Paclitaxel/multialkene paclitaxel liposome composite medicine and preparation method thereof

A liposome and drug technology, applied in the directions of liposome delivery, drug combination, pharmaceutical formulation, etc., can solve problems such as side effects, neutropenia, tumor cell death, etc. Exponentially high effect

Inactive Publication Date: 2010-02-03
HUNAN KANGDU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Paclitaxel or docetaxel is a broad-spectrum effective anticancer drug, which can act on the microtubule / tubulin system of tumor cells, promote the assembly of tubulin into microtubules, but at the same time inhibit the depolymerization of microtubules, resulting in the breakdown of microtubule bundles. Abnormal alignment, formation of stellate bodies, disabling spindle function, leading to tumor cell death
[0003] However, in the prior art, paclitaxel or docetaxel preparations are common injections, and 47% of people have decreased blood neutrophils after using this type of drug, and 62% of people have decreased blood neutrophils after using this type of drug. Systemic toxicity and limb numbness, side effects on the liver, skin, and digestive system are common and obvious
In recent years, a large number of invention patents of liposomes, biodegradable polymer nanospheres, and cyclodextrin-containing liposome-combined preparations have appeared, which has significantly improved the curative effect of the drug and alleviated side effects. However, There are still side effects caused by liposome material and drug itself peroxidation in vivo and liposome material oxidation in vitro
There are also nanospheres, liposomes, and cyclodextrins containing drug leakage and sudden release in the body to produce instant toxic and side effects, which endanger the physical and mental health of patients.
Also have prior art medicine before use, the patient needs to take diphenhydramine and inject cimetidine to prevent side effects in advance, more troublesome

Method used

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  • Paclitaxel/multialkene paclitaxel liposome composite medicine and preparation method thereof
  • Paclitaxel/multialkene paclitaxel liposome composite medicine and preparation method thereof
  • Paclitaxel/multialkene paclitaxel liposome composite medicine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The formula that present embodiment adopts is as follows:

[0035] 300g of a mixture of hydrogenated soybean lecithin and sheep brain lecithin in a weight ratio of 2:1;

[0036] 200g of a mixture of cholesterol, stearylamide, and β-sitosterol in a weight ratio of 1:1:0.1;

[0037] 100g of a mixture of tiopronin and vitamin E in a weight ratio of 4:1;

[0038] 150g of any ratio mixture of Polyethylene Glycol-4000 and Polyethylene Glycol 6000;

[0039] Vitamin C 150g;

[0040] 4000g of mixture of tert-butanol and absolute ethanol in a weight ratio of 1.5-2.2:0.01-0.05;

[0041] A mixture of paclitaxel and docetaxel in any ratio 20g;

[0042] Diphenhydramine, cimetidine weight ratio 1: 6 mixture 350g;

[0043] Mix in 12000g of 0.01M, pH6.0-7.5 phosphate buffer.

[0044] The present invention also provides a preparation method of the above-mentioned combination medicine, which is characterized in that it comprises the following steps:

[0045] (1) Add the arbitrary r...

Embodiment 2

[0069] The formula adopted in the present embodiment is as follows (consumption: gram):

[0070] A mixture of hydrogenated soybean lecithin and sheep brain lecithin in a weight ratio of 2:1 550;

[0071] Cholesterol, stearylamide, β-sitosterol mixture with a weight ratio of 1:1:0.1 400;

[0072] The mixture of tiopronin and vitamin E in a weight ratio of 4:1 200;

[0073] Any ratio mixture of polyethylene glycol-4000 and polyethylene glycol 6000 200;

[0074] Vitamin C 180;

[0075] A mixture of tert-butanol and absolute ethanol in a weight ratio of 1.5-2.2:0.01-0.05 7000;

[0076] Mixture of paclitaxel and docetaxel in any ratio 40;

[0077] A mixture of diphenhydramine and cimetidine in a weight ratio of 1:6 500;

[0078] Mix in 12000g of 0.01M, pH6.0-7.5 phosphate buffer.

[0079] The present invention also provides a preparation method of the above-mentioned combination medicine, which is characterized in that it comprises the following steps:

[0080] (1) Add the a...

Embodiment 3

[0104] The formula adopted in the present embodiment is as follows (consumption: gram):

[0105] A mixture of hydrogenated soybean lecithin and sheep brain lecithin in a weight ratio of 2:1 400;

[0106] Cholesterol, stearylamide, β-sitosterol mixture with a weight ratio of 1:1:0.1 300;

[0107] The mixture of tiopronin and vitamin E in a weight ratio of 4:1 150;

[0108] Any ratio mixture of polyethylene glycol-4000 and polyethylene glycol 6000 180;

[0109] Vitamin C 165;

[0110] A mixture of tert-butanol and absolute ethanol in a weight ratio of 1.5-2.2:0.01-0.05 6000;

[0111] Mixture of paclitaxel and docetaxel in any ratio 32;

[0112] A mixture of diphenhydramine and cimetidine in a weight ratio of 1:6 420;

[0113] Mix in 12000g of 0.01M, pH6.0-7.5 phosphate buffer.

[0114] The present invention also provides a preparation method of the above-mentioned combination medicine, which is characterized in that it comprises the following steps:

[0115] (1) Add the a...

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Abstract

The invention relates to a liposome drug combination and a preparation method of the drug combination. The weights of the effective drug components are listed as follows: the weight of the admixture for hydrogenated soybean phosphatide and sheep brain lecithin with a weight ratio of 2:1 is 300 to 550; the weight of the admixture for cholesterol, stearamide and beta-sitosterol with a weight ratio of 1:1:0.1 is 200 to 400; the weight of the admixture for tiopronin and vitamin E with a weight ratio of 4:1 is 100 to 200; the weight of the admixture for polyethylene glycol-4000 and polyethylene glycol-6000 with a discretional weight ratio is 150 to 200; the weight of vitamin C is 150 to 180; the weight of the admixture for tert-butyl alcohol and anhydrous alcohol with a weight ratio of 1.5 to 2.2:0.01 to 0.05 is 4000 to 7000; the weight of the admixture for paclitaxel and polyene paclitaxel with a discretional weight ratio is 20 and 40; the weight of the admixture for diphenhydramine and cimetidine with a weight ratio of 1:6 is 350 to 500. The invention has the advantages of reducing the drug dosage by nearly one time, increasing the curative effect by over 15 percent, and greatly reducing the side effect of the drugs.

Description

technical field [0001] The invention relates to a paclitaxel / docetaxel liposome combination drug and a preparation method thereof. Background technique [0002] Paclitaxel or docetaxel is a broad-spectrum effective anticancer drug, which can act on the microtubule / tubulin system of tumor cells, promote the assembly of tubulin into microtubules, but at the same time inhibit the depolymerization of microtubules, resulting in the breakdown of microtubule bundles. Abnormal alignment, formation of stellate bodies, disabling the normal function of the spindle, leading to tumor cell death. [0003] However, in the prior art, paclitaxel or docetaxel preparations are common injections, and 47% of people have decreased blood neutrophils after using this type of drug, and 62% of people have decreased blood neutrophils after using this type of drug. Systemic poisoning and numbness of the limbs, side effects on the liver, skin, and digestive system are common and obvious. In recent yea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/337A61K31/4164A61K31/355A61K31/375A61K31/135A61K31/198A61K9/127A61K47/24A61K47/28A61K47/18A61K47/32A61K47/20A61P35/00
Inventor 蔡海德
Owner HUNAN KANGDU PHARMA
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