CN103919719B - A kind of preparation method of Vinpocetine injection - Google Patents
A kind of preparation method of Vinpocetine injection Download PDFInfo
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- CN103919719B CN103919719B CN201410149121.2A CN201410149121A CN103919719B CN 103919719 B CN103919719 B CN 103919719B CN 201410149121 A CN201410149121 A CN 201410149121A CN 103919719 B CN103919719 B CN 103919719B
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Abstract
The invention belongs to technical field of medicine, be specifically related to a kind of preparation method of Vinpocetine injection.The method comprises the following steps: get water for injection, adds antioxidant A, vinpocetine successively, stirring and evenly mixing, slowly adding antioxidant synergist stirring makes vinpocetine dissolve completely, add antioxidant B, physically stable agent more successively, stirring and dissolving is complete, injects by the nearly full dose of water; Adjust pH is 3.0 ~ 3.5, adds water for injection to 1000ml, stirring and evenly mixing, and absorption, filtration, fill nitrogen embedding, sterilizing.The stable content of vinpocetine in the injection that the present invention obtains, related substance is not increased significantly, and occurs, have the advantages such as effect duration length, steady quality in storage process without denaturalization phenomenon.
Description
Technical field
The invention belongs to technical field of medicine, be specifically related to a kind of preparation method of Vinpocetine injection.
Background technology
Herba Catharanthi Rosei (Vincamajor, Vineaminor) is the green cover plant of length of common similar liana, is distributed in the areas such as middle southern Europe, has the applicating history of nearly 2000 years as medicinal plants.Vinpocetine is a kind of natural drug obtained from Herba Catharanthi Rosei, and belong to indoles alkaloid, chemical name is: ethyl (13as, 13bs)-13a-ethyl-2,3,5,6-13a, 13b six hydrogen-1H-indole [3,2,1-de] pyridine [3,2,1-ij] [1,5]-benzodiazine-12-carboxylic acid, is widely used in treatment and the prevention of ischemic cerebrovascular.First vinpocetine is succeeded in developing by GedeonRichter company of Hungary, and rear mandate in the world Duo Jia drugmaker is produced.This medicine is not only effective to the high blood viscosity of prevention and therapy cerebral arteriosclerosis, cerebral ischemia and hemorrhagic apoplexy sequela and hypertension, coronary heart disease, and also has important value to the Pathophysiology of research cerebrovascular disease.
Vinpocetine injection is in production and storage process, easy oxidative degradation, produce various catabolite, and adopt 121 DEG C of excessive sterilizings, the appearance of meeting accelerated degradation product, therefore in listing injection, producer often adds antioxidant to prevent the increase of vinpocetine related substance, but single antioxidant effect is bad, the easy variable color of injection long term storage.When the adjuvant of Vinpocetine injection is too much, through 121 DEG C of excessive sterilizings, during placement, there will be white point, cause visible foreign matters defective.
Therefore, need that a kind of production process is simple and easy to control, standing time long and stay-in-grade Vinpocetine injection.
Summary of the invention
The invention provides and grow and the preparation method of stay-in-grade Vinpocetine injection a kind of standing time.
For achieving the above object, the present invention is by the following technical solutions:
A kind of preparation method of Vinpocetine injection, comprise the following steps: the water for injection getting 60-70ml, be cooled to less than 50 DEG C, deoxygenation, adds 0.2-0.6g antioxidant A, 5-10g vinpocetine, stirring and evenly mixing successively, adding the stirring of 1-3g antioxidant synergist makes vinpocetine dissolve completely, add the agent of 1-3g antioxidant B, 30-60g physically stable more successively, stirring and dissolving is complete, injects by the nearly full dose of water; Adding pH value regulator adjust pH is 3.0 ~ 3.5, adds water for injection to 1000ml, stirring and evenly mixing, and absorption, filtration, fill nitrogen embedding, sterilizing.
Described antioxidant A is vitamin C, and described antioxidant B is sodium pyrosulfite, and antioxidant synergist is L-TARTARIC ACID, and physically stable agent is sorbitol, and pH value regulator is 10%L-tartaric acid solution.
