CN103705933A - Oxcarbazepine medicinal composition and preparation method thereof - Google Patents
Oxcarbazepine medicinal composition and preparation method thereof Download PDFInfo
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- CN103705933A CN103705933A CN201310699911.3A CN201310699911A CN103705933A CN 103705933 A CN103705933 A CN 103705933A CN 201310699911 A CN201310699911 A CN 201310699911A CN 103705933 A CN103705933 A CN 103705933A
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Abstract
The invention discloses an oxcarbazepine hydrochloride medicinal composition. The medicinal composition is characterized by comprising the following components in percentage by weight: 20-60 percent of oxcarbazepine hydrochloride, 20-50 percent of lactose anhydrous, 10-30 percent of microcrystalline cellulose, 1-10 percent of crospolyvinylpyrrolidone, 1-10 percent of poloxamer, and 1-2 percent of superfine silica gel powder. The oxcarbazepine hydrochloride medicinal composition is good in stability, and has more remarkable advantages of improving product yield, reducing cost, realizing industrialization and better clinically applying.
Description
Technical field
The invention belongs to medical technology preparation field, be specifically related to a kind of oxcarbazepine pharmaceutical composition having good stability and preparation method thereof.
Background technology
Main component is that oxcarbazepine is used for the treatment of constitutional generalized tonic-clonic seizure and partial seizures, with or without Secondary cases Generalized seizure.
Although at present the precise mechanism of most antiepileptic effects is understood fully not yet completely, still can think that such medicine is by changing the activity of the basic medium of neuronal excitability, i.e. regulation and control of the voltage of brain and neurotransmitter ion channel and produce its effectiveness.Find in the light of recent researches, the anticonvulsant action of oxcarbazepine and its monohydroxy derivant (MHD) is mainly the Voltage-gated Sodium Channels of having blocked brain.In treatment, during concentration, these two kinds of compounds have suppressed the persistence high frequency reignition of the neuronic sodium dependency of the Mus in cell culture action potential, and this effect may contribute to block the propagation of the epilepsy electrical activity of epileptogenic focus.In addition, the results of in vitro studies of Mus hippocampal tissue section shows, the antiepileptic action of racemization MHD and two kinds of enantiomer thereof is also because there is the participation of potassium-channel to regulate.
Oxcarbazepine essential information is as follows:
English name: Oxcarbazepine
No. CAS: 28721-07-5
Chemical name: 10,11-dihydro-10-oxo-5H-Dibenzo [b, f] azepine-5-carboxylic acid amides
Chemical structural formula:
Molecular formula: C15H12N2O2
Molecular weight: 252.27
In order to meet the requirement of clinical application to product quality, stability, the inventor has invented oxcarbazepine pharmaceutical composition through lot of experiments research, successfully solved the problem of oxcarbazepine less stable, and dissolution rate is fast, improved bioavailability, also reduced production cost simultaneously, easy to implement, can realize industrialization, remarkable in economical benefits.
Summary of the invention
The first object of the present invention is to provide a kind of oxcarbazepine pharmaceutical composition, this oxcarbazepine pharmaceutical composition good stability, and dissolution rate is fast, bioavailability is high, to improving product yield, reduces costs, realize industrialization, be better applied to clinically, there is more obvious advantage.
The second object of the present invention is to provide the preparation method of oxcarbazepine compositions of the present invention, and the method is simple, prepared oxcarbazepine pharmaceutical composition good stability.
The inventor, through a large amount of tests, is surprised to find in oxcarbazepine pharmaceutical composition, gives lactose and the microcrystalline Cellulose of proper proportion, adds other adjuvants, can meet preparation requirement.
Pharmaceutical composition provided by the present invention, is characterized in that, the oxcarbazepine pharmaceutical composition described in it, and every its formula of 1000 capsules consists of:
Oxcarbazepine pharmaceutical composition of the present invention is adopted preparation with the following method:
Oxcarbazepine, lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, poloxamer are placed in to mixer, mix 5-10 minute, make mix homogeneously; In the material of above-mentioned mix homogeneously, add purified water appropriate, make the soft material that hardness is suitable; Adopt 18 eye mesh screens to make the granule that granularity is suitable soft material; Under 55 ± 5 ℃ of conditions, airpillow-dry to pellet moisture is less than 3%; Granule is taken out, add micropowder silica gel to mix 20 minutes, mix homogeneously; Intermediate detects, and detects index and comprises content, and moisture etc., according to cubage loading amount scope; Filling, in No. 1 capsule, obtains.
