CN107802608A - A kind of atomoxetine tablet composition - Google Patents
A kind of atomoxetine tablet composition Download PDFInfo
- Publication number
- CN107802608A CN107802608A CN201711379236.0A CN201711379236A CN107802608A CN 107802608 A CN107802608 A CN 107802608A CN 201711379236 A CN201711379236 A CN 201711379236A CN 107802608 A CN107802608 A CN 107802608A
- Authority
- CN
- China
- Prior art keywords
- atomoxetine
- recipe quantity
- lactose
- calcium sulfate
- tablet composition
- 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.)
- Withdrawn
Links
Classifications
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K9/2009—Inorganic compounds
-
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of atomoxetine composition, belong to technical field of medicine.The technical scheme is that：A kind of atomoxetine tablet composition, in the composition of unit dose, contain the 30mg of atomoxetine 5, the 26mg of beta cyclodextrin 18, the 46mg of calcium sulfate 30, the 16mg of aerosil 8, the 50mg of lactose 30, the 12mg of low substituted hydroxy-propyl methylcellulose 6, the 5mg of sorbierite 2, the 1.5mg of magnesium stearate 0.8.Technical solution of the present invention provides a kind of atomoxetine tablet of the stabilization of taste masking.
Description
Technical field
The present invention relates to a kind of atomoxetine composition, belong to technical field of medicine.
Background technology
Attention deficit hyperactivity disorder（ADHD）, it is referred to as hyperactivity in China, common a kind of mental handicape childhood being.Table
Be now with age and developmental level be disproportionate absent minded and attention the time is of short duration, hyperactivity hyperkinesia and impulsion, be often accompanied by
Difficulty of learning, conduct disorder and maladjustment.Domestic external survey finds illness rate 3%~7%, and men and women's ratio is 4~9：1.Suffer from part
Still there is symptom after youngster's adult, hence it is evident that influence family life and sociability after patient's school work, physical and mental health and adult.
Atomoxetine（Atomoxetine）, chemical name：(R)-N- methyl -3- (2- methylphenoxies) amphetamine.For one
Kind is used to treat attention deficit-hyperactivity disorder（ADHD）Medicine, belong to non-nervous centralis stimulating drug.
Atomoxetine has strong bitter taste, and does not allow easy-clear for a long time in mouth.
Atomoxetine is known height bitter taste and high water soluble medicine.In addition, atomoxetine has for a long time
Bitter taste.Commercially available atomoxetine is capsule, to avoid it from being discharged in mouth.But some crowds are unwilling to take capsule, especially
It is children, it is believed that is difficult to swallow.
Chinese patent 201380080783.2 discloses the composition of the form of the aqueous solution of atomoxetine.Said composition
The strong bitter taste of atomoxetine can be significantly reduced.However, liquid preparation is inconvenient there is carrying, the bad control of dose
The defects of.
It is one of most widely used method for taste masked, especially in paediatrics system using sweetener and flavor enhancement
In the case of agent such as chewable tablets and liquid preparation.However, there is document report, this method is for height bitter taste and high water soluble medicine
Thing is not extremely successful.In addition, the easy moisture absorption of atomoxetine, tablet room temperature is deposited 1 year or so, and slice, thin piece has loose situation to send out
It is raw, and the rise of relevant material is obvious, influences its normal use.
Therefore it provides a kind of taste masking, steady quality atomoxetine tablet composition is one challenging
Work.
The content of the invention
It is an object of the invention to provide a kind of taste masking, steady quality atomoxetine tablet composition.
Technical scheme：
The technical scheme is that：A kind of atomoxetine tablet composition, in the composition of unit dose, containing atropic not
Western spit of fland 5-30mg, beta cyclodextrin 18-26mg, calcium sulfate 30-46mg, aerosil 8-16mg, lactose 30-50mg, low substitution
Hydroxypropyl methyl cellulose 6-12mg, sorbierite 2-5mg, magnesium stearate 0.8-1.5mg.
Currently preferred technical scheme, in the atomoxetine tablet composition of unit dose, contain atomoxetine
5-30mg, beta cyclodextrin 20-25mg, calcium sulfate 35-42mg, aerosil 10-15mg, lactose 34-48mg, low substitution hydroxyl
Propyl methocel 8-10mg, sorbierite 3-5mg, magnesium stearate 0.8-1.5mg.
Currently preferred technical scheme, in the atomoxetine tablet composition of unit dose, contain atomoxetine
10mg, beta cyclodextrin 22mg, calcium sulfate 40mg, aerosil 12mg, lactose 40mg, low substituted hydroxy-propyl methylcellulose
9mg, sorbierite 4mg, magnesium stearate 1.0mg.
