IP Library Granted Patent US 9,795,562
Granted Patent B2
US 9,795,562 · App. 14/717,641 · Granted Oct 24, 2017

Method for stabilizing amphiphilic block copolymer micelle composition containing poorly water-soluble drug

Inventors: Sa-Won Lee (Daejeon, KR); Min-Hyo Seo (Daejeon, KR)
Assignee: SAMYANG BIOPHARMACEUTICALS CORPORATION
A61K9/1075A61K9/0019A61K9/19A61K31/337A61K31/436A61K47/34
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Quick Facts
Patent No.
US 9,795,562
App. No.
14/717,641
Granted
Oct 24, 2017
Kind
B2
Abstract

A method for stabilizing a poorly water-soluble drug-containing amphiphilic block copolymer micelle composition via simplified steps in short time is described. Also described is a stabilized poorly water-soluble drug-containing amphiphilic block copolymer micelle composition having improved stability.

Claims (6)

1. A taxane-containing amphiphilic block copolymer micelle formation aqueous solution, consisting of 1.0-15 wt % of paclitaxel or docetaxel, 20-98wt % of an amphiphilic block copolymer containing a hydrophilic block (A) and a hydrophobic block (B), and 1.0-10 wt % of sodium chloride, in an aqueous ethanol solution, wherein the weight percentages are based on the total dry weight of the taxane-containing amphiphilic block copolymer micelle aqueous solution,

wherein the hydrophilic block (A) is polyethylene glycol or monomethoxypolyethylene glycol having a weight average molecular weight of 1,000-2,500 daltons, and the hydrophobic block (B) is polylactic acid (PLA) or a copolymer of polylactic acid and glycolic acid (PLGA) having a weight average molecular weight of 1,000-2,500 daltons, and

wherein the amphiphilic block copolymer comprises 50-60 wt % of the hydrophilic block (A) and 40-50 wt % of the hydrophobic block (B).

2. A reconstituted taxane-containing amphiphilic block copolymer micelle aqueous solution for intravenous infusion, consisting of 0.1-15 wt % of paclitaxel or docetaxel, based on the total dry weight of the aqueous solution, 10-150 mg/ml of an amphiphilic block copolymer containing a hydrophilic block (A) and a hydrophobic block (B), 5-30 mg/ml of sodium chloride, and 1-100 mg/ml of lactose or mannitol,

wherein the hydrophilic block (A) is polyethylene glycol or monomethoxypolyethylene glycol having a weight average molecular weight of 1,000-2,500 daltons, and the hydrophobic block (B) is polylactic acid (PLA) or a copolymer of polylactic acid and glycolic acid (PLGA) having a weight average molecular weight of 1,000-2,500 daltons, and

wherein the amphiphilic block copolymer comprises 50-60 wt % of the hydrophilic block (A) and 40-50 wt % of the hydrophobic block (B).

Assignments (2)
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 →
Priority Claims (2)
KR 10-2007-0141181 · Dec 31, 2007 · national
KR 10-2008-0098521 · Oct 8, 2008 · national
Continuity (3)
Continuation 13960177 · Aug 6, 2013
Continuation In Part 12810473
Related Publication 20150250721A1 · Sep 10, 2015