Found by great many of experiments when the present invention studies, single antioxidant is not fine to the antioxidant effect of vinpocetine.The present invention changes original mode and adopts two kinds of special antioxidant to combine, and add antioxidant synergist, it can strengthen the usefulness of antioxidant, particularly strengthens the effect of the antioxidant of retardance automatic oxidation reaction chain reaction, also with some metal ion, pseudo-complexing can occur.In order to prevent the oxidation of vinpocetine, guarantee vinpocetine injection stablizing within the longer time, the amount of antioxidant A and B improves under the condition of safe and reasonable in the present compositions.Simultaneously antioxidant A and antioxidant synergist select the preparation being also conducive to said composition, make layoutprocedure simple.In layoutprocedure, regulate pH with 10wt%L-tartaric acid solution, define pH scope, ensure that the pH of finished product stablizes, ensure the quality of finished product.
Vinpocetine injection adopts 121 DEG C of excessive sterilizings, and in prior art, physically stable agent consumption is crossed conference and caused particulate matter to increase, and visible foreign matters is also defective, therefore decreases the consumption of physically stable agent in the present invention.
Vascular stimulation tests as intravenous injection and intramuscular dose Drug safety assessment one of main test item and be widely used, this product administering mode adopts intravenous drip, can not intramuscular injection, not diluted can not use by vein, the administration concentration of intravenous drip of the present invention more than 0.06mg/ml, therefore must not eliminate vascular stimulation regulator in the present invention.
The present invention can be used for 2ml:10mg, 2ml:20mg, 5ml:30mg equal-specification, is not limited only to this three kinds of specifications.
Adopt through preferred compositions ratio and technique, the steady quality of the Vinpocetine injection that the present invention obtains, national standard YBHO3852013 is adopted to test, this standard is that I independently drafts foundation at company, and relative domestic standard and the former target level of product quality of grinding of import have significantly lifting from different.Through long-term reserved sample observing, the stable content of vinpocetine in obtained injection, related substance is not increased significantly, and occurs, have the advantages such as effect duration length, steady quality in storage process without denaturalization phenomenon.
Detailed description of the invention
Embodiment 1 (specification: 2ml:10mg)
Vinpocetine injection (10000ml) consists of: vinpocetine 50g, Catergen g, sodium pyrosulfite 10g, L-TARTARIC ACID 30g, sorbitol 600g, the water for injection of appropriate 10%L-tartaric acid solution and surplus.
Its preparation method is: the water for injection getting 60ml, be cooled to less than 50 DEG C, deoxygenation, add Catergen g, vinpocetine 50g successively, stirring and evenly mixing, slowly adds L-TARTARIC ACID 30g stirring and vinpocetine is dissolved completely, then add sodium pyrosulfite 10g, sorbitol 600g successively, and it is complete to make it stirring and dissolving, injects by the nearly full dose of water; The pH value regulating medicinal liquid with 10wt%L-tartaric acid solution is 3.0 ~ 3.5, adds water for injection to full dose, stirring and evenly mixing, adds the medicinal charcoal absorption accounting for amount of liquid medicine 0.03% and stirs, filter, fill nitrogen embedding, sterilizing.
Embodiment 2 (specification: 2ml:20mg)
Vinpocetine injection (10000ml) consists of: vinpocetine 100g, vitamin C 5g, sodium pyrosulfite 10g, L-TARTARIC ACID 30g, sorbitol 600g, the water for injection of appropriate 10%L-tartaric acid solution and surplus.
Its preparation method is: the water for injection getting 70ml, be cooled to less than 50 DEG C, deoxygenation, add vitamin C 5g, vinpocetine 100g successively, stirring and evenly mixing, slowly adds L-TARTARIC ACID 30g stirring and vinpocetine is dissolved completely, then add sodium pyrosulfite 10g, sorbitol 600g successively, and it is complete to make it stirring and dissolving, injects by the nearly full dose of water; The pH value regulating medicinal liquid with 10wt%L-tartaric acid solution is 3.0 ~ 3.5, adds water for injection to full dose, stirring and evenly mixing, adds the medicinal charcoal absorption accounting for amount of liquid medicine 0.03% and stirs, filter, fill nitrogen embedding, sterilizing.
Embodiment 3 (specification: 5ml:30mg)
Vinpocetine injection (10000ml) consists of: vinpocetine 60g, Catergen g, sodium pyrosulfite 10g, L-TARTARIC ACID 30g, sorbitol 600g, the water for injection of appropriate 10%L-tartaric acid solution and surplus.
