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Docetaxel polymer nano-micelle injection, and preparation method and application thereof in preparation of tumor drugs

A technology of nanomicelles and docetaxel, which is applied in antitumor drugs, drug combinations, drug delivery, etc., can solve the problems of limiting the clinical application of PEG-based polymer micelles, so as to improve the antitumor efficacy and increase the stability. , the effect of high safety

Inactive Publication Date: 2017-07-28
江苏富泽药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, anti-PEG antibodies already exist in 25% of patients (due to shampoos and other daily chemical products and some foods containing a large amount of PEG), and anti-PEG antibodies may be produced after multiple administrations, thereby limiting PEG Clinical application of polymer-like micelles

Method used

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  • Docetaxel polymer nano-micelle injection, and preparation method and application thereof in preparation of tumor drugs
  • Docetaxel polymer nano-micelle injection, and preparation method and application thereof in preparation of tumor drugs
  • Docetaxel polymer nano-micelle injection, and preparation method and application thereof in preparation of tumor drugs

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Embodiment 1

[0039] In the present invention, the preparation of docetaxel polymer nano micelles comprises the following steps:

[0040] 1) Weigh 10 mg of docetaxel and add 1 ml of anhydrous ethanol for ultrasonic dissolution; weigh 100 mg of PMOZ-PLA polymer and add 10 ml of absolute ethanol for ultrasonic dissolution; mix docetaxel and PMOZ-PLA polymer. The degree of polymerization of PMOZ is 50 units, and the average molecular weight is 4400Da. The degree of polymerization of polylactic acid PLA is 115 units, and the average molecular weight is 3300Da.

[0041] 2) Add the mixed solution to a 50 ml round-bottomed flask, slowly evaporate the solvent under reduced pressure at 40 degrees Celsius, and vacuum to remove solvent residues, forming a thin film (medicine+PMOZ-PLA polymer) at the bottom of the round-bottomed flask.

[0042] 3) At 45 degrees Celsius, add 10 ml of distilled water and shake slightly until the thin film is completely dissolved into a clear solution;

[0043] 4) Place...

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Abstract

The invention provides docetaxel polymer nano-micelle injection, and a preparation method and application thereof in preparation of tumor drugs; the docetaxel polymer nano-micelle injection comprises, by weight, 1 part of docetaxel and 10-100 parts of a nano-micelle polymer; the docetaxel nano-micelles are uniform in particle size and have 20-200 nm in average particle size. The docetaxel polymer nano-micelle injection can provide greatly improved water-solubility of docetaxel and has greatly improved stability, the cycle time of docetaxel in blood is extended, and toxic and side effects of commercially available preparations are decreased; docetaxel is passively targeted to a tumor part through EPR (enhanced permeability and retention) effect, anti-tumor effect of docetaxel is thereby improved, and the case that polymer nano-micelle preparations using PEG (polyethylene glycol) as a shell layer are not applicable (such as to the treatment of a patient having PEG antibodies or a patient having PEG antibodies generated in multiple administration) can be avoided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a docetaxel polymer nano-micelle injection, a preparation method and an application in medicine for treating tumors. Background technique [0002] Docetaxel is the second-generation semi-synthetic paclitaxel derivative, which uses n-butanol group to replace the phenyl group on paclitaxel. The mechanism of drug action is to promote tubulin polymerization and inhibit microtubule depolymerization, forming a stable non-functional Sexual microtubule bundles, thereby destroying tumor cell mitosis and inhibiting tumor cell growth. The affinity of docetaxel to microtubules is twice that of paclitaxel, so the pharmacological effect and activity are stronger than paclitaxel. Docetaxel exhibits 2-10 times higher anticancer activity than paclitaxel in in vitro cell tests, and has therapeutic effects on non-small cell lung cancer, ovarian cancer, prostate cancer, advanced breast canc...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/337A61K47/34A61P35/00
CPCA61K9/1075A61K9/0019A61K9/19A61K31/337A61K47/34
Inventor 何智健谢卫锋吴鹏程李浩源
Owner 江苏富泽药业有限公司
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