CN105726466A - Oxcarbazepine injection and preparation method thereof - Google Patents
Oxcarbazepine injection and preparation method thereof Download PDFInfo
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- CN105726466A CN105726466A CN201410747831.5A CN201410747831A CN105726466A CN 105726466 A CN105726466 A CN 105726466A CN 201410747831 A CN201410747831 A CN 201410747831A CN 105726466 A CN105726466 A CN 105726466A
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- injection
- oxcarbazepine
- cyclodextrin
- water
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Abstract
The invention discloses an injection, which takes oxcarbazepine as a major ingredient and is added with an inclusion agent, so that the injection is in the form of a homogeneous and stable colorless and transparent solution; the injection, after being preserved for a long time, is stable in character, and the content of active ingredients can reach 0.5-5%. In the case of emergency, for example patients are undergoing operations or some patients suffer from gastrointestinal diseases, the oxcarbazepine injection can be administrated timely when diseases attack in the patients who have trouble in taking drugs through oral administration.
Description
Technical field
The present invention relates to the preparing technical field of oxcarbazepine medicament, especially a kind of oxcarbazepine injection and preparation method thereof.
Background technology
Oxcarbazepine (10,11-dihydro-10-oxo-5H-dibenzo [b, f] azepine-5-carboxamide), white is to light yellow crystalline powder, and this product is antuepileptic, is the 10-ketone group derivant of carbamazepine, its drug effect is similar to carbamazepine, acts on identical or slightly strong, but its untoward reaction is few.There is the inhibitory action of high selectivity cerebral cortex layer motor region by this product, it is therefore prevented that the propagation of abnormal electric wave, epilepsy limitation or tonic clonic seizure and affective disorders is all had satisfied curative effect, trigeminal neuralgia also has good analgesic effect.For treating epilepsy limitation and tonic clonic seizure, can effectively improve the Vigilance of patient, identification and memory.Can be additionally used in anti-trigeminal neuralgia, the untoward reaction such as it is tired, movement disorder, impotence is less.
Oxcarbazepine is slightly molten in chloroform, slightly soluble in methanol, acetone and dichloromethane, almost insoluble in water, ethanol, 0.1mol/L hydrochloric acid or sodium hydroxide solution.Due to the indissoluble character of oxcarbazepine, the inclusion technique of cyclodextrin is utilized to improve oxcarbazepine dissolubility in water, in order to make injection.
Summary of the invention
It is an object of the invention in emergency situations, as patient in operation, some gastroenteropathys patient, morbidity time oral drugs have an obstacle, oxcarbazepine injection can drug treatment in time.
The technical solution used in the present invention is:
A kind of oxcarbazepine injection, it is characterised in that: every 100 milliliters comprise following components:
Oxcarbazepine 0.5-5g
Solubilizing agent 0.5-5g
And, described solubilizing agent is hydroxypropyl-beta-cyclodextrin, sulfoalkyl cyclodextrin, sulphur butyl-beta-cyclodextrin.Through investigating, when the ratio of oxcarbazepine and cyclodextrin is 1:1, effect is best.
The preparation method that it is a further object to provide a kind of oxcarbazepine injection, comprises the following steps:
Cyclodextrin is mixed with water for injection；
Above-mentioned solution adds oxcarbazepine；
Water for injection is settled to 100ml, prepares finished product after membrane filtration is degerming.
Advantages of the present invention and good effect: in the present invention, with oxcarbazepine for main component, add cyclodextrin, makes injection form the colourless transparent solution of isotropic stable, and after long-term storage, character is stable, easy to use, safety.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is further described, and following embodiment is illustrative is not determinate, it is impossible to limit protection scope of the present invention with following embodiment.
Embodiment 1
0.5g cyclodextrin is mixed with 50ml water for injection, forms settled solution
Above-mentioned solution adds 0.5g oxcarbazepine, stirs 24 hours
Water for injection is settled to 100ml, with 0.22um membrane filtration degerming after, through inspection fill after prepare finished product.
The active constituent content preparing oxcarbazepine injection is 0.5%.
Embodiment 2
1g cyclodextrin is mixed with 50ml water for injection, forms settled solution
Above-mentioned solution adds 1g oxcarbazepine, stirs 24 hours
Water for injection is settled to 100ml, with 0.22um membrane filtration degerming after, through inspection fill after prepare finished product.
The active constituent content preparing oxcarbazepine injection is 1%.
Embodiment 3
2g cyclodextrin is mixed with 50ml water for injection, forms settled solution
Above-mentioned solution adds 2g oxcarbazepine, stirs 24 hours
Water for injection is settled to 100ml, with 0.22um membrane filtration degerming after, through inspection fill after prepare finished product.
The active constituent content preparing oxcarbazepine injection is 2%.