Its preparation method is: the water for injection getting 65ml, be cooled to less than 50 DEG C, deoxygenation, add Catergen g, vinpocetine 50g successively, stirring and evenly mixing, slowly adds L-TARTARIC ACID 30g stirring and vinpocetine is dissolved completely, then add sodium pyrosulfite 10g, sorbitol 600g successively, and it is complete to make it stirring and dissolving, injects by the nearly full dose of water; The pH value regulating medicinal liquid with 10wt%L-tartaric acid solution is 3.0 ~ 3.5, adds water for injection to full dose, stirring and evenly mixing, adds the medicinal charcoal absorption accounting for amount of liquid medicine 0.03% and stirs, filter, fill nitrogen embedding, sterilizing.
Through keeping sample stability observing, the constant product quality that the present invention obtains, occur in storage process without denaturalization phenomenon, product quality all meets the regulation under the normal term of the Vinpocetine injection that state food pharmaceuticals administration general bureau issues, and product is reliable and stable.
Stability data
Accelerated test
1, the Vinpocetine injection packaging that embodiment 1 is obtained: low borosilicate glass ampoule
Investigation condition: temperature 40 ± 2 DEG C, relative humidity 75 ± 5%; Result is as following table 1:
2, the Vinpocetine injection packaging that embodiment 2 is obtained: low borosilicate glass ampoule
Investigation condition: temperature 40 ± 2 DEG C, relative humidity 75 ± 5%; Result is as following table 2:
3, the Vinpocetine injection packaging that embodiment 3 is obtained: low borosilicate glass ampoule
Investigation condition: temperature 40 ± 2 DEG C, relative humidity 75 ± 5%; Result is as following table 3:
Found out by above test, in long-term stability experiment, the content of the effective ingredient vinpocetine in the injection that the present invention obtains is basicly stable, does not obviously decline, and related substance increasing degree is little, and character is clarified, and has good stability.
Claims (1)
1. the preparation method of a Vinpocetine injection, it is characterized in that, preparation method is: the water for injection getting 60ml, is cooled to less than 50 DEG C, deoxygenation, add Catergen g, vinpocetine 50g successively, stirring and evenly mixing, slowly adds L-TARTARIC ACID 30g stirring and vinpocetine is dissolved completely, then add sodium pyrosulfite 10g, sorbitol 600g successively, and it is complete to make it stirring and dissolving, injects by the nearly full dose of water; The pH value regulating medicinal liquid with 10wt%L-tartaric acid solution is 3.0 ~ 3.5, adds water for injection to full dose, stirring and evenly mixing, adds the medicinal charcoal absorption accounting for amount of liquid medicine 0.03% and stirs, filter, fill nitrogen embedding, sterilizing.
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| CN201410149121.2A CN103919719B (en) | 2014-04-15 | 2014-04-15 | A kind of preparation method of Vinpocetine injection |
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| CN201410149121.2A CN103919719B (en) | 2014-04-15 | 2014-04-15 | A kind of preparation method of Vinpocetine injection |
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| CN103919719B true CN103919719B (en) | 2016-02-03 |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102113994A (en) * | 2010-01-04 | 2011-07-06 | 长春富春制药有限公司 | Medicament for treating cerebral blood-vessel dilate and preparation method thereof |
| CN102716066A (en) * | 2011-11-14 | 2012-10-10 | 河南润弘制药股份有限公司 | Vinpocetine injection and preparation method thereof |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102113994A (en) * | 2010-01-04 | 2011-07-06 | 长春富春制药有限公司 | Medicament for treating cerebral blood-vessel dilate and preparation method thereof |
| CN102716066A (en) * | 2011-11-14 | 2012-10-10 | 河南润弘制药股份有限公司 | Vinpocetine injection and preparation method thereof |
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Address after: 462000 No. 6 Renmin Middle Road, Zhengzhou, Henan, Xinzheng Applicant after: Suicheng Pharmaceutical Co., Ltd. Address before: 462000 No. 6 Renmin Middle Road, Zhengzhou, Henan, Xinzheng Applicant before: Tianjin Pharmaceutical Group Xinzheng Co., Ltd. |
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Inventor after: Li Junxia Inventor after: Cheng Yongke Inventor after: Bai Yanhe Inventor before: Cheng Yongke Inventor before: Li Junxia Inventor before: Bai Yanhe |
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