CN102716065B - Vinpocetine injection and preparation method thereof - Google Patents
Vinpocetine injection and preparation method thereof Download PDFInfo
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- CN102716065B CN102716065B CN201110361192.5A CN201110361192A CN102716065B CN 102716065 B CN102716065 B CN 102716065B CN 201110361192 A CN201110361192 A CN 201110361192A CN 102716065 B CN102716065 B CN 102716065B
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- injection
- vinpocetine
- water
- tartaric acid
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- DDNCQMVWWZOMLN-IRLDBZIGSA-N Vinpocetine Chemical compound C1=CC=C2C(CCN3CCC4)=C5[C@@H]3[C@]4(CC)C=C(C(=O)OCC)N5C2=C1 DDNCQMVWWZOMLN-IRLDBZIGSA-N 0.000 title claims abstract description 53
- 229960000744 vinpocetine Drugs 0.000 title claims abstract description 53
- 238000002347 injection Methods 0.000 title claims abstract description 36
- 239000007924 injection Substances 0.000 title claims abstract description 36
- 238000002360 preparation method Methods 0.000 title claims abstract description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 37
- 238000003756 stirring Methods 0.000 claims abstract description 33
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims abstract description 20
- 239000011975 tartaric acid Substances 0.000 claims abstract description 20
- 235000002906 tartaric acid Nutrition 0.000 claims abstract description 20
- 239000008215 water for injection Substances 0.000 claims abstract description 18
- 230000001954 sterilising effect Effects 0.000 claims abstract description 13
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229910052799 carbon Inorganic materials 0.000 claims abstract description 11
- 238000006392 deoxygenation reaction Methods 0.000 claims abstract description 11
- 239000000243 solution Substances 0.000 claims abstract description 4
- 239000000203 mixture Substances 0.000 claims abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 239000008400 supply water Substances 0.000 claims description 10
- 239000003814 drug Substances 0.000 abstract description 4
- 238000002474 experimental method Methods 0.000 abstract description 4
- 239000002245 particle Substances 0.000 abstract description 4
- 238000004519 manufacturing process Methods 0.000 abstract description 3
- 238000003860 storage Methods 0.000 abstract description 3
- 239000006184 cosolvent Substances 0.000 abstract description 2
- 238000004090 dissolution Methods 0.000 abstract 3
- 229940079593 drug Drugs 0.000 abstract 1
- 238000011049 filling Methods 0.000 abstract 1
- 238000001914 filtration Methods 0.000 abstract 1
- 238000010438 heat treatment Methods 0.000 abstract 1
- 238000011068 loading method Methods 0.000 abstract 1
- 239000011259 mixed solution Substances 0.000 abstract 1
- 238000001179 sorption measurement Methods 0.000 abstract 1
- 238000004659 sterilization and disinfection Methods 0.000 abstract 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 239000013618 particulate matter Substances 0.000 description 4
- 239000008187 granular material Substances 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 230000002490 cerebral effect Effects 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 210000003462 vein Anatomy 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 102000004861 Phosphoric Diester Hydrolases Human genes 0.000 description 1
- 108090001050 Phosphoric Diester Hydrolases Proteins 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000003727 cerebral blood flow Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000004089 microcirculation Effects 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000033904 relaxation of vascular smooth muscle Effects 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a vinpocetine injection and a preparation method thereof. The vinpocetine injection comprises 10 to 20 parts of vinpocetine, 7 to 15 parts of tartaric acid and 2000 parts of water. The preparation method of the vinpocetine injection comprises the following steps of 1, taking 80% of water for injection, carrying out filtration deoxygenation, heating to a temperature of 40 to 50 DEG C, adding tartaric acid into the heated water for injection, and stirring until complete dissolution, 2, adding vinpocetine into the solution obtained by the step 1, stirring until complete dissolution, supplying enough water for injection to the mixed solution, and carrying out stirring adsorption by 0.3% of active carbon, and 3, carrying out sterilization at a temperature of 121 DEG C for 15 minutes and carrying out nitrogen-filling loading. Utilization of tartaric acid in the components of the vinpocetine injection is conducive to dissolution of alkaline vinpocetine and can effectively inhibit the production of insoluble particles. A contrast experiment proves that through the preparation method, drug composition stability is improved. The production of insoluble particles shows that products are unstable due to prolonging of a storage period. The vinpocetine injection adopting tartaric acid as a cosolvent is stable and can produce a small amount of insoluble particles in a long time and thus the safety of the vinpocetine injection in use is ensured.
Description
Technical field
The invention belongs to field of medicine preparations, relate to a kind of Vinpocetine injection, meanwhile, the invention still further relates to a kind of preparation method of this Vinpocetine injection.
Background technology
Vinpocetine belongs to cerebral vasodilator, can suppress phosphodiesterase activity, increase the effect of the courier c-GMP of vascular smooth muscle relaxation, optionally increase cerebral blood flow, can also suppress platelet aggregation in addition, reduce human blood viscosity, strengthen erythrocyte deformabiliy, improve blood fluidity and microcirculation, promote cerebral tissue ingestion of glucose, increase brain oxygen consumption, improve brain metabolism.
