Pauline E Leary

US Patent:

20060074059, Apr 6, 2006

Filed:

Aug 25, 2005

Appl. No.:

11/211784

Inventors:

Philip Goliber - Brookfield CT, US
Pauline Leary - Stanfordville NY, US
Helen Danagher - Cambridge, GB
Matthew Hartenstein - Glenmoore PA, US

International Classification:

A61K 31/58
C07J 43/00

US Classification:

514176000, 540107000

Abstract:

The present invention provides stable particles of 3a-hydroxy-21-(1′-imidazolyl)-3β-methoxymethyl-5a-pregnan-20-one (Compound I), which possess and retain a shape and size appropriate for handling and manufacture of large-scale pharmaceutical preparations, even in the absence of further milling. Further provided is a method for obtaining such reproducible, stable particles by subjecting crude Compound I to controlled crystallization conditions comprising slow cooling of a solution of Compound I. Further provided is a pharmaceutical composition of unmilled crystalline Compound I, which does not require milling prior to formulation, and a method of modulating brain excitability using the same.