Stable liquid medicinal composition

A light-stable, injection technology, applied in the fields of drug combination, drug delivery, blood diseases, etc., can solve the problems of product safety, high temperature instability, poor water solubility, etc., to improve product quality, simplify prescription composition, reduce The effect of production costs

Active Publication Date: 2013-12-11
吉瑞医药(中国)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Stable liquid medicinal composition
  • Stable liquid medicinal composition
  • Stable liquid medicinal composition

Examples

Experimental program
Comparison scheme
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preparation example Construction

[0039] Preparation of samples for comparative study: Take 1400ml of water for injection, add tartaric acid to adjust the pH to 2.0, add 10g of vinpocetine, stir to dissolve, add 1mol / l NaOH aqueous solution to adjust the pH to 3.0-4.0, add water to a sufficient amount, add injection-grade Activated carbon (0.1%, w / v) was incubated and stirred at 60°C for 30 minutes, filtered, filled in colorless transparent glass ampoules, 2ml each, and sterilized at 121°C for 15 minutes.

[0040] Separately take lactic acid and phosphoric acid to prepare samples in the same way as above, and set aside.

Embodiment 1

[0042] prescription:

[0043] Vinpocetine 10g

[0044] 1mol / l hydrochloric acid 200ml

[0045] Water was added to 2000ml.

[0046] Preparation method: add hydrochloric acid into water and stir evenly to obtain a hydrochloric acid solution with a volume of about 70% of the prepared volume, add vinpocetine, stir to dissolve it completely, add 1mol / l NaOH aqueous solution to adjust the pH to 3.0-4.0, and replenish Add water to a sufficient amount, add injection-grade activated carbon (0.1%, w / v), insulate and stir at 60°C for 30 minutes, filter, fill in colorless transparent glass ampoules, 2ml each, and sterilize at 121°C for 15 minutes. That is, Vinpocetine Injection.

Embodiment 2

[0048] prescription:

[0049] Vinpocetine 10g

[0050] 1mol / l hydrochloric acid 160ml

[0051] Water was added to 2000ml.

[0052] Preparation method: add hydrochloric acid into water and stir evenly to obtain a hydrochloric acid solution with a volume of about 70% of the prepared volume, add vinpocetine, stir to dissolve it completely, add 1mol / l NaOH aqueous solution to adjust the pH to 3.0-4.0, and replenish Add water to a sufficient amount, add injection-grade activated carbon (0.1%, w / v), insulate and stir at 60°C for 30 minutes, filter, fill in colorless transparent glass ampoules, 2ml each, and sterilize at 121°C for 15 minutes. That is, Vinpocetine Injection.

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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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4375A61K47/04A61K9/08A61P9/10A61P9/00A61P25/00A61P7/04
Inventor 常建晖林金平
Owner 吉瑞医药(中国)有限公司
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