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Micelles and freeze-dried preparations of diblock polymer-supported taxane medicines and preparation and use thereof

A technology of diblock polymers and taxanes, which can be applied in the directions of drug combination, drug delivery, medical preparations of inactive ingredients, etc., can solve the problem of death, increase in toxic and side effects, and limit taxane drugs such as paclitaxel Clinical application and other problems, to achieve the effect of simple preparation process, easy operation of preparation process and good stability

Inactive Publication Date: 2011-09-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Docetaxel injection is also a solution composed of docetaxel Tween 80 and ethanol, and the clinical trials are somewhat similar to paclitaxel injection; but Tween 80 and ethanol often cause strong side effects, such as hypersensitivity, hemolysis, nephrotoxicity, neurotoxicity, and cardiotoxicity, which may lead to death in severe cases
And with the dose increasing, the side effects tend to increase
Therefore, the clinical application of taxanes such as paclitaxel is greatly limited.
[0003] Those skilled in the art have been working on reducing toxic and side effects, or increasing its drug concentration in target organs, in order to better exert its curative effect, but there is still no effective solution to the problems encountered by taxanes in clinical anti-tumor

Method used

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  • Micelles and freeze-dried preparations of diblock polymer-supported taxane medicines and preparation and use thereof
  • Micelles and freeze-dried preparations of diblock polymer-supported taxane medicines and preparation and use thereof
  • Micelles and freeze-dried preparations of diblock polymer-supported taxane medicines and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] (1) Combine 92mg of methoxy polyethylene glycol poly(ε-caprolactone) copolymer (MPEG 2000 -PCL 2000 ) And 8mg paclitaxel dissolved in 2ml absolute ethanol, heated or ultrasonically stirred until completely dissolved, to obtain a clear solution A;

[0075] (2) Rotate and evaporate the clarified solution A under heating to remove the organic solvent to make it a transparent gel B;

[0076] (3) Add 5ml of preheated water for injection to gel B, make it clear and transparent under heating and stirring, and pass through a 0.22μm filter membrane to prepare micelle C with a particle size of 10nm-100nm;

[0077] (4) The micelle C is lyophilized to obtain the final stable nano-medicine lyophilized powder D.

[0078] Before the lyophilized powder is used clinically, the nano-sized micelles formed automatically under the condition of heating with water for injection.

[0079] The resulting micelle C, lyophilized powder D and the final reconstituted micelle, see figure 2 . The average diam...

Embodiment 2

[0081] (1) Put 85mg of methoxy polyethylene glycol poly(ε-caprolactone) copolymer (MPEG 2000 -PCL 2000 ) And 15mg of docetaxel are dissolved in 2ml of absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0082] (2) Rotate and evaporate the clarified solution A under heating to remove the organic solvent to make it a transparent gel B;

[0083] (3) Add 5ml of preheated water for injection to gel B, make it clear and transparent under heating and stirring, and pass through a 0.22μm filter membrane to prepare micelle C with a particle size of 10nm-100nm;

[0084] (4) The micelle C is lyophilized to obtain the final stable nano-medicine lyophilized powder D.

[0085] Before the lyophilized powder is used clinically, the nano-sized micelles formed automatically under the condition of heating with water for injection.

[0086] The properties of the obtained micelle C, lyophilized powder D and the final reconstituted micelle are the same figure 2 the...

Embodiment 3

[0088] (1) Combine 92mg of methoxy polyethylene glycol poly(ε-caprolactone) copolymer (MPEG 2000 -PCL 2000 ) And 5mg paclitaxel are dissolved in 2ml absolute ethanol, heated and stirred until completely dissolved to obtain a clear solution A;

[0089] (2) Rotate and evaporate the clarified solution A under heating to remove the organic solvent to make it a transparent gel B;

[0090] (3) Add 5ml of preheated water for injection to gel B, make it clear and transparent under heating and stirring, and pass through a 0.22μm filter membrane to prepare micelle C with a particle size of 10nm-100nm;

[0091] (4) The micelle C is lyophilized to obtain the final stable nano-medicine lyophilized powder D.

[0092] Before the lyophilized powder is used clinically, the nano-sized micelles formed automatically under the condition of heating with water for injection. The resulting micelles have a drug loading capacity of 5.09% and an encapsulation efficiency of 99.17%; the resulting micelles C, lyop...

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Abstract

The invention belongs to the technical field of medicinal preparations and nano medicine preparation and relates to the micelles and freeze-dried preparations of diblock polymer-supported taxane medicines and preparation and use thereof. For using the micelles in clinic, the medicine load capacity, encapsulation rate and stability of the preparation are required to be ensured. The micelles are prepared from 1.5 to 99 parts of methoxypolyethylene glycol (MPEG)-polycaprolactone (PCL) diblock polymer and 1 part of taxane medicines; and in the diblock polymer, the molecular weight ratio of the MPEG to the PCL is 0.5 to 2. The micelles and freeze-dried preparations of taxane medicines can be used for treating patients with cancers, tumors, Kaposi sarcoma, malignant tumors, tissue and cell hyperplasia due to tissue injuring disorder, and any of other diseases that can react with taxane medicines, and the treatment effects of the micelles and freeze-dried preparations are obvious particularly on hepatocellular carcinoma, ovarian cancer and breast cancer.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical dosage forms and nano-medicine preparations, and particularly relates to a diblock polymer loaded micelle of taxane drugs, a freeze-dried preparation, and a preparation method and application thereof. Background technique [0002] Taxane compounds are a large class of natural products obtained from plants. They belong to the diterpenoids from the structural classification, so they are also called taxane diterpenes. Paclitaxel, as the star molecule in these compounds, is an important anticancer drug used clinically. Paclitaxel (Taxol, trade name) is a natural anti-cancer raw material extracted from yew or yew trees. It is a white crystalline powder, insoluble in water, and easily soluble in organic solvents such as chloroform and acetone. Docetaxel (trade name: Taxotere) is a compound synthesized from the berry yew (Taxusbaccata, Europeanyew) needle leaf extract through structural modification. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/337A61K47/34A61P35/00A61P35/04
Inventor 钱志勇魏于全王成赵霞
Owner SICHUAN UNIV
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