The preparation method of atomoxetine tablet composition of the present invention, comprises the following steps：
The first step weighs recipe quantity beta cyclodextrin, adds 2.5 times of amounts（Quality multiple）Water dissolving, add the atropic Moses of recipe quantity
Spit of fland, pasty state is fully ground into, 35 DEG C of dryings, obtains inclusion compound；
Second step first step inclusion compound, add the calcium sulfate of half recipe quantity, the gas phase titanium dioxide of half recipe quantity
Silicon, the lactose of 1/3rd recipe quantities, the low substituted hydroxy-propyl methylcellulose of a quarter recipe quantity, it is well mixed, with 45%
Ethanol wet is pelletized, 35 DEG C of dryings, crosses 60 mesh sieves；
Particle obtained by 3rd step second step, add calcium sulfate, aerosil, lactose, the low-substituted hydroxypropyl of remaining recipe quantity
Ylmethyl cellulose, it is well mixed；The sorbierite of recipe quantity is added, is pelletized with 45% ethanol wet, 35 DEG C of dryings, crosses 60 mesh
Sieve；
Particle obtained by the step of 4th step the 3rd, add the magnesium stearate of recipe quantity, tabletting.
Beneficial effect：
In technical solution of the present invention, the use of the inclusion technique of beta cyclodextrin, and the seasoning of sorbierite, effectively mask atropic
The addition of the bitter taste in Moses spit of fland, calcium sulfate and aerosil, improve the stability of tablet.
Because of the atomoxetine of below 10mg specifications, due to atomoxetine, viscosity is big in itself, and uniformity of dosage units is not easily-controllable
System, preparation method of the present invention, using secondary granulation technique, the uniformity of dosage units of product is effectively improved, and for tablet
Stabilization also have certain positive role.Technical solution of the present invention provides a kind of atomoxetine tablet of the stabilization of taste masking.
Embodiment 1, atomoxetine 5g, beta cyclodextrin 18g, calcium sulfate 30g, aerosil 16g, lactose 30g are low
Substitute hydroxypropyl methyl cellulose 6g, sorbierite 2g, magnesium stearate 0.8g, preparation method prepares 1000 as described in technical scheme
Piece.
Embodiment 2, atomoxetine 30g, beta cyclodextrin 26g, calcium sulfate 46g, aerosil 8g, lactose 50g are low
Substitute hydroxypropyl methyl cellulose 12g, sorbierite 5g, magnesium stearate 1.5g, preparation method prepares 1000 as described in technical scheme
Piece.
Embodiment 3, atomoxetine 10g, beta cyclodextrin 22g, calcium sulfate 40g, aerosil 12g, lactose 40g are low
Substitute hydroxypropyl methyl cellulose 9g, sorbierite 4g, magnesium stearate 1.0g, preparation method prepares 1000 as described in technical scheme
Piece.
Reference examples 1, the prescription of embodiment 3 cut calcium sulfate, and corresponding weight is supplemented by lactose.It is specific as follows：
Prescription：Atomoxetine 10g, beta cyclodextrin 22g, aerosil 12g, lactose 80g, low-substituted hydroxypropyl ylmethyl are fine
Plain 9g, sorbierite 4g, magnesium stearate 1.0g are tieed up, 1000 are prepared by following preparation methods.
The first step weighs recipe quantity beta cyclodextrin, adds 2.5 times of amounts（Quality multiple）Water dissolving, add the atropic of recipe quantity
Moses spit of fland, pasty state is fully ground into, 35 DEG C of dryings, obtains inclusion compound；
Second step first step inclusion compound, add the aerosil of half recipe quantity, the breast of 1/3rd recipe quantities
Sugar, the low substituted hydroxy-propyl methylcellulose of a quarter recipe quantity, it is well mixed, is pelletized with 45% ethanol wet, 35 DEG C dry
It is dry, cross 60 mesh sieves；
Particle obtained by 3rd step second step, it is fine to add remaining recipe quantity aerosil, lactose, low-substituted hydroxypropyl ylmethyl
Dimension element, is well mixed；The sorbierite of recipe quantity is added, is pelletized with 45% ethanol wet, 35 DEG C of dryings, crosses 60 mesh sieves；
Particle obtained by the step of 4th step the 3rd, add the magnesium stearate of recipe quantity, tabletting.
Reference examples 2, the prescription of embodiment 3 cut calcium sulfate and aerosil, and corresponding weight is supplemented by lactose.Specifically such as
Under：
Prescription：Atomoxetine 10g, beta cyclodextrin 22g, lactose 92g, low substituted hydroxy-propyl methylcellulose 9g, sorbierite 4g,
Magnesium stearate 1.0g, 1000 are prepared by following preparation methods.
