TH14009U - The formula for an aqueous solution of risperidone. - Google Patents

Abstract

------05/10/2017------(OCR) Page 1 of 1. Abstract of the Invention: This invention relates to a chemically and physically stable aqueous solution of risperidone in a slightly acidic solution suitable for oral and injectable administration. It consists of the active ingredient risperidone base or risperidone hydrochloride salt in a solution with a pH in the range of 6.1-7.2. Parabens or BHT (preservative) and sucralose or saccharin (sweetener) can be added to make it suitable for oral administration without compromising the stability of the active ingredient. Oral aqueous solutions of risperidone contain risperidone base ranging from 0.02% (or 0.2 mg/ml) to 0.1% (or 1.0 mg/ml) and risperidone hydrochloride ranging from 0.0218% (or 0.218 mg/ml) to 0.109% (or 1.09 mg/ml) as weight/volume of the solution. Intravenous solutions contain rispericone hydrochloride ranging from 0.109% (or 1.09 mg/ml) to 0.654% (or 6.54 mg/ml) as weight/volume of the solution. ------------ This invention relates to aqueous solution formulations of risperidone that are physicostically stable in slightly acidic solutions, suitable for oral and injectable administration, and contain the active ingredient. Importantly, the solution of risperidone contains either a risperidone base or risperidone hydrochloride salt in the pH range of 6.1-7.2. Parabens, sodium benzoate, or BHT preservatives, along with sucralose or saccharin as sweeteners, can be added to make it suitable for oral administration without compromising the stability of the active ingredient. Oral aqueous risperidone solutions contain risperidone base ranging from 0.02% (or 0.2 mg/ml) to 0.1% (or 1.0 mg/ml) by weight/volume of the solution. Intravenous solutions contain risperidone hydrochloride ranging from 0.109% (or 1.09 mg/ml) to 1.09% (or 10.9 mg/ml) by weight/volume of the solution.

Claims (4)

------05/10/2017------(OCR) Page 1 of 1 page. Claims 1. An aqueous solution formulation of risperidone suitable for injection or oral administration, consisting of water and risperidone base or rispericone hydrochloride salt, with the characteristic that the solution is maintained at an optimal pH of 6.1 to 7.2. 2. An aqueous solution formulation of risperidone according to claim 1, in which the formulation suitable for oral administration contains risperidone base in the range of 0.02% (or 0.2 mg/ml) to 0.1% (or 1.0 mg/ml) by weight/volume of the total solution. 3. An aqueous solution formulation of risperidone according to claim 1, in which the formulation suitable for oral administration contains... The amount of risperidone hydrochloride is in the range of 0.0218% (or 0.218 mg/ml) to 0.109% (or 1.09 mg/ml) as weight by volume of the solution. 4. An aqueous solution formulation of risperidone according to claim 1 where the formulation suitable for injection contains risperidone hydrochloride in the range of 0.109% (or 1.09 mg/ml) to 0.654% (or 6.54 mg/ml) as weight by volume of the solution. ------------ Revised 27/03/2017 (13/03/2017) 1. An aqueous solution formulation of risperidone suitable for injection or oral administration consisting of water and risperidone base or risperidone hydrochloride salt, with specific characteristics of the solution. 1. The aqueous solution formulation of risperidone according to Patent 1, where the formulation suitable for oral administration contains risperidone base in the range of 0.02% (or 0.2 mg/ml) to 0.1% (or 1.0 mg/ml) by weight/volume of the solution. 2. The aqueous solution formulation of risperidone according to Patent 1, where the formulation suitable for oral administration contains risperidone hydrochloride in the range of 0.0218% (or 0.218 mg/ml) to 0.109% (or 1.09 mg/ml) by weight/volume of the solution. 3. The aqueous solution formulation of risperidone according to Patent 1, where the formulation suitable for injection contains... Risperidone hydrochloride concentrations ranged from 0.109% (or 1.09 mg/ml) to 0.654% (or 6.54 mg/ml), expressed by weight to volume of the solution. 1. An aqueous formulation of risperidone suitable for injection or oral administration consists of water and a risperidone base or risperidone hydrochloride salt. The specific characteristic of such a solution is that the pH is maintained at an optimal level, i.e., in the range of 6.1 to 7.2. 2. An aqueous solution formulation of risperidone according to Patent 1 in which the formulation suitable for oral administration contains risperidone base in the range of 0.02% (or 0.2 mg/ml) to 0.1% (or 1.0 mg/ml) by weight/volume of the solution. 3. An aqueous solution formulation of risperidone according to Patent 1 in which the formulation suitable for oral administration contains risperidone hydrochloride in the range of 0.0218% (or 0.218 mg/ml) to 0.218% (or 2.18 mg/ml) by weight/volume of the solution. 4. An aqueous solution formulation of risperidone pursuant to claim 1, in which the appropriate formulation for injection contains risperidone hydrochloride in the range of 0.109% (or 1.09 mg/ml) to 1.09% (or 10.9 mg/ml) by weight/volume of the solution.