The inventor finds through a large amount of experimental study, when oxcarbazepine compositions is above-mentioned formula, and described pharmaceutical composition the best in quality, stability is best.
Another aspect of the present invention provides the preparation method of oxcarbazepine pharmaceutical composition of the present invention, and the method is simple, prepared oxcarbazepine pharmaceutical composition good stability, and bioavailability is high.
The oxcarbazepine pharmaceutical composition making according to the inventive method is through industrial amplification production and study on the stability, proves that product is stable, through pharmacology, toxicological test, to human body without injury.
By test data, beneficial effect of the present invention is described below.
With the product of the embodiment of the present invention 1, investigate indices as follows:
Embodiment 1 accelerated test result
Result shows, the sample quality of the embodiment of the present invention 1 is stable, and stripping is fast, and bioavailability is high, and impurity changes little, and steady quality is reliable.
The invention has the advantages that, overcome problem in prior art, product can be maintained a long-term stability.
Tool of the present invention has the following advantages:
1) new oxcarbazepine compositions provided by the present invention has thoroughly solved the stability problem of oxcarbazepine.
2) oxcarbazepine pharmaceutical composition provided by the present invention is for improving the yield of this product, the market risk of reduction product, and being better applied to clinical treatment has very large help.
3) new oxcarbazepine compositions provided by the present invention, through industrialized great production and study on the stability, proves constant product quality.
4) preparation method of new oxcarbazepine compositions provided by the present invention, the method is simple, prepared oxcarbazepine pharmaceutical composition good stability, bioavailability is high.
The specific embodiment
Below will describe oxcarbazepine pharmaceutical composition of the present invention in detail.Enumerate embodiment below, the present invention is described in more detail, but these concrete examples are not intended to limit the present invention.
Embodiment 1
Oxcarbazepine pharmaceutical composition described in every 1000 capsules, its formula consists of:
Preparation technology:
Oxcarbazepine, lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, poloxamer are placed in to mixer, mix 5-10 minute, make mix homogeneously; In the material of above-mentioned mix homogeneously, add purified water appropriate, make the soft material that hardness is suitable; Adopt 18 eye mesh screens to make the granule that granularity is suitable soft material; Under 55 ± 5 ℃ of conditions, airpillow-dry to pellet moisture is less than 3%; Granule is taken out, add micropowder silica gel to mix 20 minutes, mix homogeneously; Intermediate detects, and detects index and comprises content, and moisture etc., according to cubage loading amount scope; Filling, in No. 1 capsule, obtains.
Embodiment 2
Oxcarbazepine pharmaceutical composition described in every 1000 capsules, its formula consists of:
Preparation technology: with embodiment 1.
Embodiment 3
Oxcarbazepine pharmaceutical composition described in every 1000 capsules, its formula consists of:
Preparation technology: with embodiment 1.
Embodiment 4
Oxcarbazepine pharmaceutical composition described in every 1000 capsules, its formula consists of:
Preparation technology: with embodiment 1.
Embodiment 5
Oxcarbazepine pharmaceutical composition described in every 1000 capsules, its formula consists of:
Preparation technology: with embodiment 1.
Test example 1
This test example is to investigate the stability of oxcarbazepine compositions provided by the present invention.
The accelerated test of oxcarbazepine pharmaceutical composition
According to the method for the embodiment of the present invention 1, prepare three batches of oxcarbazepine pharmaceutical compositions (lot number is respectively 20130301,20130302,20130303) according to commercially available back, at 40 ℃ ± 2 ℃, the condition of RH75% ± 5% is placed 6 months, during this time respectively at sampling in the 1st, 2,3,6 months, according to stability inspection item, detect, and with 0 day data comparison.
Above conclusion (of pressure testing) can be found out: this product is placed 6 months every detection indexs and compared no significant difference, good stability with 0 month under accelerated test condition.
Claims (3)
1. containing an oxcarbazepine pharmaceutical composition, it is characterized in that being formed by following ingredients and percentage by weight: 20%-60% oxcarbazepine, 20%-50% lactose, 10%-30% microcrystalline Cellulose, 1%-10% crospolyvinylpyrrolidone, 1%-10% poloxamer, 1%-2% micropowder silica gel.
