40 mesh sieves；Mannitol crushed 100 mesh sieves, standby；
（2）Additional low-substituted hydroxypropyl cellulose is separately dried to moisture less than 3%, standby.
（3）By mannitol, microcrystalline cellulose, the mode of pelletizing is made particle to interior plus low-substituted hydroxypropyl cellulose in a wet process, will
Escitalopram oxalate and particle are mixed, and add additional low-substituted hydroxypropyl cellulose, appropriate green apple essence, Steviosin, thin
Lotus brain, heavy silica, magnesium stearate are mixed；With the flat stampings of ф 6, piece weight 100mg, hardness 30-40N；
（4）With the flat stampings of ф 6, piece weight 100mg, hardness 20-30N.
Embodiment 3：
Preparation process：（1）Escitalopram oxalate is crossed into 40 mesh sieves, it is standby；Additional microcrystalline cellulose PH101 and low substitution
Hydroxypropylcellulose is separately dried to moisture less than 3%, standby；It is additional microcrystalline cellulose PH101 and green apple powdered flavor, sweet
The broken mesh sieve of mistake 60 of levigation is made blend altogether for chrysanthemum element, menthol, standby；
（2）After by escitalopram oxalate and silica premix, by mixed powder and interior plus microcrystalline cellulose PH101, it is interior plus
Adding magnesium stearate to mix after low-substituted hydroxypropyl cellulose, mannitol are well mixed must mix powder 1；
（3）Mixed powder 1 is pelletized with dry granulating machine, with 30 mesh sieve whole grains, it is ensured that the grain amount of 30 mesh sieves can be passed through>80%；
（4）Adding blend, additional low-substituted hydroxypropyl cellulose and magnesium stearate to be well mixed in particle must mix powder 2；
（5）By the φ flat stampings of 6mm of mixed powder 2, hardness 20-30N.
2nd, quality evaluating method
1st, compressibility inspection：The mobility of particle is observed before compressing tablet, tableting processes are suppressed with the tablet press machine of same model,
By hardness control in the range of 20-40N.Emphasis checks hardness, and has seen whether fragmentation, softens and/or glued puckery punching etc. and be abnormal
Situation.
2nd, disintegration time and mouthfeel inspection：Mouth tastes sample, and record slice, thin piece was put into mouth to the time of perfectly sound disintegration；Meanwhile,
Sensation after experiencing slice, thin piece from being placed in mouth to being disintegrated completely in oral cavity, it is such as sweet/bitter, whether there is grittiness etc..
3rd, stripping curve detection
Dissolution detection is carried out according to the escitalopram oxalate piece elution test method that FDA is announced, condition is as follows：
Paddle method, 0.1MHCL media, 37 DEG C, 50r/min, 900ml medium take 10ml and mend 10ml.Sample time：5min,10min,
15min,30min。
If dissolution rate is more than 85% during 15min, as Fast Stripping, meet the requirements.
Three, testing results
As seen from the above table, the method for the present invention improves the mobility and compact property in product preparation process, it is ensured that product
Good outward appearance, disintegration and dissolution and process is simple and easy to apply.
Claims (7)
1. a kind of preparation method of escitalopram oxalate oral disintegrating tablet, it is characterised in that dry granulation technology is used, with weight
The escitalopram oxalate of the 5-15% of percentages is bulk drug, be equipped with the filler of 20-90%, the disintegrant of 5-20%,
The flavouring of 0.5-5%, the lubricant of 0.05-5%.
2. the oral disintegrating tablet of escitalopram oxalate according to claim 1, it is characterised in that described filler is sweet
Reveal one or more in alcohol, lactose, microcrystalline cellulose, starch, particularly preferred mannitol and microcrystalline cellulose.
3. the oral disintegrating tablet of escitalopram oxalate according to claim 1, it is characterised in that described disintegrant is to hand over
One or more in connection sodium carboxymethylcellulose, PVPP, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch, especially
It is preferred that low-substituted hydroxypropyl cellulose.
4. the oral disintegrating tablet of escitalopram oxalate according to claim 1, it is characterised in that described flavouring is thin
One or more in lotus brain, acesulfame potassium, fruit essence, Sucralose, Steviosin, particularly preferred menthol, Steviosin, blue or green apple
One or more in fruity essence.
5. the oral disintegrating tablet of escitalopram oxalate according to claim 1, it is characterised in that described lubricant is two
One or more in silica, talcum powder, magnesium stearate, stearic acid, particularly preferred silica, one kind of magnesium stearate or
It is various.
