CN107441052A - A kind of tablet containing escitalopram oxalate and preparation method thereof - Google Patents
A kind of tablet containing escitalopram oxalate and preparation method thereof Download PDFInfo
- Publication number
- CN107441052A CN107441052A CN201710473553.2A CN201710473553A CN107441052A CN 107441052 A CN107441052 A CN 107441052A CN 201710473553 A CN201710473553 A CN 201710473553A CN 107441052 A CN107441052 A CN 107441052A
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- CN
- China
- Prior art keywords
- escitalopram oxalate
- magnesium stearate
- tablet
- preparation
- less
- 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.)
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Classifications
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- 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
-
- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material 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)
- Medicinal Preparation (AREA)
Abstract
The invention belongs to technical field of medicine, more particularly to a kind of escitalopram oxalate tablet and ensure the preparation method of its steady quality, it is not less than 300um escitalopram oxalate raw material using median particle diameter, auxiliary material includes magnesium stearate and other components, and the wherein percentage by weight of magnesium stearate in tablets is less than 0.1%.The problem of it is poor that the preparation method of the present invention efficiently solves material flow, easy sticking, and material mixing is uneven, solve the problems, such as magnesium stearate and active component poor compatibility and cause relevant material increase.This method is simple to operate, is easy to industrialization, and obtained tablet content is uniform, and quality is stablized before the deadline.
Description
Technical field
The invention belongs to pharmaceutical technology field, is specifically related to a kind of escitalopram oxalate tablet, and ensure it
The preparation method that quality is stablized before the deadline.
Background technology
Escitalopram oxalate piece（escitalopram oxalate）, researched and developed by Denmark's Lundbeck, 2002 by FDA batches
Quasi- listing, is ratified, is a kind of oral serotonin reuptake inhibitor in Discussion on Chinese Listed for 2005 by CFDA；Its structural formula is such as
Under：
Original grind Lundbeck China patent CN02815031, disclose it is a kind of prepare median particle diameter be 40-200um oxalic acid Chinese mugwort department
The method of Citalopram raw material, and direct powder compression or capsule filling are carried out using this raw material, but the crystal formation of this raw material needs to use
It is prepared by special process；
WO03/011278A1 patents are mentioned, when using direct tablet compressing technique, if raw material particle size and auxiliary material difference are excessive, and meeting
Raw material is caused to be not easy uniformly with auxiliary material when mixing, because machine vibration is also possible to cause particle to be layered in tableting processes,
Especially for this product, when piece weight is 64mg or so, such a phenomenon can be more obvious, and it is excessive to also result in tablet weight variation sometimes
It is not inconsistent standardization requirement；
WO2006123243A2 patents are pointed out, directly use 2-20um escitalopram oxalate raw material tabletting, flow of powder
Property is too poor, it is necessary to which after a dry granulation, material can just have preferable mobility, could also be used for commercial process
In；
CN 104523638 discloses a kind of wet granulation technology, and for preparing escitalopram oxalate piece, it is straight to mention powder
When connecing tabletting, because raw material electrostatic is big, easy sticking, the present inventor also confirms that such a phenomenon in practical operation, once causes
Production can not be normally carried out；
Therefore, it is necessary to develop a kind of simple to operate, it is easy to industrialization, the guaranteed preparation method of quality；The present inventor is through excessive
Experimental study is measured, achieves wonderful result, above mentioned problem is properly settled.
The content of the invention
The present inventor has surprisingly found that, using preparation method of the present invention, can solve content uniformity, glue by experiment
Problem is rushed, and product quality level can be effectively improved, technical characteristic of the invention is：
A kind of tablet containing escitalopram oxalate of the present invention, it is characterised in that：Described oxalic acid Escitalopram
Pulan tablet includes escitalopram oxalate and magnesium stearate, and the percentage by weight of magnesium stearate in tablets is less than 0.1%；
The median particle diameter of described escitalopram oxalate raw material is not less than 300 μm.
A kind of method of escitalopram oxalate tablet described in described preparation claim 1, it is characterised in that：Its
Step includes：By escitalopram oxalate（Median particle diameter is not less than 300um）, microcrystalline cellulose, cross-linked carboxymethyl cellulose
Sodium, colloidal silica, talcum powder are well mixed, magnesium stearate is sprayed onto punch head surface, with rotation in efficient mixer-granulator
Press tabletting.
Preparation method of the present invention is more than 300um raw material using median particle diameter, and the raw material can be prepared by commonsense method, into
This is low, and it is uniform to solve the problems, such as that poor fluidity, mixing are not easy；Prescription mesoxalic acid escitalopram weight is than little
In 35%；Magnesium stearate is that tableting die surface is sprayed in a manner of atomization in the present invention so that the institute of magnesium stearate in tablets
The percentage amounts accounted for are less than 0.1%, and use conventional method, and the amount of magnesium stearate is less than 0.5%, easily causes sticking, weight difference
The problems such as different big.Obtained escitalopram oxalate tablet content is uniform, and quality is stablized before the deadline.
