# US 9,040,695 B2 · Acid addition salts of risperidone and pharmaceutical compositions thereof

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- Number: US 9,040,695 B2
- Document ID: US9040695B2
- Status: Granted
- Kind: B2
- Application number: 14/114,379
- Filed: 2012-04-25
- Published: 2014-02-13
- Granted: 2015-05-26
- Earliest claimed: 2011-04-26
- Assignees: Torrent Pharmaceuticals Limited
- Applicants: Sunil Sadanand Nadkarni; Arunkumar Gupta; Manish Parikh; Jaya Abraham; Vivek Mishra
- Inventors: Sunil Sadanand Nadkarni; Arunkumar Gupta; Manish Parikh; Jaya Abraham; Vivek Mishra
- Web page: https://patentgrep.com/patent/US9040695B2

## CPC

- C07D 471/04: Ortho-condensed systems
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- C07D 401/14: containing three or more hetero rings
- C07D 403/14: containing three or more hetero rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to a novel acid addition salt of risperidone, wherein acid counterion is selected from the group consisting of pamoic acid, caproic acid, cypionic acid, decanoic acid, camphor sulfonic acid, enanthic acid, palmitic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, levulinic acid and valeric acid, a process for the preparation and pharmaceutical composition comprising the same. Further, the invention relates to the use of said pharmaceutical composition comprising the acid addition salt of risperidone in the treatment of patient suffering from psychotic disorders.

## Claims

### Claim 1

A compound which is Risperidone hemipamoate.

### Claim 2 (depends on 1)

Risperidone hemipamoate according to claim 1 in crystalline form T1 characterized by a powder X-ray diffraction pattern having characteristic peaks at about 6.51, 7.26, 9.26, 9.81, 13.55, 16.00, 19.52, 20.82 and 23.6±0.2 degree two theta, which is substantially in accordance with FIG. 1.

### Claim 3 (depends on 2)

A process for the preparation of risperidone hemipamoate in crystalline form T1 according to claim 2, comprises:
a) providing solution of risperidone in methanol;
b) reacting above solution of step a) with pamoic acid solution prepared in suitable solvent; and
c) isolating risperidone hemipamoate crystalline Form-T1.

### Claim 4 (depends on 1)

Risperidone hemipamoate according to claim 1 in crystalline form T2 characterized by a powder X-ray diffraction pattern having characteristic peaks at about 5.24, 5.94, 6.92, 8.81, 15.50, 16.23, 17.68, 18.19, 21.84 and 22.21±0.2 degree two theta, which is substantially in accordance with FIG. 2.

### Claim 5 (depends on 4)

A process for the preparation of risperidone hemipamoate in crystalline form T2 according to claim 4, comprises:
a) providing solution of risperidone in ethanol;
b) reacting the above solution of step a) with pamoic acid solution prepared in suitable solvent; and
c) isolating risperidone hemipamoate crystalline Form-T2.

### Claim 6 (depends on 5)

The process according to claim 5, wherein suitable solvent is selected from water, methanol, ethanol, n-butanol, isopropanol, iso-butanol, dimethylformamide, tetrahydrofuran, acetone, benzene, ethyl methyl ketone, acetonitrile, toluene, dimethyl sulfoxide, chloroform and ethylacetate.

### Claim 7 (depends on 1)

A pharmaceutical composition comprising a therapeutically effective amount of risperidone hemipamoate according to claim 1 and one or more pharmaceutically acceptable excipients.

### Claim 8

A long acting formulation comprising a therapeutically effective amount of risperidone hemipamoate or mixtures thereof and suitable vehicle for injection.

### Claim 9 (depends on 8)

The long acting formulation according to claim 8, wherein vehicle is selected from biocompatible vehicle or oily vehicle or buffered aqueous vehicle.

### Claim 10 (depends on 8)

The long acting formulation according to claim 8, wherein duration of drug release is about 7 days to 1 month.

### Claim 11 (depends on 8)

The long acting formulation according to claim 8, wherein risperidone hemipamoate is in crystalline Form T1 or T2.

### Claim 12 (depends on 3)

The process according to claim 3, wherein suitable solvent is selected from water, methanol, ethanol, n-butanol, isopropanol, iso-butanol, dimethylformamide, tetrahydrofuran, acetone, benzene, ethyl methyl ketone, acetonitrile, toluene, dimethylsulfoxide, chloroform and ethyl acetate.