The first step weighs recipe quantity beta cyclodextrin, adds 2.5 times of amounts（Quality multiple）Water dissolving, add the atropic of recipe quantity
Moses spit of fland, pasty state is fully ground into, 35 DEG C of dryings, obtains inclusion compound；
Second step first step inclusion compound, add the lactose of 1/3rd recipe quantities, the low substituted hydroxy-propyl of a quarter recipe quantity
Methylcellulose, it is well mixed, is pelletized with 45% ethanol wet, 35 DEG C of dryings, crosses 60 mesh sieves；
Particle obtained by 3rd step second step, it is fine to add remaining recipe quantity aerosil, lactose, low-substituted hydroxypropyl ylmethyl
Dimension element, is well mixed；The sorbierite of recipe quantity is added, is pelletized with 45% ethanol wet, 35 DEG C of dryings, crosses 60 mesh sieves；
Particle obtained by the step of 4th step the 3rd, add the magnesium stearate of recipe quantity, tabletting.
The prescription of reference examples 3, embodiment 3, one-step method granulation are specific as follows：
Prescription：Atomoxetine 10g, beta cyclodextrin 22g, calcium sulfate 40g, aerosil 12g, lactose 40g, low substitution hydroxyl
Propyl methocel 9g, sorbierite 4g, magnesium stearate 1.0g, 1000 are prepared by following preparation methods.
The first step weighs recipe quantity beta cyclodextrin, adds 2.5 times of amounts（Quality multiple）Water dissolving, add the atropic of recipe quantity
Moses spit of fland, pasty state is fully ground into, 35 DEG C of dryings, obtains inclusion compound；
Second step first step inclusion compound, add calcium sulfate, aerosil, lactose, the low-substituted hydroxypropyl ylmethyl of recipe quantity
Cellulose, sorbierite, it is well mixed, is pelletized with 45% ethanol wet, 35 DEG C of dryings, crosses 60 mesh sieves；
Particle obtained by 3rd step second step, add the magnesium stearate of recipe quantity, tabletting.
Test example, respectively Example 1-3 and reference examples 1-3 each 100 of product, it is aluminum-plastic packaged respectively, it is placed in constant temperature
In constant humidity cabinet, 30 DEG C, relative humidity 65% is deposited 12 months, and the 12nd the end of month took out, and observes outward appearance, high effective liquid chromatography for measuring
Relevant content of material, data record and table 1.
Table 1
The data of table 1 illustrate that product of the embodiment of the present invention is stable during storage, and tablet appearance keeps fine and relevant
Material does not change substantially.Illustrate that technical solution of the present invention serves unexpected effect in terms of stability.
Test example 2 finds the people of health worker 60 of office 20-36 year, and it is each to take 1-3 products of the embodiment of the present invention respectively
1,50ml warm water takes, and record takes impression, does not all foretaste person and reflects, without bitter taste, there is light sweet taste.Illustrate this hair
Bright technical scheme has reached taste masking purpose.
Claims (4)
1. a kind of atomoxetine tablet composition, it is characterised in that in the composition of unit dose, contain atomoxetine 5-
30mg, beta cyclodextrin 18-26mg, calcium sulfate 30-46mg, aerosil 8-16mg, lactose 30-50mg, low substituted hydroxy-propyl
Methylcellulose 6-12mg, sorbierite 2-5mg, magnesium stearate 0.8-1.5mg.
2. according to atomoxetine tablet composition described in claim 1, it is characterised in that the tablet composition of unit dose
In, contain atomoxetine 5-30mg, beta cyclodextrin 20-25mg, calcium sulfate 35-42mg, aerosil 10-15mg, lactose
34-48mg, low substituted hydroxy-propyl methylcellulose 8-10mg, sorbierite 3-5mg, magnesium stearate 0.8-1.5mg.
3. according to atomoxetine tablet composition described in claim 1, it is characterised in that the tablet composition of unit dose
In, contain atomoxetine 10mg, beta cyclodextrin 22mg, calcium sulfate 40mg, aerosil 12mg, lactose 40mg, low substitution
Hydroxypropyl methyl cellulose 9mg, sorbierite 4mg, magnesium stearate 1.0mg.
