Crystalline form of tiotropium bromide with lactose

Kristalline Form von Tiotropiumbromid mit Lactose

Forme cristalline de bromure de tiotropium et de lactose

Abstract

A cocrystal of tiotropium bromide and lactose monohydrate is herein disclosed. In the cocrystal the components tiotropium bromide and lactose are preferably present in an almost stoichiometric ratio. Said cocrystal has a a single endothermic event at about 191-3°C determined by DSC. A process for the preparation of the cocrystal is also disclosed. Preferably, the cocrystal has a particle size distribution of D90 < 10µ. The cocrystal is also disclosed for use as medicament, in particular for the treatment of a respiratory complaint, such as chronic obstructive pulmonary disease (COPD), bronchitis, emphysema and asthma. A pharmaceutical composition comprising the cocrystal as active ingredient is also disclosed, in particular for administration by inhalation. In the latter case, said cocrystal has a mean particle size of 0.5 to 10 µm, preferably 1 to 6 µm, more preferably 1.5 to 5 µm.

Claims

Description

Topics

Download Full PDF Version (Non-Commercial Use)

Patent Citations (16)

    Publication numberPublication dateAssigneeTitle
    EP-0418716-A1March 27, 1991Boehringer Ingelheim Kg, BOEHRINGER INGELHEIM INTERNATIONAL GmbHNeue Thienylcarbonsäureester von Aminoalkoholen, ihre Quaternierungsprodukte sowie die Herstellung und Verwendung dieser Verbindungen
    EP-1682542-A1July 26, 2006Boehringer Ingelheim International GmbH, Boehringer Ingelheim Pharma GmbH & Co.KGNouvel anhydrate cristallin a effet anticholinergique
    EP-2201934-A1June 30, 2010CHIESI FARMACEUTICI S.p.A.Tiotropium aerosol formulation products with improved chemical stability
    US-2003087927-A1May 08, 2003Boehringer Ingelheim Pharma KgCrystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
    US-2011257215-A1October 20, 2011Boehringer Ingelheim Pharma GmbH CO.KGNovel co-crystal of tiotropium bromide
    US-6608055-B2August 19, 2003Boehringer Ingelheim Pharma KgCrystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
    US-677423-AJuly 02, 1901George Alfred OwenMail-service system.
    US-6777423-B2August 17, 2004Boehringer Ingelheim Pharma KgCrystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions
    US-7070800-B2July 04, 2006Boehringer Ingelheim Pharma KgInhalable powder containing tiotropium
    US-7694676-B2April 13, 2010Boehringer Ingelheim GmbhDry powder inhaler
    US-7879871-B2February 01, 2011Boehringer Ingelheim International GmbhCrystalline forms of tiotropium bromide
    US-8022082-B2September 20, 2011Boehringer Ingelheim Pharma Gmbh & Co., KgMethod for the administration of an anticholinergic by inhalation
    WO-2006117300-A2November 09, 2006Boehringer Ingelheim International Gmbh, Boehringer Ingelheim Pharma Gmbh & Co. KgFormes cristallines de bromure de tiotropium
    WO-2009007687-A2January 15, 2009Norton Healthcare LimitedAn inhalable medicament
    WO-2010101538-A2September 10, 2010Bilgic MahmutNouvelles formes de cristaux
    WO-2011015882-A2February 10, 2011Generics [Uk] Limited, Mylan India Private LimitedNovel anhydrate

NO-Patent Citations (2)

    Title
    HYUNNSOOK KO ET AL., BULL. KOREAN CHEM. SOC., vol. 26, no. 2, 2005, pages 2001 - 6
    ZHENGUANG LIN ET AL., SPECTROCHIMICA ACTA PART A, vol. 75, 2010, pages 1159 - 1162

Cited By (0)

    Publication numberPublication dateAssigneeTitle