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Nano-preparation and preparation method of an anticancer drug composition and its application in the treatment of malignant tumors

A nano preparation and composition technology, applied in the field of pharmaceutical preparations, can solve the problems of large toxic and side effects, poor water solubility, short half-life, etc., and achieve the effects of reducing toxic and side effects, reducing IC50, and improving blocking effect.

Active Publication Date: 2019-11-05
SICHUAN PROVINCIAL PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to overcome the above-mentioned shortcomings of poor water solubility, short half-life and large toxic and side effects in the existing anticancer drug dosage forms, and provide a nano-preparation of anticancer drug composition

Method used

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  • Nano-preparation and preparation method of an anticancer drug composition and its application in the treatment of malignant tumors
  • Nano-preparation and preparation method of an anticancer drug composition and its application in the treatment of malignant tumors
  • Nano-preparation and preparation method of an anticancer drug composition and its application in the treatment of malignant tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 A nano-preparation A of an anticancer drug composition

[0037] Contains 0.4g paclitaxel, 2g HS-ASA, 10g mPEG-PCL, 1g polyvinyl alcohol and 1000g water.

[0038] The preparation method of above-mentioned nano preparation, comprises the following steps:

[0039] First synthesize aspirin derivatives that release hydrogen sulfide:

[0040]

[0041] 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 (HS-ASA).

[0042] Dissolve 1g of polyvinyl alcohol in 1000g of water and set aside.

[0043] Mix 0.4g paclitaxel, 2g HS-ASA and 10g mPEG-PCL evenly, add 50g dichloromethane to dissolve, vortex for 2min to completely dissolve, then vacuum rot...

Embodiment 2

[0044] Example 2 A nano-preparation B of an anticancer drug composition

[0045] Contains 0.4g paclitaxel, 1g HS-ASA, 20g mPEG-PCL, 10g polyvinyl alcohol and 1000g water.

[0046] The preparation method of above-mentioned nano preparation, comprises the following steps:

[0047] First synthesize aspirin derivatives that release hydrogen sulfide:

[0048]

[0049] 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 (HS-ASA).

[0050] Dissolve 10g of polyvinyl alcohol in 1000g of water and set aside.

[0051] Mix 0.4g paclitaxel, 1g HS-ASA and 20g mPEG-PCL evenly, add 45g dichloromethane to dissolve, vortex for 2min to completely dissolve, then vacuum ...

Embodiment 3

[0052] Example 3 A nano-preparation C of an anticancer drug composition

[0053] Contains 0.2g paclitaxel, 1.5g HS-ASA, 30g mPEG-PCL, 5g polyvinyl alcohol and 4000g water.

[0054] The preparation method of above-mentioned nano preparation, comprises the following steps:

[0055] First synthesize aspirin derivatives that release hydrogen sulfide:

[0056]

[0057] 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 (HS-ASA).

[0058] Dissolve 5g of polyvinyl alcohol in 4000g of water and set aside.

[0059] Mix 0.2g paclitaxel, 1.5g HS-ASA and 30g mPEG-PCL evenly, add 40g dichloromethane to dissolve, vortex for 3min to dissolve completely, then vacuum...

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Abstract

The invention discloses an anticancer drug composition nano-preparation which comprises PTX (paclitaxel), an aspirin derivative (HS-ASA) capable of releasing hydrogen sulphide in a formula (I), methoxy polyethylene glycol-poly-epsilon-caprolactone, polyvinyl alcohol and water as shown in the specification. In combination with PTX and HS-ASA, the invention can improve the anti-cancer effect and reduce the dose of PTX, thereby reduce the side effects of PTX, improve the treatment index and compliance of a patient. The invention further provides the preparation of a nano formulation of the anticancer drugs composition which controls the release of the drug in the microbial environment of the tumor cell and prevents the drug from being released and degraded in a large amount in blood circulation and greatly improves stability of drugs and tumor targeting.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nano-preparation and preparation method of an anticancer pharmaceutical composition and its application in treating malignant tumors. Background technique [0002] Cancer is one of the major diseases that threaten human health. It has become the first cause of death for human beings, and its incidence continues to rise. Finding high-efficiency, low-toxic anticancer drugs and new preparations to completely conquer cancer is one of the important research topics in the world medical community. [0003] As the first-line chemotherapy drug for advanced non-small cell lung cancer, paclitaxel has shown encouraging curative effect in the treatment of breast cancer, leukemia, gastrointestinal cancer and vascular restenosis after interventional therapy. At present, there are mainly three preparations of paclitaxel used clinically in my country: one is polyoxyethylene castor oi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/616A61K9/107A61K47/34A61K47/32A61P35/00A61K31/337A61K9/14
CPCA61K9/1075A61K9/146A61K31/337A61K31/616A61K47/32A61K47/34B82Y5/00A61K2300/00
Inventor 蔡璐璐闫峻峰余继英王岩
Owner SICHUAN PROVINCIAL PEOPLES HOSPITAL
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