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Paclitaxel oral polymeric micelle and preparation method and application thereof

A technology of polymer glue and paclitaxel, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients, etc., can solve the problems of poor water solubility of paclitaxel, prone to allergic reactions, and clinical application limitations, etc., and achieve good thermodynamic stability , Improve bioavailability, good effect of micellar shape

Active Publication Date: 2020-04-24
GUANGXI UNIV OF CHINESE MEDICINE +1
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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 polymeric micelle and preparation method and application thereof
  • Paclitaxel oral polymeric micelle and preparation method and application thereof
  • Paclitaxel oral polymeric micelle and preparation method and application thereof

Examples

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example 1

[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 2

[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...

example 3

[0067] The preparation method of paclitaxel oral polymer micelles:

[0068] (1) Weigh 3.6g 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;

[0069] (2) Add a solution of 0.025g of 4-dimethylaminopyridine and 7mL of ethanol, and an ethanol solution of 0.055g 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;

[0070] (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);

[0071]

[0072] (4) Mix 0.5g of polyethylene glycol 1000-vitamin-E-succinate (TPGS), 0.75g of succinic anhydride (SA), and 0.06g of 4-dimethylaminopyridine (DMAP) after vacuum drying. Purified 10mL d...

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Abstract

The invention discloses a paclitaxel oral polymeric micelle. Paclitaxel is used as a model drug, and a GA-CS-TPGS copolymer is used as a carrier for oral medication. The critical micelle concentrationof the GA-CS-TPGS copolymer is 0.0109 mg / mL to 0.0203 mg / mL, and the partical size of the paclitaxel oral polymeric micelle is controlled to be 98-182nm, wherein the molecular structural formula of the GA-CS-TPGS copolymer is shown as a formula (1). The invention also discloses a preparation method and application of the paclitaxel oral polymeric micelle. The paclitaxel oral polymeric micelle hasgood adhesion and intestinal absorption, the bioavailability of paclitaxel is improved, and the requirement of oral medication of paclitaxel can be met.

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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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 GUANGXI UNIV OF CHINESE MEDICINE
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