Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12128132-B2
Publication Date
2024-10-29
Expiration Date
Abstract
The present invention is directed to methods of treating psychiatric diseases and disorders comprising administering to a subject in need thereof an injectable formulation comprising risperidone, triblock and diblock copolymers wherein the concentration of the risperidone is 250-400 mg/mL and injection volume is 1 mL or less.
Core Innovation
The invention relates to injectable risperidone drug delivery formulations for treating a psychiatric disease or disorder in a subject. The disclosed approach subcutaneously administers a pharmaceutical formulation with about 250-400 mg/mL risperidone or a pharmaceutically acceptable salt in a low injection volume of about 0.1 mL to 0.8 mL, using insoluble biodegradable triblock and diblock copolymers.
The formulation is based on an insoluble in an aqueous environment biodegradable triblock copolymer poly(lactic acid)v-poly(ethylene glycol)w-poly(lactic acid)x and a biodegradable diblock copolymer methoxy poly(ethylene glycol)y-poly(lactic acid)z. The copolymers are defined by repeat unit ranges and by ratios of triblock:diblock, together with specified w/w % copolymer loading in the formulation.
The disclosed compositions are intended to provide long release over about 21-90 days while using a regimen without a loading dose or supplemental oral risperidone. The document further describes excisability of in situ formed implants and provides in vitro release model support, injectability measurement concepts, and preclinical and clinical study support including excision feasibility and PK/PD and safety/tolerability data.
Claims Coverage
The partial content provides two independent claims. Across the independent claims, the core coverage is the defined risperidone concentration and injection volume combined with an insoluble biodegradable triblock/diblock copolymer system at specified repeat-unit ranges, ratios, and w/w % loadings.
Subcutaneous treating regimen with defined low-dose frequency and formulation volume
A method of treating a psychiatric disease or disorder in a subject comprising subcutaneously administering, no more than once every 21 days, about 0.1 mL to 0.8 mL of a pharmaceutical formulation comprising risperidone or a pharmaceutically acceptable salt at about 300-400 mg/mL, together with an insoluble biodegradable triblock copolymer and an insoluble biodegradable diblock copolymer at defined repeat-unit ranges, copolymer ratios, and w/w % loadings.
Injectable risperidone pharmaceutical formulation with insoluble biodegradable triblock/diblock copolymer system
A pharmaceutical formulation comprising about 0.1 mL to 0.8 mL of risperidone or a pharmaceutically acceptable salt at about 300-400 mg/mL, combined with a biodegradable triblock copolymer and a biodegradable diblock copolymer defined by repeat-unit ranges, with a triblock:diblock ratio of 1:3 to 1:8 or 1:1 to 1:19 or 3:2 to 1:19, wherein the copolymer mixture is insoluble in an aqueous environment and includes specified triblock, diblock, and total copolymer amounts for use in treating a psychiatric disease or disorder.
Across the independent claims, the inventive concept is concentrated on subcutaneous injectable risperidone at about 300-400 mg/mL in about 0.1-0.8 mL, formulated with specified insoluble biodegradable triblock and diblock copolymers. Coverage is defined by the copolymer repeat-unit ranges, triblock:diblock ratios, and copolymer loading w/w % limits, with a method claim further constraining the dosing frequency to no more than once every 21 days.
Stated Advantages
Long release over about 21-90 days.
Low initial burst.
No loading dose and no supplemental oral risperidone.
Excisability of in situ formed implants.
Documented Applications
Treating a psychiatric disease or disorder in a subject using subcutaneous administration.
Use of the specified injectable risperidone formulation for treating a psychiatric disease or disorder.
Interested in licensing this patent?