Pharmaceutical composition
Inventors
Roberge, Christophe • RECH, Anthony • CROS, Jean-Manuel • ABBASSI, Myriam • LÓPEZ-NORIEGA, Adolfo • PEBREL, Lea • Petit, Audrey • SERINDOUX, Juliette
Assignees
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Publication Number
US-11612563-B2
Publication Date
2023-03-28
Expiration Date
Abstract
The present invention provides a biodegradable drug delivery composition comprising a mixture of at least two block copolymers taken among triblock and diblock copolymers comprising: (a) a biodegradable triblock copolymer having the formula: Av-Bw-Ax wherein A is a polyester and B is polyethylene glycol and v and x are from 1 to 3,000 and w is from 3 to 300 and v=x or v≠x; (b) a biodegradable diblock copolymer having the formula: Cy-Az wherein A is a polyester and C is an end-capped polyethylene glycol and y and z are the number of repeat units with y=2 to 250 and z=1 to 3,000; wherein the weight ratio between (a) and (b) is 1:19 to 5:1; and for at least one of the copolymers according to (a) or (b) A is poly(ε-caprolactone-co-lactide); and (c) at least one pharmaceutically active ingredient.
Core Innovation
The disclosure relates to biodegradable drug delivery compositions comprising a mixture of block copolymers that include biodegradable triblock copolymers of the formula A_v–B_w–A_x and biodegradable diblock copolymers of the formula C_y–A_z. In these copolymers, A is a polyester and B is polyethylene glycol, while C is an end-capped polyethylene glycol. The compositions are defined by repeat-unit ranges for v, w, x, y, and z, and by a weight ratio between the triblock and diblock components.
In at least one copolymer, the polyester A is selected from poly(ε-caprolactone-co-lactide) (PCLA). The mixture comprises at least one triblock and at least one diblock copolymer, and the triblock:diblok weight ratio is specified as 1:19 to 5:1. The formulation further includes at least one pharmaceutically active ingredient and at least one pharmaceutically acceptable solvent.
The technical finding described for these compositions is that the presence of PCLA increases drug release rate by modulating release kinetics while maintaining formulation physical parameters such as injectability and viscosity. The document describes polymer and active-ingredient loading ranges together with example contexts including injectable liquids forming in situ depots and rod implant or other depot-forming administration contexts.
Claims Coverage
The independent claims cover biodegradable drug delivery compositions that combine specified biodegradable polyester–PEG triblock and end-capped-PEG polyester diblock copolymers with a defined weight ratio, and further require at least one pharmaceutically active ingredient and a pharmaceutically acceptable solvent. Across the independent claims, the inventive features are quantified by repeat-unit ranges, include PCLA as a selected polyester A in at least one copolymer, and constrain the solvent to either a general pharmaceutically acceptable solvent or to a listed set of organic solvents.
Mixture of biodegradable triblock and diblock block copolymers with defined weight ratio
The composition includes one or more biodegradable triblock copolymers of A_v–B_w–A_x and one or more biodegradable diblock copolymers of C_y–A_z, wherein the weight ratio between (a) and (b) is 1:19 to 5:1, and wherein the mixture comprises at least one (a) and at least one (b).
PCLA selection for polyester block A in at least one copolymer
The polyester A in at least one copolymer as defined in (a) or (b) is selected from poly(ε-caprolactone-co-lactide) (PCLA).
Biodegradable composition including pharmaceutically active ingredient and pharmaceutically acceptable solvent
The mixture comprises at least one pharmaceutically active ingredient and at least one pharmaceutically acceptable solvent.
Specified organic solvent selection for the composition
The organic solvent is selected from benzyl alcohol, benzyl benzoate, dimethyl isosorbide (DMI), dimethyl sulfoxide (DMSO), ethyl acetate, ethyl benzoate, ethyl lactate, glycerol formal, methyl ethyl ketone, methyl isobutyl ketone, N-ethyl-2-pyrrolidone, N-methyl-2-pyrrolidinone (NMP), pyrrolidone-2, tetraglycol, triacetin, tributyrin, tripropionin (tripro), or mixtures thereof.
The independent claims collectively require a biodegradable drug delivery composition formed from specified biodegradable polyester–PEG triblock and end-capped-PEG polyester diblock copolymers combined at a defined triblock:diblok weight ratio, with polyester A selected to include PCLA in at least one copolymer. Each independent claim further requires at least one pharmaceutically active ingredient and an appropriate solvent, with one independent claim expressly restricting the solvent to a listed group of organic solvents.
Stated Advantages
Presence of PCLA increases drug release rate by modulating release kinetics while maintaining formulation physical parameters such as injectability and viscosity.
Documented Applications
Injectable liquids forming in situ depots.
Depot-forming administration contexts including implants/solid or rod implants.
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