Vinpocetine injection and preparation method thereof

Abstract

The invention relates to a vinpocetine injection and a production method thereof. The vinpocetine injection comprises 10 to 20 parts of vinpocetine, 0.1 to 0.45 parts of ascorbic acid, 1 to 5 parts of one or more antioxidants, 6 to 15 parts of one or more cosolvents and 2000 parts of water. The preparation method comprises the following steps of 1, filtering 80% of injection water to remove oxygen, heating to a temperature of 40 to 50 DEG C, adding ascorbic acid, the one or more cosolvents and the one or more antioxidants into the injection water, and stirring for complete dissolution, 2, adding vinpocetine into the solution obtained by the step 1, stirring for full dissolution, supplying enough injection water, and carrying out stirring adsorption by 0.3% of active carbon, and 3, carrying out disinfection at a temperature of 121 DEG C for 15 minutes, and carrying out filling under nitrogen atmosphere. The vinpocetine injection obtained by the preparation method can be subjected to sterilization at a temperature of 121 DEG C for 15 minutes. A result of detection shows that impurity content is not improved obviously and thus the vinpocetine injection is stable and can be used for industrial production. Compared with the original vinpocetine injection, the vinpocetine injection obtained by the preparation method can be subjected to overkill sterilization at a temperature of 121 DEG C for 15 minutes so that a sterility assurance level of the vinpocetine injection can be ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, relates to a vinpocetine injection, and also relates to a preparation method of the vinpocetine injection. Background technique [0002] Vinpocetine, whose chemical name is ethyl(13as,13bs)-13a-ethyl-2,3,5,6-13a,13bhexahydro-1H-indole[3,2,1-de]pyridine[ 3,2,1-ij][1,5]naphthalene-12-carboxylic acid. Molecular formula: C 22 h 26 N 2 o 2 , molecular weight: 350.46. Vinpocetine is an indole alkaloid. A large number of scientific studies have confirmed that it can selectively improve the blood circulation of the brain, promote the energy metabolism of the brain, regulate the function of the neurotransmitter system, and protect the brain from deficiency in many aspects. The damage caused by blood hypoxia is especially suitable for the treatment of cardiovascular and cerebrovascular diseases, and it also has a significant effect on brain diseases caused by aging. Clinically, it is mainl...

AI Technical Summary

Problems solved by technology

[0004] Vinpocetine injection is easily oxidatively degraded during production and storage, producing various degradation products. Currently, there are four main degradation products of vinpocetine, and over-sterilization at 121°C will accelerate the degradation of the degradation products. Appear

At present, too many antioxidants are often added to vinpocetine injections on the market. Although it can effectively ensure that vinpocetine will not be degraded, it is also easy to oxidize and degrade under high temperature sterilization conditions, resulting in more degradation products and affecting the clarification of the solution. Spend

In addition, vinpocetine injection is prone to produce insoluble particles during long-term storage, which affects the safety of the drug. The formation of insoluble particles shows the instability of the product caused by prolonged storage, which can cause two types of hazards. Insoluble particles enter the patient's body Clogging of veins in veins and clogging of filters when administering IV medications

[0005] Since the injection needs to use water for injection in the production process, although it has gone through the process of deoxygenation and nitrogen filling, the presence of dissolved oxygen in the water for injection cannot be ruled out.

Moreover, the final sterilization process of the injection needs to be sterilized at 121°C for 15 minutes, and the high heat condition will aggravate the rate of the oxidation reaction.

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