BIODEGRADABLE, SEMI-CRYSTALLINE, PHASE SEPARATED, THERMOPLASTIC MULTI-BLOCK COPOLYMERS FOR CONTROLLED RELEASE OF BIOLOGICALLY ACTIVE COMPOUNDS Russian patent published in 2018 - IPC C08G81/00 C08G63/91 C08L101/16 C08L67/04 A61K47/34 A61K9/16 

Abstract RU 2662818 C2

FIELD: medicine.

SUBSTANCE: described is a biodegradable, semi-crystalline, phase separated thermoplastic multi-block copolymer, characterised in that: a) it comprises at least one segment of hydrolysable prepolymer (A), said prepolymer segment (A) being derived from lactide and / or ε-caprolactone, and at least one segment of hydrolysable prepolymer (B), wherein said prepolymer segment (B) is a crystalline polymer derived from L-lactide, D-lactide, glycolide, or a combination of these monomers with Mn 1000 g / mol or higher; wherein said segment of prepolymer (A) forms an amorphous phase, and segment of prepolymer (B) forms a crystalline phase; b) said multiblock copolymer is characterised by Tst 37°C or lower and Tpl 110-250°C under physiological conditions; c) the segments are linked via a polyfunctional chain extender, said polyfunctional chain extender being 1,4-butane diisocyanate; d) the segments are randomly distributed across the polymer chain; e) at least a portion of the segment of prepolymer (A) is derived from a water-soluble polymer, said water-soluble polymer being poly(ethylene glycol) (PEG) having Mn of 150-5000 g / mol. Also described is a process for the preparation of said biodegradable, semi-crystalline, phase separated thermoplastic multi-block copolymer, comprising: i) performing a chain extension reaction of prepolymer (A) and prepolymer (B) in the presence of a polyfunctional chain-extender, said polyfunctional chain extender being 1,4-butane diisocyanate, wherein prepolymers (A) and (B) both have diol or dibasic acid end groups. Described is the use of said biodegradable, semi-crystalline, phase separated thermoplastic multi-block copolymer for drug delivery. Also described is a composition for delivering a biologically active compound to a host, comprising a biologically active compound encapsulated in a matrix, said matrix comprising said biodegradable, semi-crystalline, phase separated thermoplastic multi-block copolymer. Methods of preparing said composition are also described.

EFFECT: present invention relates to a biodegradable, semi-crystalline, phase separated thermoplastic multi-block copolymer.

24 cl, 22 dwg, 5 tbl, 23 ex

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RU 2 662 818 C2

Authors

Stendam Rob

Flipsen Teodorus Adrianus Kornelius

Khimstra Kristin

Zejdema Jokhan

Dates

2018-07-31Published

2012-07-23Filed