6. the oral disintegrating tablet of escitalopram oxalate according to claim 1, it is characterised in that it is by following weight hundred
Point ratio into being grouped into：The escitalopram oxalate of 5-15% is bulk drug, is equipped with the disintegration of the filler, 5-20% of 20-90%
Agent, the flavouring of 0.5-5%, the lubricant of 0.05-5%.
7. the oral disintegrating tablet of escitalopram oxalate according to claim 1, it is characterised in that the preparation is by following step
Suddenly it is prepared from：
（1）Escitalopram oxalate is crossed into 40 mesh sieves, it is standby；Additional filler and disintegrant are separately dried to moisture and are less than
3%, it is standby；The broken mesh sieve of mistake 60 of levigation is made blend to additional filler altogether with flavouring, standby；
（2）After by escitalopram oxalate and silica premix, by mixed powder and interior plus filler, interior mix with disintegrant
Adding magnesium stearate to mix after even must mix powder 1；
（3）Mixed powder 1 is pelletized with dry granulating machine, with 30 mesh sieve whole grains, it is ensured that the grain amount of 30 mesh sieves can be passed through>80%；
（4）Blend, additional disintegrant are added in particle and mix lubricant is uniform must mix powder 2；
（5）By the φ flat stampings of 6mm of mixed powder 2, hardness 20-30N.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710159207.7A CN106860410A (en) | 2017-03-17 | 2017-03-17 | A kind of escitalopram oxalate oral disintegrating tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710159207.7A CN106860410A (en) | 2017-03-17 | 2017-03-17 | A kind of escitalopram oxalate oral disintegrating tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN106860410A true CN106860410A (en) | 2017-06-20 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710159207.7A Pending CN106860410A (en) | 2017-03-17 | 2017-03-17 | A kind of escitalopram oxalate oral disintegrating tablet and preparation method thereof |
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| Country | Link |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110731946A (en) * | 2018-07-18 | 2020-01-31 | 北京万全德众医药生物技术有限公司 | Escitalopram oxalate orally disintegrating tablet and preparation method thereof |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050196453A1 (en) * | 2004-03-05 | 2005-09-08 | H. Lundbeck A/S | Crystalline composition containing escitalopram |
| WO2008104880A2 (en) * | 2007-03-01 | 2008-09-04 | Aurobindo Pharma Limited | Stable solid dosage forms of an antidepressant |
| WO2009150665A1 (en) * | 2008-06-09 | 2009-12-17 | Lupin Limited | Orally disintegrating pharmaceutical compositions of escitalopram and salts thereof |
| CN103565773A (en) * | 2012-08-07 | 2014-02-12 | 广东东阳光药业有限公司 | Pharmaceutical composition of prasugrel hydrochloride |
| CN103565788A (en) * | 2013-09-30 | 2014-02-12 | 北京德众万全药物技术开发有限公司 | Pharmaceutical composition for treating depression and preparation method thereof |
| CN106038501A (en) * | 2016-06-30 | 2016-10-26 | 北京万全德众医药生物技术有限公司 | Escitalopram oxalate oral disintegrating tablet and preparation method thereof |
-
2017
- 2017-03-17 CN CN201710159207.7A patent/CN106860410A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050196453A1 (en) * | 2004-03-05 | 2005-09-08 | H. Lundbeck A/S | Crystalline composition containing escitalopram |
| WO2008104880A2 (en) * | 2007-03-01 | 2008-09-04 | Aurobindo Pharma Limited | Stable solid dosage forms of an antidepressant |
| WO2009150665A1 (en) * | 2008-06-09 | 2009-12-17 | Lupin Limited | Orally disintegrating pharmaceutical compositions of escitalopram and salts thereof |
| CN103565773A (en) * | 2012-08-07 | 2014-02-12 | 广东东阳光药业有限公司 | Pharmaceutical composition of prasugrel hydrochloride |
| CN103565788A (en) * | 2013-09-30 | 2014-02-12 | 北京德众万全药物技术开发有限公司 | Pharmaceutical composition for treating depression and preparation method thereof |
| CN106038501A (en) * | 2016-06-30 | 2016-10-26 | 北京万全德众医药生物技术有限公司 | Escitalopram oxalate oral disintegrating tablet and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 王沛主编: "《制药原理与设备》", 31 March 2014, 上海科学技术出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110731946A (en) * | 2018-07-18 | 2020-01-31 | 北京万全德众医药生物技术有限公司 | Escitalopram oxalate orally disintegrating tablet and preparation method thereof |
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