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AMORPHOUS SOLID DISPERSIONS OF LORCASERIN HYDROCHLORIDE

IP.com Disclosure Number: IPCOM000236417D
Publication Date: 2014-Apr-24
Document File: 6 page(s) / 193K

Publishing Venue

The IP.com Prior Art Database

Abstract

Reported herein are amorphous solid dispersions of lorcaserin hydrochloride and processes for their preparation.

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AMORPHOUS SOLID DISPERSIONS OF LORCASERIN HYDROCHLORIDE

Abstract

Reported herein are amorphous solid dispersions of lorcaserin hydrochloride and processes for their preparation.

The amorphous solid dispersions of lorcaserin hydrochloride reported herein are prepared by dissolving lorcaserin hydrochloride and one or more pharmaceutically acceptable carrier(s) in one or more solvent(s) at temperatures ranging from ambient temperature to reflux temperature.  Examples of pharmaceutically acceptable carriers include hydroxypropyl-β-cyclodextrine (HPβCD), polyvinyl pyrrolidone (PVP), polyethylene glycol (PEG), polyvinyl alcohol (PVA), crospovidone, starch, pectin, mannan, gelatin, gum arabic, dextrins, cyclodextrins, agar, polyoxysorbitan fatty acid esters, alginates, and cellulose derivatives.  Examples of solvents include alcohols, carboxylic acids, chlorinated hydrocarbons, ketones, amides, sulphoxides, ethers, water, and mixtures thereof.

Methods

X-ray diffraction patterns were recorded using a PANalytical® X'Pert PRO with X'Celerator® as the detector, 0.02 as step size, and 3-40° 2θ as range, using CuKα radiation at 45kV.

Spray drying was carried out using a Buchi® Mini Spray Dryer B-290; inlet temperature was maintained at about 100°C to 120°C and outlet temperature was maintained at about 50°C to 90°C.

EXAMPLES

Comparative Example: Preparation of lorcaserin hydrochloride by spray drying

Lorcaserin hydrochloride (2.5 g) was dissolved in methanol (50 mL) at about 65°C.  The solution was charged into a spray dryer maintained at an inlet temperature of about 120°C and outlet temperature of about 70°C, followed by drying in a vacuum tray dryer at about 55°C for about 6 hours.

Yield: 19.16%

WORKING EXAMPLES

Example 1: Preparation of amorphous solid dispersion of lorcaserin hydrochloride with hydroxypropyl-β-cyclodextrine

Method 1:

Lorcaserin hydrochloride (0.25 g) and hydroxypropyl-β-cyclodextrine (0.25 g) were dissolved in methanol (20 mL) at about 65°C.  Methanol was distilled-off using a rotary evaporator at about 65°C under reduced pressure, followed by drying in a vacuum tray dryer at about 60°C for about 6 hours to obtain an amorphous solid dispersion of lorcaserin hydrochloride with hydroxypropyl-β-cyclodextrine.

Yield: 58.0%

Method 2:

Lorcaserin hydrochloride (2.0 g) and hydroxypropyl-β-cyclodextrine (2.0 g) wer...