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1. (WO2018176158) NON-IONIC BLOCK COPOLYMERS AND PHARMACEUTICAL COMPOSITIONS DERIVED THEREFROM

Pub. No.:    WO/2018/176158    International Application No.:    PCT/CA2018/050399
Publication Date: Fri Oct 05 01:59:59 CEST 2018 International Filing Date: Fri Mar 30 01:59:59 CEST 2018
IPC: C08F 290/06
A61K 31/05
A61K 31/167
A61K 31/192
A61K 31/635
A61K 47/34
A61K 9/14
C07C 233/25
C07C 39/06
C07C 57/38
C07D 231/12
Applicants: ALTUS FORMULATION INC.
Inventors: SMITH, Damon
BAILLE, Wilms
KUJAWA, Piotr
Title: NON-IONIC BLOCK COPOLYMERS AND PHARMACEUTICAL COMPOSITIONS DERIVED THEREFROM
Abstract:
There are provided PVP-PLA block copolymers as defined in Formula (I): I wherein, x is an initiator alcohol having a boiling point greater than 145°C, n is, on average, from 20 and 40, and m is, on average, from 10 and 40, wherein the block copolymers have a number average molecular weight (Mn) of at least 3000 Da. Polymers demonstrating flexibility in formulating multiple low-solubility active pharmaceutical ingredients (APIs) are described. Liquid and dry pharmaceutical formulations comprising an API are described, along with delivery methods, uses, and kits. APIs may include, e.g. flurbiprofen, celecoxib, acetaminophen, or propofol. Also provided is a method of synthesizing the PVP-PLA block copolymers by (i) initiating polymerization of D,L-Lactide from the initiator alcohol x to form poly(lactic acid), adding a xanthate to form a PLA macroinitiator, and polymerizing NVP onto the PLA macroinitiator, by controlled polymerization, to form the block copolymer compound of Formula (I).