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Vinorelbine injection and preparation method thereof

A technology of vinorelbine and injection, which is applied in the direction of medical formula, medical preparations containing active ingredients, drug combinations, etc. It can solve the problems of packaging, vinorelbine drug instability, and the inability to reduce vascular irritation, and achieve Reduce irritation and side effects, improve stability, and increase fat solubility

Active Publication Date: 2018-11-02
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In oil-in-water emulsions, lipophilic drugs tend to dissolve in the oil phase and be encapsulated and / or encapsulated by oil droplets, highly water-soluble drugs like vinca alkaloids do not work well in conventional emulsion oil droplets Even if a large amount of excipients are added, it is difficult to be effectively wrapped in the oil phase or interface film, so that the purpose of reducing the irritation to blood vessels and improving the curative effect cannot be achieved.
In addition, vinorelbine is prone to oxidative degradation, and the instability of vinorelbine is also an important problem to be solved in its clinical application.

Method used

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  • Vinorelbine injection and preparation method thereof
  • Vinorelbine injection and preparation method thereof
  • Vinorelbine injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Preparation of vinorelbine phospholipid complex (I)

[0025] Take 10g of vinorelbine bitartrate and 18g of soybean lecithin, add them to ethyl acetate, heat and reflux at 40-50°C for 2-3 hours, remove ethyl acetate by rotary evaporation, and place in a vacuum dryer or freeze dryer Dry in the medium to obtain vinorelbine phospholipid complex (I).

Embodiment 2

[0027] Preparation of vinorelbine phospholipid complex (II)

[0028] Take 10g of vinorelbine bitartrate and 18g of soybean lecithin, add them to acetone, heat and reflux at 40-50°C for 2-3 hours, remove the acetone by rotary evaporation, and dry in a vacuum dryer or a freeze dryer. Obtain vinorelbine phospholipid complex (II).

Embodiment 3

[0030] Preparation of vinorelbine phospholipid complex (III)

[0031] Take 10g of vinorelbine bitartrate and 18g of soybean lecithin, add them to ethanol, heat and reflux at 40-50°C for 2-3 hours, remove the ethanol by rotary evaporation, and dry in a vacuum dryer or a freeze dryer. Obtain vinorelbine phospholipid complex (III).

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Abstract

The invention discloses vinorelbine injection and a preparation method thereof, and specifically relates to the vinorelbine injection for intravenous injection. The injection is prepared from vinorelbine phospholipid complex, beta-cyclodextrin, an isoosmotic adjusting agent, a pH modifier and injection water, wherein the beta-cyclodextrin and the vinorelbine phospholipid complex form an inclusioncompound; the irritation and toxic side effects of vinorelbine to blood vessels are effectively reduced; in addition, the vinorelbine injection has good stability and is suitable for clinical application.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an antitumor pharmaceutical preparation vinorelbine injection and a preparation method thereof. Background technique [0002] The alkaloids and their derivatives isolated from the plant Vinca alkaloids are commonly called "vinca alkaloids". Vinca alkaloids are highly cytotoxic drugs that destroy microtubules, inhibit cell division and induce cell apoptosis. It has proven effective as a first-line treatment for many types of lymphoma, leukemia and other cancers. Vincristine and vinblastine consist of a vinblastine core moiety linked to vinblastine, and their structural difference lies in a substitution in the vinblastine group. Later, vinorelbine with an 8-membered rather than 9-membered vinblastine nucleus was prepared using a new synthetic method, and vinorelbine is usually in the form of tartrate, namely vinorelbine bitartrate or vinorelbine tartrate. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/475A61P35/00
CPCA61K9/0019A61K9/08A61K31/475A61K36/24
Inventor 孙运栋曹健丁丹丹蔡超许春敏
Owner JIANGSU HANSOH PHARMA CO LTD