4. the preparation method of atomoxetine tablet composition, comprises the following steps described in claim 1：
The first step weighs recipe quantity beta cyclodextrin, adds 2.5 times of amounts（Quality multiple）Water dissolving, add the atropic Moses of recipe quantity
Spit of fland, pasty state is fully ground into, 35 DEG C of dryings, obtains inclusion compound；
Second step first step inclusion compound, add the calcium sulfate of half recipe quantity, the gas phase titanium dioxide of half recipe quantity
Silicon, the lactose of 1/3rd recipe quantities, the low substituted hydroxy-propyl methylcellulose of a quarter recipe quantity, it is well mixed, with 45%
Ethanol wet is pelletized, 35 DEG C of dryings, crosses 60 mesh sieves；
Particle obtained by 3rd step second step, add calcium sulfate, aerosil, lactose, the low-substituted hydroxypropyl of remaining recipe quantity
Ylmethyl cellulose, it is well mixed；The sorbierite of recipe quantity is added, is pelletized with 45% ethanol wet, 35 DEG C of dryings, crosses 60 mesh
Sieve；
Particle obtained by the step of 4th step the 3rd, add the magnesium stearate of recipe quantity, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711379236.0A CN107802608A (en) | 2017-12-20 | 2017-12-20 | A kind of atomoxetine tablet composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711379236.0A CN107802608A (en) | 2017-12-20 | 2017-12-20 | A kind of atomoxetine tablet composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107802608A true CN107802608A (en) | 2018-03-16 |
Family
ID=61590006
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711379236.0A Withdrawn CN107802608A (en) | 2017-12-20 | 2017-12-20 | A kind of atomoxetine tablet composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107802608A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109381440A (en) * | 2018-11-15 | 2019-02-26 | 威海贯标信息科技有限公司 | A kind of Ai Le replaces nylon 6 combination |
| CN112438949A (en) * | 2019-09-05 | 2021-03-05 | 北京兴源联合医药科技有限公司 | Tomoxxetine hydrochloride oral liquid containing calcium supplement and preparation method thereof |
-
2017
- 2017-12-20 CN CN201711379236.0A patent/CN107802608A/en not_active Withdrawn
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109381440A (en) * | 2018-11-15 | 2019-02-26 | 威海贯标信息科技有限公司 | A kind of Ai Le replaces nylon 6 combination |
| CN112438949A (en) * | 2019-09-05 | 2021-03-05 | 北京兴源联合医药科技有限公司 | Tomoxxetine hydrochloride oral liquid containing calcium supplement and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR100360130B1 (en) | Fluoxetine pharmaceutical preparations | |
| JP5222841B2 (en) | Oseltamivir phosphate granule and preparation method thereof | |
| CN101352449B (en) | Vitamin orally disintegrating tablet and preparation method thereof | |
| JP4555407B2 (en) | Kampo medicines and herbal medicines | |
| US20190269614A1 (en) | Chewable tablet containing vitamin c sodium and preparation method thereof | |
| Pawar et al. | Isolation, characterization and investigation of Plantago ovata husk polysaccharide as superdisintegrant | |
| CN113413388B (en) | Sildenafil citrate-containing pharmaceutical composition, preparation method and application thereof | |
| CN107802608A (en) | A kind of atomoxetine tablet composition | |
| CN105193803B (en) | A kind of Ilepcimide sustained release preparation and preparation method thereof | |
| CN102961371A (en) | Ibuprofen arginine granule and preparation method thereof | |
| CN102100902B (en) | Counterflow effervescent tablets | |
| CN108014085A (en) | A kind of preparation method and applications of sabril solid composite | |
| CN111617042A (en) | Composite calcium carbonate vitamin D3Water-free swallow granule and preparation method thereof | |
| TW202023594A (en) | Composition for calming nerves and benefiting sleep as well as preparation method and application thereof | |
| CN107854671A (en) | A Na series anaesthetic intragastric floating sustained-release preparations and preparation method thereof | |
| CN106063788B (en) | Application of phillyrin, phillyrin derivatives, and phillyrin-phillygenin composition in preparation of drugs for relieving or/and treating emesis | |
| CN109331093B (en) | Plant composition and application thereof | |
| JP4766941B2 (en) | Composition with reduced unpleasant odor or taste of cysteines | |
| AU2017288035A1 (en) | Pharmaceutical composition containing combination of memantine and melatonin | |
| RU2573999C2 (en) | Tabletted dietary supplement containing iodine and selenium | |
| JP4634589B2 (en) | Food or pharmaceutical ready-to-use agent | |
| CN107375225B (en) | Level release formulation of a kind of succinic acid furan Luo Qu and preparation method thereof | |
| CN104174023B (en) | One kind makes the stability-enhanced pharmaceutical composition of ambroxol hydrochloride | |
| KR101458670B1 (en) | Pharmaceutical composition comprising branched chain amino acids as active ingredients and the preparation method thereof | |
| CN103505474A (en) | Preparation of donkey-hide gelatin effervescent tablet |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20180316 |