CN106236720A - A kind of pharmaceutical composition of entacapone and preparation method thereof - Google Patents
A kind of pharmaceutical composition of entacapone and preparation method thereof Download PDFInfo
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- CN106236720A CN106236720A CN201610763398.3A CN201610763398A CN106236720A CN 106236720 A CN106236720 A CN 106236720A CN 201610763398 A CN201610763398 A CN 201610763398A CN 106236720 A CN106236720 A CN 106236720A
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- pharmaceutical composition
- entacapone
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- present
- weight
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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
-
- 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
- A61K31/275—Nitriles; Isonitriles
- A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides the pharmaceutical composition of a kind of entacapone, described pharmaceutical composition is dispersible tablet, in parts by weight, including entacapone 100 400 parts, polyvinyl alcohol 20 60 parts, sodium stearyl fumarate 50 500 parts, sodium laurylsulfate 80 200 parts, Myrj 45 50 120 parts, carboxymethyl cellulose 80 160 parts, cross-linked carboxymethyl cellulose 80 160 parts, 60% ethanol solution 30 80 parts.Dispersible tablet is made according to galenic pharmacy routine techniques.The pharmaceutical composition of the entacapone of the present invention, overcomes defect of the prior art, has stable, and safety absorbs fast, dissolves the advantages such as fast.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to pharmaceutical composition of a kind of entacapone and preparation method thereof.
Background technology
Entacapone, ((E))-2-cyano group-3-(3,4-dihydroxy-5-nitrobenzophenone)-N-diethyl-2-acrylamide),
Being catechol O-methyltransferase (COMT) inhibitor, it combines with levodopa and dopa decarboxylase inhibitor and is used for treating
Parkinson disease (PD).Independent formulations is with trade nameWithSell, and fixed Combination (levodopa:
Carbidopa: entacapone: 50mg:12.5mg:200mg, 100mg:25mg:200mg and 150mg:37.5mg:200mg) with business
The name of an articleSell.
When process suffer serious switching ripple late period PD patient symptom time pay particular attention to.Doctor is usually them
Output separate dosage forms, this is because the elasticity in terms of this dosage form dosage.If so those are suffered to obtain the dosage form conveniently taken
Person's (being especially in the presence of the patient of dysphagia) will be benefited.
In recent years, oral preparation of quick releasing develops quickly, according to statistics, and nearly 200,000,000 dollars of world's quick releasing formulation sales volume in 1996.
Wherein can the dispersible tablet of disintegrate uniformly Viscous suspension liquid rapidly, due to its taking convenience, absorb fast, bioavailability is high
Feature, is increasingly subject to the concern of people.The kind of this kind of dosage form the most gradually increases.It is predicted following 10 years, all sale in the world
In medicine, about 10% will occur with novel release dosage forms, and its market sale share is anticipated annual increases by 1%, and this is instant for dispersible tablet
Novel form is expected faster to be developed.
Entacapone dosage form is mainly tablet, owing to entacapone water solublity is bad, it is difficult to absorb, by entacapone as
The dosage form of dispersible tablet encounters difficulty.
Summary of the invention
The present invention, through screening study, have found solution, and improves the rapid disintegrate of water of a kind of chance, drug-eluting
Hurry up, bioavailability is high.It is more easy to take relative to the patient of old man and dysphagia simultaneously, good in taste, taking convenience, patient
It is prone to accept, it is simple to the novel formulation carried.
The first aspect of the invention is to provide the pharmaceutical composition of a kind of entacapone, and described pharmaceutical composition is dispersion
Tablet, in parts by weight, including:
Preferably, described pharmaceutical composition in parts by weight, including:
It is further preferred that described pharmaceutical composition is in parts by weight, including:
It is further preferred that described pharmaceutical composition is in parts by weight, including:
The second aspect of the invention is to provide the preparation side of the pharmaceutical composition described in first aspect of a kind of present invention
Method: use the component of described pharmaceutical composition, makes dispersible tablet according to galenic pharmacy routine techniques.
The pharmaceutical composition of the entacapone of the present invention, overcomes defect of the prior art, has stable, and safety is inhaled
Receive fast, dissolve the advantages such as fast.
Detailed description of the invention
The present invention is described further by the following examples, but not as limitation of the present invention.
