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Derivative of 10 - hydroxyl camptothecin, prepartion of liposome thereof, and preparation method

A technology of camptothecin and liposome, which is applied in the field of 10-hydroxycamptothecin derivatives, can solve the problems of lower total effective rate of curative effect and other problems

Inactive Publication Date: 2012-11-21
HUNAN KANGDU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And the total effective rate of curative effect is also greatly reduced, lower than 32%.

Method used

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  • Derivative of 10 - hydroxyl camptothecin, prepartion of liposome thereof, and preparation method
  • Derivative of 10 - hydroxyl camptothecin, prepartion of liposome thereof, and preparation method
  • Derivative of 10 - hydroxyl camptothecin, prepartion of liposome thereof, and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] The formula that present embodiment adopts is as follows:

[0087] Egg yolk lecithin 8mmol;

[0088] Methoxy polyethylene glycol 2000-hydrogenated soybean lecithin 2mmol;

[0089] Cholesterol 6mmol;

[0090] Octadecylamine 0.8mmol;

[0091] 10-O-(1-β-D-2,3,4,6-tetraacetylglucosyl)

[0092] Camptothecin ethyl ester 0.420g;

[0093] 0.150 g of a mixture of vitamin E and vitamin F in a weight ratio of 3:1;

[0094] tert-butanol and 0.01mol / L, pH5.0-6.5 phosphate buffer

[0095] 600ml of mixed solution with a volume ratio of 1:3;

[0096] 19.8 g of a mixture of glycine and low molecular weight dextran-40 in a weight ratio of 1:10.

[0097] The preparation steps refer to the foregoing, the difference is that the ester compound of 10-O-(1-β-D-2,3,4,6-tetraacetylglucosyl)camptothecin is changed to 10-O-(1-β- D-2,3,4,6-Tetraacetylglucosyl)camptothecin ethyl ester.

[0098] Pharmacodynamic verification experiment:

[0099] Select mice models of gastric cancer and head ...

Embodiment 2

[0114] The formula of this embodiment is as follows:

[0115] Egg yolk lecithin and hydrogenated soybean lecithin 2: 1 molar ratio mixture 10mmol;

[0116] Methoxy polyethylene glycol 2000-hydrogenated soybean lecithin 3mmol;

[0117] Cholesterol 8mmol;

[0118]Octadecylamine 1.0mmol;

[0119] 10-O-(1-β-D-2,3,4,6-tetraacetylglucosyl)

[0120] Camptothecin propyl ester 0.48g;

[0121] 0.170g of a mixture of vitamin E and vitamin F with a weight ratio of 3:1;

[0122] tert-butanol and 0.01mol / L, pH5.0-6.5 phosphate buffer

[0123] 700ml of mixed solution with a volume ratio of 1:3;

[0124] 22.40 g of a mixture of glycine and low molecular weight dextran-40 in a weight ratio of 1:10.

[0125] The preparation method refers to the aforementioned, the difference is that the ester compound of 10-O-(1-β-D-2,3,4,6-tetraacetylglucosyl)camptothecin is changed to 10-O-(1-β- D-2,3,4,6-Tetraacetylglucosyl)camptothecin propyl ester.

[0126] The pharmacodynamic verification is as f...

Embodiment 3

[0142] The formula of this embodiment is as follows:

[0143] Egg yolk lecithin and hydrogenated soybean lecithin 1:1 molar ratio mixture 12mmol;

[0144] Methoxy polyethylene glycol 2000-hydrogenated soybean lecithin 4mmol;

[0145] Cholesterol 10mmol;

[0146] Octadecylamine 1.2mmol;

[0147] 10-O-(1-β-D-2,3,4,6-tetraacetylglucosyl)

[0148] Camptothecin benzyl ester 0.520g;

[0149] 0.180g of a mixture of vitamin E and vitamin F with a weight ratio of 3:1;

[0150] tert-butanol and 0.01mol / L, pH5.0-6.5 phosphate buffer

[0151] 800ml of mixed solution with a volume ratio of 1:3;

[0152] 26.40 g of a mixture of glycine and low molecular weight dextran-40 in a weight ratio of 1:10.

[0153] The preparation method refers to the aforementioned, the difference is that the ester compound of 10-O-(1-β-D-2,3,4,6-tetraacetylglucosyl)camptothecin is changed to 10-O-(1-β- D-2,3,4,6-Tetraacetylglucosyl)camptothecin benzyl ester.

[0154] The pharmacodynamic verification is as...

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Abstract

This invention relates to 10-hydroxycamptothecine derivatives, their liposome preparations, and their preparation method. The 10-hydroxycamptothecine derivatives are shown in formula 1, wherein the R can chose form -CH3, C2H5. This invention also provides a method for preparing the 10-hydroxycamptothecine derivatives, and the liposome enveloping the ester compounds of the 10-hydroxycamptothecine derivatives, and their preparation method. The 10-hydroxycamptothecine derivatives and their liposome preparations can be used to treat tumors.

Description

technical field [0001] The invention relates to a 10-hydroxycamptothecin derivative, its liposome preparation and a preparation method. Background technique [0002] The pharmacological action of 10-hydroxycamptothecin is similar to that of camptothecin. It has a broad anti-tumor spectrum and less toxicity than camptothecin. Experimental studies have proved that 10-hydroxycamptothecin has a slight killing effect on tumor cells, and its clinical use is limited. However, studies in recent years have found that its anti-tumor effect is mainly through the inhibition of DNA topoisomerase I, so that DNA cannot be replicated, resulting in irreversible damage to the DNA chain, resulting in the death of tumor cells. This outstanding advantage makes it gain clinical attention. At the same time, it also has an outstanding advantage that it has no cross-resistance with commonly used anti-tumor drugs. The above are the advantages of this drug. However, 10-hydroxycamptothecin has extr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/00A61K9/127A61K31/706A61P35/00C07D491/22
Inventor 蔡海德
Owner HUNAN KANGDU PHARMA