Stable liquid medicinal composition

Abstract

The invention relates to a medicinal composition. The composition has high stability, is resistant to strict high-temperature sterilization, and has high light stability. An additive is reduced greatly in comparison to the conventional product of the same type, production is convenient to realize, and cost is reduced.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a liquid preparation containing vinpocetine and a preparation method thereof. Background technique [0002] Vinpocetine, the chemical name is ethyl(13as, 13bs)-13a-ethyl-2,3,5,6-13a,13b hexahydro-1H-indole[3,2,1-de] Pyridine[3,2,1-ij][1,5]naphthalene-12-carboxylic acid, the molecular formula is: C 22 h 26 N 2 o 2 , the molecular weight is 350.5, and the structural formula is: [0003] [0004] Vinpocetine has multiple effects and can improve brain metabolism, blood flow and hemorheological properties. [0005] Neuroprotective effect: Vinpocetine can alleviate the cytotoxicity induced by excitatory amino acids, inhibit voltage-dependent sodium ion channels and calcium ion channels, NMDA and AMPA receptors, and enhance the neuroprotective effect of adenosine. [0006] Promote brain metabolism: Vinpocetine can increase the intake and consumption of gluco...

AI Technical Summary

Problems solved by technology

[0011] (1) Poor water solubility. Vinpocetine is almost insoluble in water. Poor water solubility brings challenges to preparation research. If it is to be made into liquid preparations or injections, difficulties must be overcome so that the drug can be completely dissolved to meet the requirements for injection;

[0012] (2) The aqueous solution of vinpocetine is unstable at high temperature, and it is easy to degrade to produce impurities, especially in the case of heating in the solution state, the degradation can be accelerated. The main performance is the hydrolysis of the double bond in the molecule to generate ethyl vincamine. Therefore, in the European Pharmacopoeia In the quality standards of Vinpocetine and the British Pharmacopoeia, it is clear that there are four known impurities related to Vinpocetine, and the limits of other unknown impurities are also specified

[0013] (3) The vinpocetine aqueous solution is unstable to light. Under light conditions, the vinpocetine aqueous solution turns yellow, and vinpocetine degrades to produce impurities, which affects the safety of the product. Currently, vinpocetine injections on the market are in brown color. Ampoule packaging

[0018] According to the existing knowledge, the production process of Vinpocetine Injection does not include a high-temperature sterilization step, and there is no research report on the production of Vinpocetine Injection using an overkill sterilization process

In recent years, the serious adverse accidents of injections that have occurred frequently are mostly due to the instability of the drug, resulting in a low level of sterility assurance in the production process, resulting in product safety issues

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