Paclitaxel oral polymer micelle and its preparation method and application

A technology of polymer glue and paclitaxel, which can be used in drug combinations, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of poor water solubility of paclitaxel, prone to allergic reactions, clinical application limitations, etc., and achieves good thermodynamic stability. , Improve bioavailability, good effect of micelle morphology

Active Publication Date: 2022-02-22
HUNAN YINENG BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, paclitaxel has poor water solubility and poor oral absorption, which limits its clinical application. Clinically, paclitaxel is often dissolved in polyoxyethylene castor oil and absolute ethanol solvent mixed in a certain proportion, and the human body is prone to intolerance to polyoxyethylene castor oil. Infected, prone to allergic reactions, severe cases may lead to dyspnea, bone marrow suppression, etc.

Method used

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  • Paclitaxel oral polymer micelle and its preparation method and application
  • Paclitaxel oral polymer micelle and its preparation method and application
  • Paclitaxel oral polymer micelle and its preparation method and application

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preparation example Construction

[0031] The preparation method of paclitaxel oral polymer micelles:

[0032] (1) Weigh 3.4g CS into a round-bottomed flask, add 100mL water to suspend, adjust the pH to 3-6 with dilute hydrochloric acid solution, and dissolve it by magnetic stirring;

[0033] (2) Add a solution of 0.028g of 4-dimethylaminopyridine and 7mL of ethanol, and an ethanol solution of 0.049g of methyl gallate, and react in a water bath at 80°C for 24 hours under the protection of nitrogen, stop heating, and cool to room temperature;

[0034] (3) Centrifuge, take the supernatant, dialyze with water and 50% ethanol volume solution for 3 times respectively, concentrate under reduced pressure to remove ethanol, freeze-dry to obtain GA-CS sample, the molecular structure formula is as shown in formula (2);

[0035]

[0036] (4) Mix 0.5g of polyethylene glycol 1000-vitamin-E-succinate (TPGS), 0.66g of succinic anhydride (SA), and 0.04g of 4-dimethylaminopyridine (DMAP) after vacuum drying. Purified 10mL d...

example

[0049] The preparation method of paclitaxel oral polymer micelles:

[0050] (1) Weigh 3.8g CS into a round-bottomed flask, add 100mL water to suspend, adjust the pH of dilute hydrochloric acid solution to 3-6, and stir magnetically to dissolve it;

[0051] (2) Add a solution of 0.032g of 4-dimethylaminopyridine and 7mL of ethanol, and an ethanol solution of 0.046g of methyl gallate, and react in a water bath at 80°C for 24 hours under the protection of nitrogen, stop heating, and cool to room temperature;

[0052] (3) Centrifuge, take the supernatant, dialyze with water and 50% ethanol volume solution for 3 times respectively, concentrate under reduced pressure to remove ethanol, freeze-dry to obtain GA-CS sample, the molecular structure formula is as shown in formula (2);

[0053]

[0054] (4) Mix 0.5g of polyethylene glycol 1000-vitamin-E-succinate (TPGS), 0.48g of succinic anhydride (SA), and 0.02g of 4-dimethylaminopyridine (DMAP) after vacuum drying. Purified 10mL dic...

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Abstract

The invention discloses a paclitaxel oral polymer micelle, which uses paclitaxel as a model drug and uses a GA-CS-TPGS copolymer as a carrier for oral administration, and the critical micelle concentration of the GA-CS-TPGS copolymer is 0.0109 ~0.0203mg / mL, control paclitaxel oral polymer micelle particle diameter at 98~182nm, wherein, the molecular structure formula of GA-CS-TPGS copolymer is as shown in formula (1): the present invention also discloses a kind of paclitaxel oral polymeric Preparation methods and applications of micelles. The invention has good adhesion and intestinal absorption, improves the bioavailability of paclitaxel, and can meet the requirements of oral administration of paclitaxel.

Description

technical field [0001] The present invention relates to drug synthesis and application. More specifically, the present invention relates to a paclitaxel oral polymer micelle and its preparation method and application. Background technique [0002] Paclitaxel (PTX), also known as Taxol, Paclitaxel, Paclitaxel, Special Element, is an anticancer substance extracted from Taxus chinensis. Paclitaxel is white crystalline powder, odorless, tasteless, insoluble in water, easily soluble in methanol, acetonitrile, chloroform, acetone and other organic solvents. Paclitaxel is clinically used in the treatment of malignant tumors such as ovarian cancer, breast cancer, and non-small cell lung cancer. It promotes and induces tubulin polymerization of tumor cells and stabilizes microtubules, which affects the assembly of the spindle in the mitotic phase and blocks tumor cells. Mitosis, so as to achieve the purpose of anti-tumor. However, paclitaxel has poor water solubility and poor oral...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/36A61P35/00C08G81/00
CPCA61K31/337A61K9/1075A61K47/36A61P35/00C08G81/00
Inventor 奉建芳张玮高红伟陈田娥王柳萍王鸽
Owner HUNAN YINENG BIOLOGICAL PHARMA
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