Method for preparing high-load oral paclitaxel capsule for slow release in colon

Patent metadata

Field	Value
Publication number	US-11771676-B2
Application number	US-202318190372-A
Country	US
Kind code	B2
Filing date	Mar 27, 2023
Priority date	Apr 29, 2022
Publication date	Oct 3, 2023
Grant date	Oct 3, 2023

Abstract

Disclosed is a method for preparing high-load oral paclitaxel capsule for a slow release in colon, belonging to the field of porous starch drug loading. The preparation method of the present disclosure includes the following steps: (1) dripping an ethanol solution of paclitaxel into a water phase and drying the solution to obtain an amorphous paclitaxel microsphere; (2) redissolving the paclitaxel microsphere prepared in step (1) in the ethanol solution, dispersing porous starch in the ethanol solution for adsorption, volatilizing a solvent in an oven, washing the porous starch with the ethanol solution to remove unadsorbed paclitaxel, and centrifuging same to obtain a precipitate, namely the porous starch loaded with paclitaxel; and (3) dispersing the porous starch loaded with paclitaxel prepared in step (2) in a chitosan solution, dropwise adding the solution into a phytic acid solution, and stirring the solution for 4 hours to obtain a coated capsule.

First claim

What is claimed is:

1. A method for preparing a high-load oral paclitaxel capsule for slow release in colon, comprising the following steps:
(1) preparing an amorphous paclitaxel:
dripping an ethanol solution of paclitaxel into a water phase, and stirring uniformly and drying the solution to obtain an amorphous paclitaxel microsphere;
(2) adsorbing paclitaxel with porous starch:
redissolving the amorphous paclitaxel microsphere prepared in step (1) in the ethanol solution, dispersing porous starch in the ethanol solution for adsorption, volatilizing a solvent in an oven, washing the porous starch with the ethanol solution to remove unadsorbed paclitaxel, and centrifuging same to obtain a precipitate, namely the porous starch loaded with paclitaxel; and
(3) preparing a chitosan-coated capsule:
dispersing the porous starch loaded with paclitaxel prepared in step (2) in a chitosan solution, after dispersing uniformly to obtain a solution, dropwise adding the solution into a phytic acid solution, and stirring to obtain a coated capsule.

2. The method according to claim 1 , wherein a concentration of the paclitaxel in the ethanol solution of paclitaxel in step (1) is 10-20 mg/mL.

3. The method according to claim 1 , wherein a volume ratio of the water phase to the ethanol phase in step (1) is (2-4):1.

4. The method according to claim 1 , wherein a mass ratio of the porous starch to the paclitaxel microsphere in step (2) is (3-7):1.

5. The method according to claim 1 , wherein the volatilizing of the solvent is performed at a temperature of 40-55° C. for 10-20 minutes in step (2).

6. The method according to claim 1 , wherein a mass ratio of the porous starch loaded with paclitaxel to the chitosan in step (3) is (4-6):1.

7. The method according to claim 1 , wherein a volume ratio of the phytic acid solution to the chitosan solution in step (3) is (7-10):1.

8. The method according to claim 1 , wherein the chitosan solution in step (3) is an aqueous solution at a chitosan concentration of 30-50 mg/mL.

9. A high-load oral paclitaxel capsule prepared by the method according to claim 1 .

Assignees

• Univ Jiangnan

Inventors

• Hong Yan
• Zhao Beibei
• Gu Zhengbiao
• Cheng Li
• Li Zhaofeng
• Li Caiming
• Ban Xiaofeng

Classifications

• A61K31/337 Primary

  having four-membered rings, e.g. taxol · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K9/4866

  Organic macromolecular compounds · CPC title

• A61K9/5036

  Polysaccharides, e.g. gums, alginate; Cyclodextrin · CPC title

• A61K9/1652

  Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623) · CPC title