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Publication Number
US-9023897-B2
Publication Date
2015-05-05
Expiration Date
Abstract
A biodegradable drug delivery compositions comprising a triblock copolymer containing a polyester and a polyethylene glycol and a diblock copolymer containing a polyester and an end-capped polyethylene glycol, as well as a pharmaceutically active principle is disclosed.
Core Innovation
The invention relates to a biodegradable drug delivery composition that combines a biodegradable triblock copolymer of poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) with a biodegradable diblock copolymer of methoxy poly(ethylene glycol)-poly(lactic acid). The triblock copolymer and diblock copolymer are constrained by defined repeat-unit ranges and a defined triblock:diblock ratio in an aqueous environment, and the composition is insoluble in an aqueous environment.
The composition includes at least one pharmaceutically active principle. In one described embodiment, the triblock copolymer is present in an amount of 3.0% to 45% (w/w) of the total composition, the diblock copolymer is present in an amount of 8.0% to 50% (w/w) of the total composition, and the pharmaceutically active principle is present in an amount of 1% to 20% (w/w) of the total composition.
The disclosed formulations are injectable liquid formulations that form an implant in the body, and also include small solid particles, rod implants, and spatial formulations. The described preparation involves dissolving the biodegradable triblock and diblock copolymers in an organic solvent, adding at least one pharmaceutically active principle, and evaporating the solvent, producing injectable/in situ-forming biodegradable implant-like delivery.
Claims Coverage
The independent claims in the partial content are clm-00001 and clm-00002. The claim coverage centers on an aqueous-insoluble biodegradable drug delivery composition using PLA-PEG-PLA triblock and methoxy PEG-PLA diblock copolymers with defined repeat-unit ranges, a constrained triblock:diblock ratio, and at least one pharmaceutically active principle; clm-00002 further specifies weight-percent amounts for the polymers and the active principle.
Biodegradable PLA-PEG-PLA/PEG-PLA insoluble drug composition with constrained triblock:diblock ratio
A biodegradable drug delivery composition comprising a biodegradable triblock copolymer poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) with repeat-unit ranges v and x from 24 to 682 (with v=x or v≠x), a biodegradable diblock copolymer methoxy poly(ethylene glycol)-poly(lactic acid) with repeat-unit ranges y from 3 to 45 and z from 7 to 327, a triblock copolymer to diblock copolymer ratio of 1:3 to 1:8 or 1:1 to 1:19 or 3:2 to 1:19, wherein the composition is insoluble in an aqueous environment, and at least one pharmaceutically active principle.
Weight-percent constrained biodegradable triblock/diblock insoluble composition with active loading range
A biodegradable drug delivery composition comprising a biodegradable triblock copolymer present in an amount of 3.0% to 45% (w/w) of the total composition having poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) repeat-unit ranges v and x from 24 to 682 (with v=x or v≠x), a biodegradable diblock copolymer present in an amount of 8.0% to 50% (w/w) of the total composition having methoxy poly(ethylene glycol)-poly(lactic acid) repeat-unit ranges y from 3 to 45 and z from 7 to 327, a triblock copolymer to diblock copolymer ratio of 1:3 to 1:8 or 1:1 to 1:19 or 3:2 to 1:19, wherein the composition is insoluble in an aqueous environment, and at least one pharmaceutically active principle present in an amount of 1% to 20% (w/w) of the total composition.
Across clm-00001 and clm-00002, the claims are directed to an aqueous-insoluble biodegradable drug delivery composition defined by specified PLA-PEG-PLA triblock and methoxy PEG-PLA diblock copolymers, constrained triblock:diblock ratios, and at least one pharmaceutically active principle, with clm-00002 additionally fixing weight-percent amounts.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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