Ingell Technologies Holding B.v.

Mike De Leeuw

Ronald Meijboom

Peter Bruin

Audrey Petit

Sebastien Jerome Pierre

Theo Flipsen

Martin Piest

A bioresorbable triblock copolymer according to Formula 1R-B-A-B-R&#x2003;&#x2003;(1)wherein A is a hydrophilic polymer, B a hydrophobic polymer and R are end-groups, wherein R is H or a C1-C30 organic moiety and wherein the copolymer is fluid in a temperature range of 0&#xb0; C. to 37&#xb0; C. A pharmaceutical composition including the triblock copolymer and at least one therapeutically active agent. The copolymer and pharmaceutical composition can be used for forming a depot in a human or animal body or as medical device.

Liquid triblock copolymer

A special class of drug-depot forming triblock copolymers which are very suitable for the loading, containment and releasing of sensitive drugs such as proteins from biodegradable, injectable drug depots. How to visualize these depots for various imaging related purposes is described. A composition comprising a tri-block copolymer according to formula 1 B-A-B (1), wherein A stands for a linear poly-(ethylene glycol) block and wherein B stands for wherein B stands for a poly(lactide-co-&#x3b5;-caprolactone) block, wherein the hydroxyl end-groups of the tri-block copolymer are at least partially acylated with an optionally substituted acyl having 2 to 12 C-atoms, C-atoms of the substituents included; an active ingredient, preferably a pharmaceutically active ingredient and a solvent, wherein the block ratio of the tri-block copolymer, which ratio is defined as the ratio between the sum of the average molecular weight of the B-blocks and the sum of the average molecular weight of the A-block ranges from 1.4 to 3.5. This composition is suitable for controlled release of a pharmaceutically active ingredient.

Biodegradable compositions suitable for controlled release

Simple mixing/blending of a special class of drug-depot forming tri-block copolymers polymers, with the opportunity to cost-effectively tailor drug delivery performances of such biodegradable, injectable depots in a clinical and an industrial setting. How to visualize these depots for various imaging related purposes is described. A composition comprising (a) an active ingredient, preferably a pharmaceutically active ingredient (b) a solvent and (c) a mixture of at least two types of tri-block copolymers of formula (1)B-A-B&#x2003;&#x2003;(1)wherein B stands for a hydrophobic block and wherein A stands for a hydrophilic block, wherein the mixture is prepared by mixing at least two types of tri-block copolymers having a degree of modification of 100% and wherein the at least two types of B-A-B types of tri-block copolymers differ only on the type of end-group or wherein the mixture is prepared by mixing at least two types of tri-block copolymers, wherein one of the at least two tri-block copolymers has a degree of modification of 100% and one of the at least two tri-block copolymers has a degree of modification of 0% and wherein the at least two types of B-A-B types of tri-block copolymers differ only on the degree of modification of the end-groups.

Amphiphilic triblock copolymers B-A-B, wherein A is a linear poly(ethylene glycol) block, having a number average molecular weight (M) of between 900 and 3000 Daltons, determined with size exclusion chromatography; wherein B are hydrophobic blocks with at least two cyclic monomers selected from the group consisting of glycolide, lactide, 1,3-dioxan-2-one, 5,5-dimethyl-1,3-dioxan-2-one, 1,4-dioxan-2-one, 1,4-dioxepan-2-one, 1,5-dioxepan-2-one, each B-block having a number average molecular weight (M) of between 400 and 2000 Daltons, determined with size exclusion chromatography; and wherein 25% to 100% of the polymer hydroxyl end-groups are covalently modified with at least one derivative of a C-Cfatty acid. The invention also relates to compositions with such polymers and the use thereof.

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Groningen, Netherlands

Mike De Leeuw