Embodiment 1
The pharmaceutical composition of the entacapone of the present embodiment in parts by weight, including:
Galenic pharmacy routine techniques is used to prepare, as the carrier of active component and medicine is mixed, tabletting etc..
Specifically can use following methods:
1. the preparation of supplementary material and process: entacapone disperseed 200 mesh sieves standby, polyvinyl alcohol, stearoyl alcohol are rich
Horse acid sodium, sodium laurylsulfate lactose, Myrj 45, carboxymethyl cellulose, cross-linked carboxymethyl cellulose cross 100 mesh sieves
Standby.
2. weigh and mix:
Calculate inventory according to recipe quantity through double verification and weigh above-mentioned supplementary material respectively.Above-mentioned supplementary material is passed by equivalent
Addition mix homogeneously.
3. pelletize:
With 60% ethanol solution soft material, pelletizing with 20 mesh nylon wires, the granule prepared should lack particulate, neat without strip.
The temperature of 55 ± 2 DEG C, it is dried 5-7 hour in drying baker.In pelletization, there is excessive granule, need the granulate that sieves,
Make into the single-size of applicable tabletting；Sieve selection 16 mesh sieve granulate.Mix homogeneously, places in hermetic container, after the assay was approved
Tabletting.
4. measure granule content, calculate tablet weight: sampling is pressed quality standard and measured granule content, and theoretical tablet weight is 0.9g.
5. tabletting: according to the actual tablet weight of result of calculation gained, regulates tabletting machine, puts into hermetic container and take out after completing
Sample checks hardness.
6. the inspection of semifinished product: pack after the assay was approved by quality criteria requirements.
7. pack according to the requirement of product, put in storage after packaging, can dispatch from the factory after the assay was approved according to quality standard.
Embodiment 2
The present embodiment is with the difference of embodiment 1, and the pharmaceutical composition of the entacapone of the present embodiment is according to weight
Amount number meter, including:
Embodiment 3
The present embodiment is with the difference of embodiment 1, and the pharmaceutical composition of the entacapone of the present embodiment is according to weight
Amount number meter, including:
Embodiment 4
The present embodiment is with the difference of embodiment 1, and the pharmaceutical composition of the entacapone of the present embodiment is according to weight
Amount number meter, including:
Embodiment 5
The present embodiment is with the difference of embodiment 1, and the pharmaceutical composition of the entacapone of the present embodiment is according to weight
Amount number meter, including:
Embodiment 6
The present embodiment is with the difference of embodiment 1, and the pharmaceutical composition of the entacapone of the present embodiment is according to weight
Amount number meter, including:
Dissolution Rate Testing:
HPLC Example 1-6 is used to shine dissolution method (Chinese Pharmacopoeia two annex XC the second methods of version in 2000),
With water 900ml as solvent, rotating speed is 50 turns per minute, takes a little at 2,4,7,10,15 minutes respectively, precision measure filtrate 5ml →
50ml measuring bottle is diluted with water to scale shake up, mends dissolution fluid 5ml, according to spectrophotography (annex IV A), at the wavelength of 274nm
Place measures trap, the results are shown in Table 1.
Table 1 stripping curve measurement result
| 2min | 4min | 10min | 15min | Hardness | Dispersing uniformity | |
| Embodiment 1 | 38.2% | 64.4% | 95.6% | 99.9% | 12.7kg | 48s |
| Embodiment 2 | 38.1% | 63.8% | 95.1% | 99.9% | 12.6kg | 50s |
| Embodiment 3 | 37.8% | 63.6% | 94.8% | 99.8% | 12.5kg | 53s |
| Embodiment 4 | 37.9% | 63.2% | 94.7% | 99.8% | 12.4kg | 54s |
| Embodiment 5 | 37.8% | 62.4% | 94.2% | 99.7% | 12.2kg | 58s |
| Embodiment 6 | 37.9% | 62.1% | 93.8% | 99.7% | 11.9kg | 59s |
Factors affecting stability is tested:
Strong illumination is tested: Example 1-6 sheet is placed in glass dish, places under the illumination of 4500LX ± 100LX
10 days, in sampling detection in 0,5,10 days.
Hot test: Example 1-6 sheet is placed in glass dish, places 10 days in the calorstat of 60 DEG C, in 0,5,
Sampling detection in 10 days.