Embodiment 4
3g cyclodextrin is mixed with 50ml water for injection, forms settled solution
Above-mentioned solution adds 3g oxcarbazepine, stirs 24 hours
Water for injection is settled to 100ml, with 0.22um membrane filtration degerming after, through inspection fill after prepare finished product.
The active constituent content preparing oxcarbazepine injection is 3%.
Embodiment 5
4g cyclodextrin is mixed with 50ml water for injection, forms settled solution
Above-mentioned solution adds 4g oxcarbazepine, stirs 24 hours
Water for injection is settled to 100ml, with 0.22um membrane filtration degerming after, through inspection fill after prepare finished product.
The active constituent content preparing oxcarbazepine injection is 4%.
Embodiment 6
5g cyclodextrin is mixed with 50ml water for injection, forms settled solution
Above-mentioned solution adds 5g oxcarbazepine, stirs 24 hours
Water for injection is settled to 100ml, with 0.22um membrane filtration degerming after, through inspection fill after prepare finished product.
The active constituent content preparing oxcarbazepine injection is 5%.
Claims (5)
1. the injection treating epilepsy, it is characterised in that: with oxcarbazepine for main component, add solubilizing agent, improve oxcarbazepine dissolubility in water, in order to make injection.
2. the injection for the treatment of epilepsy according to claim 1, it is characterised in that can in emergency situations, as patient in operation, some gastroenteropathys patient, morbidity time oral drugs have an obstacle, oxcarbazepine injection can drug treatment in time.
3. described solubilizing agent according to claim 1 is hydroxypropyl-beta-cyclodextrin, sulfoalkyl cyclodextrin, sulphur butyl-beta-cyclodextrin etc..
4. the injection for the treatment of epilepsy according to claim 1, it is characterised in that the amount ranges of described solubilizing agent is 0.5-5% (W/V).
5. the injection for the treatment of epilepsy according to claim 1, it is characterised in that the amount ranges of oxcarbazepine used is 0.5%～5% (W/V), and the ratio of oxcarbazepine and cyclodextrin is preferably 1:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410747831.5A CN105726466A (en) | 2014-12-10 | 2014-12-10 | Oxcarbazepine injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410747831.5A CN105726466A (en) | 2014-12-10 | 2014-12-10 | Oxcarbazepine injection and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105726466A true CN105726466A (en) | 2016-07-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410747831.5A Pending CN105726466A (en) | 2014-12-10 | 2014-12-10 | Oxcarbazepine injection and preparation method thereof |
Country Status (1)
| Country | Link |
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| CN (1) | CN105726466A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265501A (en) * | 2016-09-28 | 2017-01-04 | 西安新通药物研究有限公司 | Stable fosphenytoin composition of sodium and preparation thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2017959A1 (en) * | 1989-06-02 | 1990-12-02 | Anne-Francoise Steulet | Intravenous solutions with a rapid onset of action |
| CN1274286A (en) * | 1997-10-09 | 2000-11-22 | 诺瓦提斯公司 | Parenteral formulations comprising carbamazepine or its derivatives |
| US20040157797A1 (en) * | 2003-02-03 | 2004-08-12 | Rong-Kun Chang | Drug formulation and delivery using crystalline methylated cyclodextrins |
| CN101309691A (en) * | 2005-09-30 | 2008-11-19 | 奥瓦什医药品公司 | Novel parenteral carbamazepine formulation |
| CN103536596A (en) * | 2009-01-30 | 2014-01-29 | 克迪斯药品有限公司 | Transdermal delivery of diclofenac, carbamazepine and benzydamine |
-
2014
- 2014-12-10 CN CN201410747831.5A patent/CN105726466A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2017959A1 (en) * | 1989-06-02 | 1990-12-02 | Anne-Francoise Steulet | Intravenous solutions with a rapid onset of action |
| CN1274286A (en) * | 1997-10-09 | 2000-11-22 | 诺瓦提斯公司 | Parenteral formulations comprising carbamazepine or its derivatives |
| US20040157797A1 (en) * | 2003-02-03 | 2004-08-12 | Rong-Kun Chang | Drug formulation and delivery using crystalline methylated cyclodextrins |
| CN101309691A (en) * | 2005-09-30 | 2008-11-19 | 奥瓦什医药品公司 | Novel parenteral carbamazepine formulation |
| CN103536596A (en) * | 2009-01-30 | 2014-01-29 | 克迪斯药品有限公司 | Transdermal delivery of diclofenac, carbamazepine and benzydamine |
Non-Patent Citations (1)
| Title |
|---|
| 陈满章，崔山凤: "卡马西平的制剂研究", 《黑龙江医学》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106265501A (en) * | 2016-09-28 | 2017-01-04 | 西安新通药物研究有限公司 | Stable fosphenytoin composition of sodium and preparation thereof |
| CN106265501B (en) * | 2016-09-28 | 2017-06-23 | 西安新通药物研究有限公司 | The Fosphenytoin composition of sodium and its preparation of stabilization |
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Application publication date: 20160706 |
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