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Anticancer pharmaceutical composition, preparation thereof and preparing method

An anti-cancer drug and composition technology, applied in the field of anti-tumor drug research, to achieve the effects of reducing toxic side effects, improving bioavailability and druggability, and reducing IC50

Active Publication Date: 2017-04-26
SICHUAN PROVINCIAL PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

NSAIDs have been widely used in the treatment of colds, fever, inflammation, etc., and have shown less toxic side effects, but their side effects on the upper gastrointestinal tract, such as gastrointestinal discomfort and ulcers, are still a major problem in clinical application

Method used

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  • Anticancer pharmaceutical composition, preparation thereof and preparing method
  • Anticancer pharmaceutical composition, preparation thereof and preparing method
  • Anticancer pharmaceutical composition, preparation thereof and preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of Anticancer Drug Composition A

[0036] Synthesis of aspirin derivatives that release hydrogen sulfide:

[0037]

[0038] As shown in the above reaction formula (a), 5.6 grams of compound 1 and 5.8 grams of compound 2 were added to 240 milliliters of dichloromethane, and then 0.25 grams of DMAP was added, stirred and reacted at room temperature for 6 hours, and the solvent was removed by vacuum rotary evaporation , followed by purification by column chromatography to obtain 10.9 g of compound 3.

[0039] The anticancer drug composition A is obtained by mixing paclitaxel with the compound 3 synthesized above in a weight ratio of 1:5.

Embodiment 2

[0040] Example 2 Preparation of Anticancer Drug Composition B

[0041] Synthesis of aspirin derivatives that release hydrogen sulfide:

[0042]

[0043] As shown in the above reaction formula (a), 10.2 grams of compound 1 and 9.8 grams of compound 2 were added to 420 milliliters of dichloromethane, and then 0.48 grams of DMAP was added, stirred and reacted at room temperature for 6 hours, and the solvent was removed by vacuum rotary evaporation , followed by purification by column chromatography to obtain 18.6 g of compound 3.

[0044] The anticancer drug composition B is obtained by mixing paclitaxel with the compound 3 synthesized above in a weight ratio of 1:1.

Embodiment 3

[0045] Example 3 Preparation of Anticancer Drug Composition C

[0046] Synthesis of aspirin derivatives that release hydrogen sulfide:

[0047]

[0048] As shown in the above reaction formula (a), 7.6 grams of compound 1 and 7.2 grams of compound 2 were added to 360 milliliters of dichloromethane, and then 0.36 grams of DMAP was added, stirred and reacted at room temperature for 6 hours, and the solvent was removed by vacuum rotary evaporation , followed by purification by column chromatography to obtain 15.4 g of compound 3.

[0049] The anticancer drug composition C is obtained by mixing paclitaxel with the compound 3 synthesized above at a weight ratio of 1:10.

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Abstract

The invention discloses an anticancer pharmaceutical composition and a preparation thereof. The anticancer pharmaceutical composition comprises paclitaxel (PTX) and aspirin derivatives (HS-ASP) capable of releasing hydrogen sulfide, wherein the structure of the HS-ASP is as shown in formula (I). The anticancer pharmaceutical composition has the advantages that the PTX and the HS-APS which are different in action mechanism are combined to increase the curative effect on cancer in a synergic manner, the dosage of the PTX can be reduced at the same time to reduce the toxic and side effects of the PTX, the therapeutic index of patients during clinical application can be increased, and the compliance of the patients is improved. The invention further provides a preparing method of the preparation. A solvent is used to dissolve the PTX and the HS-ASP into injection water to prepare the preparation applicable to intravenous injection or instillation, and the bioavailability of medicine is increased greatly.

Description

technical field [0001] The invention relates to the field of antitumor drug research, in particular to an anticancer drug composition and its formulation and preparation method. Background technique [0002] Paclitaxel (PTX), as the first-line chemotherapy drug for advanced non-small cell lung cancer, has shown encouraging curative effect in the treatment of breast cancer, leukemia, gastrointestinal cancer and vascular restenosis after interventional therapy. At present, there are three main preparations of paclitaxel used clinically in my country: one is polyoxyethylene castor oil-absolute ethanol 1:1 intravenous injection (such as Taxol), which can increase the solubility of paclitaxel, but polyoxyethylene castor oil Ethylene castor oil has been shown to cause severe allergic reactions, bone marrow suppression, neurotoxicity, cardiovascular toxicity, liver and kidney toxicity, etc., and cumbersome anti-allergic treatment is required before administration; another paclitaxel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/625A61K31/337A61K9/08A61K47/26A61K47/44A61K47/10A61P35/00
Inventor 蔡璐璐
Owner SICHUAN PROVINCIAL PEOPLES HOSPITAL
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