IP Library Granted Patent US 8,163,940
Granted Patent B2
US 8,163,940 · App. 12/159,812 · Granted Apr 24, 2012

Method for preparation of amorphous, anhydrous crystalline or hydrated crystalline docetaxel

Assignee: Samyang Genex Corporation
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Quick Facts
Patent No.
US 8,163,940
App. No.
12/159,812
Granted
Apr 24, 2012
Kind
B2
Abstract

This invention is directed to a method for the preparation of docetaxel having an amorphous, anhydrous crystalline, or hydrated crystalline structure. In accordance with the invention, highly pure amorphous, anhydrous crystalline, or hydrated crystalline docetaxel can be produced with a high yield by using a solvent precipitation method, colloid formation method, etc.

Claims (11)

1. A method for the preparation of amorphous docetaxel, comprising:

dissolving a docetaxel-containing matter or docetaxel in a polar solvent at a concentration of 1 to 30% (w/v);

adding the above-obtained solution to a non-polar solvent of 5 times or higher thereof by volume to cause precipitation; and

filtrating and drying the produced precipitate to obtain amorphous docetaxel, wherein the polar solvent is at least one selected from the group consisting of dichloromethane, chloroform and acetone, and the non-polar solvent is at least one selected from the group consisting of hexane, pentane, cyclohexane, cyclopentane and dialkylether.

2. A method for the preparation of anhydrous crystalline docetaxel, comprising:

mixing 1 to 30% (w/v) of a docetaxel-containing matter or docetaxel and acetone and colloidizing it in a suspended state; and

evaporating the acetone among the obtained colloid solution at 35° C. to 40° C. and drying it under a reduced pressure to obtain anhydrous crystalline docetaxel of fine powders.

3. A method for the preparation of hydrated crystalline docetaxel, comprising:

dissolving a docetaxel-containing matter of docetaxel in a mixed solvent of an organic solvent and purified water having a mixing ratio of 7:0.5 to 7:5 by volume or a mixed solvent of an organic solvent and a buffer solution having a mixing ratio of 7:0.5 to 7:5 by volume at a concentration of 0.1 to 5% (w/v);

producing a precipitate by evaporating the obtained solution at 35° C. to 40° C., thereby eliminating the organic solvent among the mixed solvent; and

filtrating the obtained precipitate at a reduced pressure and drying it to prepare hydrated crystalline docetaxel, wherein the organic solvent is at least one selected from the group consisting of methanol, ethanol, propanol, acetone and acetonitrile, and the hydrated crystalline docetaxel is dihydrate.

Assignments (5)
CHANGE OF ADDRESS Recorded Nov 3, 2021
From: SAMYANG BIOPHARMACEUTICALS CORPORATION
To: SAMYANG BIOPHARMACEUTICALS CORPORATION
Reel/Frame 058013/0696 →
MERGER Recorded Nov 3, 2021
From: SAMYANG BIOPHARMACEUTICALS CORPORATION
To: SAMYANG HOLDINGS CORPORATION
Reel/Frame 058013/0766 →
MERGER Recorded Feb 14, 2014
From: SAMYANG GENEXBIO CORPORATION
To: SAMYANG BIOPHARMACEUTICALS CORPORATION
Reel/Frame 032265/0093 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2012
From: SAMYANG GENEX CORPORATION
To: SAMYANG GENEXBIO CORPORATION
Reel/Frame 028189/0351 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2008
From: PYO, SANG-HYUN; CHO, JIN-SUK; KIM, MOON-SUK; SONG, BONG-KYU; CHOI, HO-JOON
To: SAMYANG GENEX CORPORATION
Reel/Frame 021308/0051 →
Priority Claims (1)
KR 10-2006-0000276 · Jan 2, 2006 · national
Continuity (1)
Related Publication 20090018353A1 · Jan 15, 2009