Sustained delivery formulations of risperidone compound

Patent metadata

Field	Value
Publication number	US-11712475-B2
Application number	US-202117237207-A
Country	US
Kind code	B2
Filing date	Apr 22, 2021
Priority date	May 25, 2007
Publication date	Aug 1, 2023
Grant date	Aug 1, 2023

Abstract

The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating to delusional psychosis, schizophrenia, bipolar disorder, psychotic depression, obsessive-compulsion disorder, Tourette syndrome, and autistic spectrum disorders. The sustained release delivery system includes a flowable composition containing risperidone, a metabolite, or a prodrug thereof and an implant containing risperidone, a metabolite, or a prodrug thereof. The flowable composition may be infected into tissue whereupon it coagulates to become a solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite or a prodrug thereof.

First claim

What is claimed is:

1. A method of treating schizophrenia in a subject in need thereof, the method comprising subcutaneously injecting the subject with a composition comprising about 15 wt % of risperidone base in a solution comprising: (i) about 45 wt % of an 80/20 poly(DL-lactide-co-glycolide) having a carboxy terminal group; and (ii) about 55 wt % of N-methyl-2-pyrrolidone.

2. The method of claim 1 , wherein the composition comprises 15 wt % of risperidone base in a solution comprising: (i) 45 wt % of an 80/20 poly(DL-lactide-co-glycolide) having a carboxy terminal group; and (ii) 55 wt % of N-methyl-2-pyrrolidone.

3. The method of claim 1 , wherein the composition comprises about 90 mg or about 120 mg of risperidone base.

4. The method of claim 1 , wherein the composition comprises about 90 mg of risperidone base.

5. The method of claim 1 , wherein the composition comprises about 120 mg of risperidone base.

6. The method of claim 1 , wherein the copolymer has an average molecular weight from about 10,000 Daltons to about 45,000 Daltons.

7. The method of claim 1 , wherein the copolymer has an average molecular weight from about 15,000 Daltons to about 40,000 Daltons.

8. The method of claim 1 , comprising subcutaneously injecting the subject with the composition once per month.

9. The method of claim 1 , wherein the subject is not administered a supplemental daily oral dose of risperidone.

10. The method of claim 1 , wherein the subject is not administered a supplemental daily oral dose of risperidone for the first twenty-one days of the method of treating schizophrenia.

11. The method of claim 1 , wherein the method provides therapeutic plasma risperidone levels immediately after injection.

12. The method of claim 1 , wherein the method provides steady-state risperidone plasma levels from four to six weeks.

Assignees

• Indivior Uk Ltd

Inventors

• Dadey Eric
• Li Qi
• Lindemann Christopher M

Classifications

• A61K47/34 Primary

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title

• A61K9/0024

  Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L) · CPC title

• A61K31/519

  ortho- or peri-condensed with heterocyclic rings · CPC title

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title

• A61K47/32

  Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} · CPC title