2. pharmaceutical compositions according to claim 1, is characterized in that the oxcarbazepine pharmaceutical composition described in it, and every its formula of 1000 capsules consists of:
3. the preparation method of oxcarbazepine pharmaceutical composition according to claim 1, it is characterized in that, the method comprises the steps: oxcarbazepine, lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, poloxamer to be placed in mixer, mixes 5-10 minute, makes mix homogeneously; In the material of above-mentioned mix homogeneously, add purified water appropriate, make the soft material that hardness is suitable; Adopt 18 eye mesh screens to make the granule that granularity is suitable soft material; Under 55 ± 5 ℃ of conditions, airpillow-dry to pellet moisture is less than 3%; Granule is taken out, add micropowder silica gel to mix 20 minutes, mix homogeneously; Intermediate detects, and detects index and comprises content, and moisture etc., according to cubage loading amount scope; Filling, in No. 1 capsule, obtains.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310699911.3A CN103705933A (en) | 2013-12-18 | 2013-12-18 | Oxcarbazepine medicinal composition and preparation method thereof |
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| CN201310699911.3A CN103705933A (en) | 2013-12-18 | 2013-12-18 | Oxcarbazepine medicinal composition and preparation method thereof |
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| CN103705933A true CN103705933A (en) | 2014-04-09 |
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| CN201310699911.3A Pending CN103705933A (en) | 2013-12-18 | 2013-12-18 | Oxcarbazepine medicinal composition and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111481521A (en) * | 2020-04-14 | 2020-08-04 | 上海奥科达生物医药科技有限公司 | Oxcarbazepine sustained release preparation, preparation method and application thereof |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1522140A (en) * | 2001-05-18 | 2004-08-18 | 兰贝克赛实验室有限公司 | Oxcarbazepine dosage forms |
| US20060141037A1 (en) * | 2004-12-29 | 2006-06-29 | J. B. Chemicals & Pharmaceuticals Ltd. | Bilayer tablets of oxcarbazepine for controlled delivery and a process of preparation thereof |
| US20070178164A1 (en) * | 2006-01-31 | 2007-08-02 | Sigal Blau | Pharmaceutical formulations of oxcarbazepine and methods for its preparation |
| WO2008021875A2 (en) * | 2006-08-08 | 2008-02-21 | Accu-Break Technologies, Inc. | Pharmaceutical tablets containing a plurality of active segments |
| CN101212958A (en) * | 2005-06-29 | 2008-07-02 | 万能药生物有限公司 | Modified release pharmaceutical compositions on the basis of two polymers and processes thereof |
| CN101212957A (en) * | 2005-06-29 | 2008-07-02 | 万能药生物有限公司 | Novel pharmaceutical sustained release compositions and processes thereof |
-
2013
- 2013-12-18 CN CN201310699911.3A patent/CN103705933A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1522140A (en) * | 2001-05-18 | 2004-08-18 | 兰贝克赛实验室有限公司 | Oxcarbazepine dosage forms |
| US20060141037A1 (en) * | 2004-12-29 | 2006-06-29 | J. B. Chemicals & Pharmaceuticals Ltd. | Bilayer tablets of oxcarbazepine for controlled delivery and a process of preparation thereof |
| CN101212958A (en) * | 2005-06-29 | 2008-07-02 | 万能药生物有限公司 | Modified release pharmaceutical compositions on the basis of two polymers and processes thereof |
| CN101212957A (en) * | 2005-06-29 | 2008-07-02 | 万能药生物有限公司 | Novel pharmaceutical sustained release compositions and processes thereof |
| US20070178164A1 (en) * | 2006-01-31 | 2007-08-02 | Sigal Blau | Pharmaceutical formulations of oxcarbazepine and methods for its preparation |
| WO2008021875A2 (en) * | 2006-08-08 | 2008-02-21 | Accu-Break Technologies, Inc. | Pharmaceutical tablets containing a plurality of active segments |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111481521A (en) * | 2020-04-14 | 2020-08-04 | 上海奥科达生物医药科技有限公司 | Oxcarbazepine sustained release preparation, preparation method and application thereof |
| CN111481521B (en) * | 2020-04-14 | 2021-04-02 | 上海奥科达生物医药科技有限公司 | Oxcarbazepine sustained release preparation, preparation method and application thereof |
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Application publication date: 20140409 |