Embodiment：
In order to be best understood from the present invention, technical scheme, but the present invention are described in detail underneath with specific embodiment
Specific implementation is clearly not limited to this two：
Embodiment 1：
| Sequence number | Title | Prescription（g) |
| 1 | Escitalopram oxalate | 64g |
| 2 | Microcrystalline cellulose | 508g |
| 3 | Ac-Di-Sol | 35g |
| 4 | Colloidal silica | 10g |
| 5 | Talcum powder | 20g |
| 6 | Magnesium stearate | 0.6g |
By escitalopram oxalate（Median particle diameter is not less than 300 μm）, microcrystalline cellulose, Ac-Di-Sol, glue
State silica, talcum powder are well mixed in efficient mixer-granulator, and magnesium stearate is ejected into punch head surface, are pressed with rotation
Machine tabletting.
Embodiment 2：
| Sequence number | Title | Prescription（g) |
| 1 | Escitalopram oxalate | 64g |
| 2 | Microcrystalline cellulose | 511g |
| 3 | Ac-Di-Sol | 35g |
| 4 | Colloidal silica | 10g |
| 5 | Talcum powder | 20g |
| 6 | Magnesium stearate | 0.3g |
By escitalopram oxalate（Median particle diameter is not less than 300 μm）, microcrystalline cellulose, Ac-Di-Sol, glue
State silica, talcum powder are well mixed in efficient mixer-granulator, and magnesium stearate is sprayed onto punch head surface, are pressed using rotation
Piece machine tabletting.
Embodiment 3
Sample is made using Examples 1 and 2, is detected with detection method of the Chinese Pharmacopoeia version in 2015 about the tablet content uniformity
Plain piece is as a result as follows：
| Sample ID | Content average (n=10) | Scope | Conclusion |
| Embodiment 1 | 10.02% | 9.84%-10.24% | Meet the requirements |
| Embodiment 2 | 9.98% | 9.80%-10.20% | Meet the requirements |
The sample of Example 1 and 2, the finish of plain piece and complete situation are observed, it is as a result as follows：
| Sample ID | Finish | Complete situation | Punch head surface situation |
| Embodiment 1 | It is bright and clean | Completely | It is bright |
| Embodiment 2 | It is bright and clean | Completely | It is bright |
The sample of Example 1 and 2, stripping curve investigation, the factors influencing about material are done, and grind listing product with original and do
Compare, it is as a result as follows：
Stripping curve comparing result
Relevant material comparing result
Claims (2)
- A kind of 1. tablet containing escitalopram oxalate, it is characterised in that：Described escitalopram oxalate tablet bag Containing escitalopram oxalate and magnesium stearate, the percentage by weight of magnesium stearate in tablets is less than 0.1%；Described oxalic acid The median particle diameter of escitalopram raw material is not less than 300 μm.
- 2. prepare a kind of method of escitalopram oxalate tablet described in claim 1, it is characterised in that：Its step bag Include：By escitalopram oxalate, microcrystalline cellulose, Ac-Di-Sol, colloidal silica, talcum powder in efficient In mixer-granulator, it is well mixed, then magnesium stearate is sprayed onto punch head surface, rotary press tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710473553.2A CN107441052A (en) | 2017-06-21 | 2017-06-21 | A kind of tablet containing escitalopram oxalate and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710473553.2A CN107441052A (en) | 2017-06-21 | 2017-06-21 | A kind of tablet containing escitalopram oxalate and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107441052A true CN107441052A (en) | 2017-12-08 |
Family
ID=60486826
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710473553.2A Pending CN107441052A (en) | 2017-06-21 | 2017-06-21 | A kind of tablet containing escitalopram oxalate and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107441052A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111514110A (en) * | 2020-05-07 | 2020-08-11 | 福建海西新药创制有限公司 | Pharmaceutical composition containing escitalopram oxalate and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1536997A (en) * | 2001-07-31 | 2004-10-13 | H��¡�±�������˾ | Crystalline composition containing escitalopram |
-
2017
- 2017-06-21 CN CN201710473553.2A patent/CN107441052A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1536997A (en) * | 2001-07-31 | 2004-10-13 | H��¡�±�������˾ | Crystalline composition containing escitalopram |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111514110A (en) * | 2020-05-07 | 2020-08-11 | 福建海西新药创制有限公司 | Pharmaceutical composition containing escitalopram oxalate and preparation method thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20171208 |
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| RJ01 | Rejection of invention patent application after publication |