High wet test: Example 1-6 sheet is placed in glass dish, at relative humidity 75%, (NaCl is saturated molten respectively
Liquid), 92.5% (KNO3Saturated solution) calorstat in place 10 days, in 0,5,10 days sampling detection.
More than test result indicate that, this product is the most stable under conditions of illumination, 60 DEG C of high temperature and high humidity.
Being described in detail the specific embodiment of the present invention above, but it is intended only as example, the present invention does not limit
It is formed on particular embodiments described above.To those skilled in the art, any equivalent modifications that the present invention is carried out and
Substitute the most all among scope of the invention.Therefore, the impartial conversion made without departing from the spirit and scope of the invention and
Amendment, all should contain within the scope of the invention.
Claims (5)
1. the pharmaceutical composition of an entacapone, it is characterised in that described pharmaceutical composition is dispersible tablet, according to weight portion
Number meter, including:
The pharmaceutical composition of entacapone the most according to claim 1, it is characterised in that described pharmaceutical composition is according to weight
Amount number meter, including:
The pharmaceutical composition of entacapone the most according to claim 2, it is characterised in that described pharmaceutical composition is according to weight
Amount number meter, including:
The pharmaceutical composition of entacapone the most according to claim 2, it is characterised in that described pharmaceutical composition is according to weight
Amount number meter, including:
5. the preparation method of the pharmaceutical composition as described in any one in claim 1-4, it is characterised in that use institute
State the component of pharmaceutical composition, make dispersible tablet according to galenic pharmacy routine techniques.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610763398.3A CN106236720A (en) | 2016-08-29 | 2016-08-29 | A kind of pharmaceutical composition of entacapone and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610763398.3A CN106236720A (en) | 2016-08-29 | 2016-08-29 | A kind of pharmaceutical composition of entacapone and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106236720A true CN106236720A (en) | 2016-12-21 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610763398.3A Pending CN106236720A (en) | 2016-08-29 | 2016-08-29 | A kind of pharmaceutical composition of entacapone and preparation method thereof |
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| CN (1) | CN106236720A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113109465A (en) * | 2021-03-22 | 2021-07-13 | 海南通用康力制药有限公司 | Entacapone quality detection method and application |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1319005A (en) * | 1998-09-14 | 2001-10-24 | 欧里恩公司 | Pharmaceutical composition comprising entacapone or nitecapone as well as cross-linked cellulose derivative |
| CN101184483A (en) * | 2005-06-08 | 2008-05-21 | 奥赖恩公司 | An entacapone-containging oral dosage form |
| CN101780073A (en) * | 2009-01-21 | 2010-07-21 | 重庆圣华曦药业有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
| CN101939003A (en) * | 2008-02-06 | 2011-01-05 | 沃克哈特研究中心 | Pharmaceutical compositions of entacapone, levodopa and carbidopa with improved bioavailability |
| CN103127123A (en) * | 2011-12-02 | 2013-06-05 | 苏州法莫生物技术有限公司 | Entacapone/folic acid compound medicine composition and application thereof |
| CN103845318A (en) * | 2012-12-07 | 2014-06-11 | 天津市汉康医药生物技术有限公司 | Entacapone dispersible tablet |
-
2016
- 2016-08-29 CN CN201610763398.3A patent/CN106236720A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1319005A (en) * | 1998-09-14 | 2001-10-24 | 欧里恩公司 | Pharmaceutical composition comprising entacapone or nitecapone as well as cross-linked cellulose derivative |
| CN101184483A (en) * | 2005-06-08 | 2008-05-21 | 奥赖恩公司 | An entacapone-containging oral dosage form |
| CN101939003A (en) * | 2008-02-06 | 2011-01-05 | 沃克哈特研究中心 | Pharmaceutical compositions of entacapone, levodopa and carbidopa with improved bioavailability |
| CN101780073A (en) * | 2009-01-21 | 2010-07-21 | 重庆圣华曦药业有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
| CN103127123A (en) * | 2011-12-02 | 2013-06-05 | 苏州法莫生物技术有限公司 | Entacapone/folic acid compound medicine composition and application thereof |
| CN103845318A (en) * | 2012-12-07 | 2014-06-11 | 天津市汉康医药生物技术有限公司 | Entacapone dispersible tablet |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113109465A (en) * | 2021-03-22 | 2021-07-13 | 海南通用康力制药有限公司 | Entacapone quality detection method and application |
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| PB01 | Publication | ||
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| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20161221 |