In Vinpocetine injection long term storage process, easily produce insoluble particulates, affect the use safety of medicine, cause two classes to endanger, the insoluble granule filter that results in blockage while entering patient's vein obstruction vein blood vessel and intravenously administrable.
Summary of the invention
One of object of the present invention is to provide a kind of stable Vinpocetine injection.
To achieve these goals, technical program of the present invention lies in adopting a kind of Vinpocetine injection, consist of: vinpocetine 10-20 part, tartaric acid 7-15 part, 2000 parts, water.
Described water is water for injection.
In addition, the present invention also aims to provide a kind of preparation method of Vinpocetine injection safely and effectively.
To achieve these goals, the preparation method of Vinpocetine injection of the present invention, its step is as follows:
(1) get 80% water for injection and filter deoxygenation, be heated to 40-50 ℃, add tartaric acid, stir completely and dissolve;
(2) will in the resulting solution of step (1), add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
(3), at the temperature of 121 ℃, sterilizing 15min, fills nitrogen fill.
In each component of the present invention, tartaricly add the dissolving that not only contributes to alkaline vinpocetine, and can effectively stop the generation of particulate matter.Through Experimental Comparison, adopt technical solution of the present invention can strengthen the stability of pharmaceutical composition, the formation of insoluble granule has shown the product unstability that extends storage period and cause, with other acids contrasts, tartaric acid is more stable as the Vinpocetine injection of cosolvent, the insoluble granule quantity producing within the longer time still less, more can be guaranteed the safety that injection is used.
In addition, preparation method of the present invention can be used 121 ℃ of 15min sterilizings, illustrates that this prescription is stable, can be applied to suitability for industrialized production.Than original prescription, can adopt 121 ℃, the excessive sterilizing of 15min, guarantees the aseptic level of medicine.
The specific embodiment
Embodiment 1
In the present embodiment, Vinpocetine injection consists of:
Vinpocetine 10g, tartaric acid 7g, all the other are water for injection, make altogether injection 2000ml.Preparation method is as follows:
(1) water for injection of getting 80% consumption filters deoxygenation, is heated to 40 ℃, adds tartaric acid, stirs completely and dissolves.
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%.
At the temperature of (3) 121 ℃, sterilizing 15min, fills nitrogen fill.
Embodiment 2
The Vinpocetine injection of the present embodiment consists of: vinpocetine 12g, and tartaric acid 9g, all the other are injection water use, make altogether injection 2000ml.
Preparation method is as follows:
(1) get 80% water for injection and filter deoxygenation, be heated to 40 ℃, add tartaric acid, stir completely and dissolve;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
At the temperature of (3) 121 ℃, sterilizing 15min, fills nitrogen fill.
Embodiment 3
The Vinpocetine injection of the present embodiment consists of: vinpocetine 20g, and tartaric acid 13g, all the other are water for injection, make altogether injection 2000ml.
Preparation method is as follows:
(1) get 80% water for injection and filter deoxygenation, be heated to 40 ℃, add tartaric acid, stir completely and dissolve;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
At the temperature of (3) 121 ℃, sterilizing 15min, fills nitrogen fill.
Embodiment 4
The Vinpocetine injection of the present embodiment consists of:
Vinpocetine 10g, tartaric acid 10g, all the other are water for injection, make altogether injection 2000ml.Preparation method is as follows:
(1) 80% water for injection filters deoxygenation, is heated to 45 ℃, adds tartaric acid, stirs completely and dissolves;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
(3) 121 ℃, 15min sterilizing, fills nitrogen fill.
Embodiment 5
The Vinpocetine injection of the present embodiment consists of: in every injection 2000ml, contain vinpocetine 20g, tartaric acid 15g.
Preparation method is as follows:
(1) get 80% water for injection and filter deoxygenation, be heated to 50 ℃, add tartaric acid, stir completely and dissolve;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
The temperature of (3) 121 ℃, sterilizing 15min, fills nitrogen fill.
Vinpocetine injection different prescription stability and safety comparison
Comparative sample; Embodiment 1-5
Contrast experiment's example 1
Form:
Vinpocetine 10g citric acid 10g adds water to 2000ml
Preparation method is as follows:
The water for injection of (1) 80% consumption filters deoxygenation, is heated to 40 ℃, adds citric acid, stirs completely and dissolves;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
(3) 121 ℃, 15min sterilizing, fills nitrogen fill.
Contrast experiment's example 2
Form:
Vinpocetine 10g acetic acid 15g adds water to 2000ml.
Preparation method is as follows:
The water for injection of (1) 80% consumption filters deoxygenation, is heated to 45 ℃, adds acetic acid, stirs completely and dissolves;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
(3) 121 ℃, 15min sterilizing, fills nitrogen fill.
