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Method for preparing block polymer micelle freeze-drying preparation carrying docetaxel

A technology of block polymer and docetaxel, which is applied in the field of medicine and chemical industry, can solve the problems of inconvenient, unsolved, low drug safety, etc. in clinical medicine, prolong the residence time in the body, and is suitable for clinical application. , the effect of increasing solubility

Inactive Publication Date: 2010-06-16
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation dissolves docetaxel in Tween-80, and needs to be diluted with a special injection solvent before use. The requirements for operators are extremely strict and the method of use is cumbersome; a large amount of Tween in the preparation can easily cause hemolysis and allergies Adverse reactions such as dexamethasone and other drugs need to be taken in advance for prevention and treatment, which is inconvenient for clinical use and has low drug safety
So far, this problem has not been well resolved

Method used

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  • Method for preparing block polymer micelle freeze-drying preparation carrying docetaxel
  • Method for preparing block polymer micelle freeze-drying preparation carrying docetaxel
  • Method for preparing block polymer micelle freeze-drying preparation carrying docetaxel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of block polymer micelles lyophilized formulation loaded with docetaxel:

[0028] (1) Weigh 100mg of P123 type PEO-PPO-PEO block copolymer, 2mg of docetaxel, add 2mL of acetonitrile, ultrasonically dissolve the carrier material and the drug, the solution is rotatively evaporated in a water bath at 40°C to exhaust the acetonitrile, and vacuum at 25°C After drying overnight, a colorless and transparent drug film was obtained, and 5 mL of double-distilled water was used as the hydration medium, and stirred for 1-2 hours to obtain a colorless and transparent docetaxel-P123 micellar solution;

[0029] (2) Add 0.01g mannose as a freeze-drying protective agent, pass through a 0.22μm microporous membrane to sterilize, divide the solution into sterile penicillin vials, each 1mL, and freeze-dry to obtain white loose docetaxel - P123 micellar freeze-dried preparation, each containing 0.4mg of docetaxel, the freeze-dried preparation can be completely reconstit...

Embodiment 2

[0030] Example 2 Preparation of block polymer micelles lyophilized formulation loaded with docetaxel:

[0031] (1) Weigh 100mg P123 type PEO-PPO-PEO block copolymer, 100mgD-α-tocopheryl polyethylene glycol succinate (TPGS), 4mg docetaxel, add 2mL acetonitrile, ultrasonically make the carrier material and drug Fully dissolved, the solution was evaporated in a water bath at 40°C to exhaust the acetonitrile, and dried in vacuum at 25°C overnight to obtain a colorless and transparent drug film. With 5 mL double-distilled water as the hydration medium, stir for 1-2 hours to obtain colorless and transparent docetaxel - P123 micellar solution;

[0032] (2) Add 0.01g mannose as a freeze-drying protective agent, pass through a 0.22μm microporous membrane to sterilize, divide the solution into sterile penicillin vials, each 1mL, and freeze-dry to obtain white loose docetaxel -P123 / TPGS micellar lyophilized preparation, each containing 0.8 mg of docetaxel, the lyophilized preparation ca...

Embodiment 3

[0033] Example 3 Preparation of block polymer micelles lyophilized formulation loaded with docetaxel:

[0034] (1) Weigh 200 mg of F127 type PEO-PPO-PEO block copolymer, 1 mg of docetaxel, add 1 mL of acetonitrile, and ultrasonically dissolve the carrier material and drug in a water bath for 10 minutes. After vacuum drying overnight at ℃ to obtain a colorless and transparent drug film, use 10mL double-distilled water as the hydration medium, and stir for 1-2 hours to obtain a colorless and transparent docetaxel-F127 micellar solution;

[0035] (2) Add 0.04 g of mannitol as a freeze-drying protective agent, pass through a 0.22 μm microporous membrane to sterilize, divide the solution into sterile penicillin vials, 2 mL each, and freeze-dry to obtain white and loose docetaxel - F127 micellar lyophilized preparation, which can be completely reconstituted within 1 min by adding 2 mL of double distilled water and shaking, and the obtained micelle solution is clear and transparent. ...

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Abstract

The invention discloses a method for preparing a block polymer micelle freeze-drying preparation carrying docetaxel, which uses a PEO-PPO-PEO block polymer as a micelle carrier to wrap the docetaxel inside the micelle and comprises the following steps: (1) dissolving the carrier and the docetaxel into an organic solvent to make the PEO-PPO-PEO block polymer and the docetaxel fully dissolved in the organic solvent, and then preparing aqueous solution of the docetaxel micelle by using the PEO-PPO-PEO block polymer as the carrier; and (2) adding a freeze-drying protective agent into the aqueous solution of the PEO-PPO-PEO block polymer carrying micelle, and filtering, sterilizing and freeze-drying the mixture to obtain freeze-drying preparation of the carrier micelle system. The block polymer micelle freeze-drying preparation carrying the docetaxel can increase the dissolubility, metabolic stability and in vivo circulation time of the docetaxel, reduce the toxicity and improve the bioavailability, and is more suitable for clinical application.

Description

technical field [0001] The invention relates to a preparation method of a docetaxel-loaded block polymer micelle freeze-dried preparation, which belongs to the technical field of medicine and chemical industry. Background technique [0002] At present, effective measures to conquer cancer include surgery, radiotherapy, chemotherapy, etc., but they all have their limitations. For example, radiotherapy and chemotherapy generally have toxic side effects such as killing healthy red and white blood cells, liver and kidney toxicity, and nervous system damage. Therefore, the development of effective anticancer drugs has become a long-term key research topic in the world's medical circles. [0003] Docetaxel is a paclitaxel antineoplastic drug that has been approved by the U.S. Food and Drug Administration as a cancer treatment drug. It plays an antitumor role by interfering with the microtubule network necessary for cell mitosis and interphase cell functions. Docetaxel can bind to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K31/337A61P35/00A61K47/10
Inventor 张娜刘志红刘东华黄桂华
Owner SHANDONG UNIV
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