Contrast experiment's example 3
Form:
Vinpocetine 10g hydrochloric acid 10g adds water to 2000ml
Preparation method is as follows:
(1) water for injection of getting 80% consumption filters deoxygenation, is heated to 50 ℃, adds hydrochloric acid, stirs completely and dissolves;
(2) add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
(3) 121 ℃, 15min sterilizing, fills nitrogen fill.
Detection method:
(1) particulate matter: adopt light blockage method, in accordance with the law the particulate matter number of particle diameter > 10 μ m and > 25 μ m in the 1ml of each product that are prepared into of writing out a prescription of mensuration (2010 editions two appendix IX C of Chinese Pharmacopoeia).
The particulate matter number that 24 months results show to write out a prescription the present invention Vinpocetine injection produces is starkly lower than other comparative examples' prescriptions, illustrates that injection prepared by technical scheme of the present invention is safer.The results are shown in following table.
A table 124 month stability test Data Comparison
Claims (4)
1. a Vinpocetine injection, is characterized in that: consist of the following composition: vinpocetine 10-20 part, tartaric acid 7-15 part, 2000 parts, water.
2. Vinpocetine injection according to claim 1, is characterized in that: described water is water for injection.
3. Vinpocetine injection according to claim 1 and 2, is characterized in that: be preferably in every 2000ml injection and contain vinpocetine 10-20g, tartaric acid 7-15g.
4. a preparation method for the Vinpocetine injection as described in any one in claim 1-3, is characterized in that, comprises the following steps:
(1) get 80% water for injection and filter deoxygenation, be heated to 40-50 ℃, add tartaric acid, stir completely and dissolve;
(2) will in the resulting solution of step (1), add vinpocetine, stir, dissolve completely, supply water for injection, the active carbon stirring and adsorbing with 0.3%;
(3), at the temperature of 121 ℃, sterilizing 15min, fills nitrogen fill.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110361192.5A CN102716065B (en) | 2011-11-14 | 2011-11-14 | Vinpocetine injection and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110361192.5A CN102716065B (en) | 2011-11-14 | 2011-11-14 | Vinpocetine injection and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN102716065A CN102716065A (en) | 2012-10-10 |
| CN102716065B true CN102716065B (en) | 2014-04-16 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201110361192.5A Active CN102716065B (en) | 2011-11-14 | 2011-11-14 | Vinpocetine injection and preparation method thereof |
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| CN103462888B (en) * | 2013-09-16 | 2016-03-02 | 江苏正大清江制药有限公司 | Vinpocetine injection of a kind of beta-cyclodextrin inclusion compound of replacement and preparation method thereof |
| CN116858739B (en) * | 2023-07-19 | 2024-08-09 | 浙江天瑞药业有限公司 | Impurity detection method for iohexol injection |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101791310A (en) * | 2010-02-24 | 2010-08-04 | 王保明 | Vinpocetine medicine composition and preparation method thereof |
| CN101991530A (en) * | 2009-08-28 | 2011-03-30 | 沈阳志鹰制药厂 | Vinpocetine containing high-capacity sodium chloride injection and preparation method thereof |
| CN102091030A (en) * | 2011-01-20 | 2011-06-15 | 罗军 | Vinpocetine injection and preparation method thereof |
| CN102160853A (en) * | 2011-02-11 | 2011-08-24 | 方宝林 | Vinpocetine injection and preparation method thereof |
| CN102228428A (en) * | 2011-06-30 | 2011-11-02 | 武汉同源药业有限公司 | Large volume injection composition containing vinpocetine and preparation method thereof |
-
2011
- 2011-11-14 CN CN201110361192.5A patent/CN102716065B/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101991530A (en) * | 2009-08-28 | 2011-03-30 | 沈阳志鹰制药厂 | Vinpocetine containing high-capacity sodium chloride injection and preparation method thereof |
| CN101791310A (en) * | 2010-02-24 | 2010-08-04 | 王保明 | Vinpocetine medicine composition and preparation method thereof |
| CN102091030A (en) * | 2011-01-20 | 2011-06-15 | 罗军 | Vinpocetine injection and preparation method thereof |
| CN102160853A (en) * | 2011-02-11 | 2011-08-24 | 方宝林 | Vinpocetine injection and preparation method thereof |
| CN102228428A (en) * | 2011-06-30 | 2011-11-02 | 武汉同源药业有限公司 | Large volume injection composition containing vinpocetine and preparation method thereof |
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| CN102716065A (en) | 2012-10-10 |
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Denomination of invention: A vinpocetine injection and its preparation method Effective date of registration: 20230222 Granted publication date: 20140416 Pledgee: CITIC Bank Limited by Share Ltd. Zhengzhou branch Pledgor: HENAN RUNHONG PHARMACEUTICAL Co.,Ltd. Registration number: Y2023980033250 |
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Denomination of invention: A Changchun Xiting Injection and Its Preparation Method Granted publication date: 20140416 Pledgee: CITIC Bank Limited by Share Ltd. Zhengzhou branch Pledgor: HENAN RUNHONG PHARMACEUTICAL Co.,Ltd. Registration number: Y2024980003580 |
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