Global Patent Index - EP 2590627 A1

EP 2590627 A1 20130515 - ALISKIREN IN FORM OF A SOLID DISPERSION

Title (en)

ALISKIREN IN FORM OF A SOLID DISPERSION

Title (de)

ALISKIREN IM FORM EINER FESTEN DISPERSION

Title (fr)

ALISKIRÈNE SOUS FORME D'UNE DISPERSION SOLIDE

Publication

EP 2590627 A1 20130515 (EN)

Application

EP 11718287 A 20110419

Priority

  • EP 10004251 A 20100421
  • EP 2011001990 W 20110419
  • EP 11718287 A 20110419

Abstract (en)

[origin: EP2382967A1] A pharmaceutical intermediate comprises aliskiren base and substrate. The aliskiren base is present as a solid dispersion. Independent claims are included for: (1) preparation of the intermediate containing aliskiren and substrate, comprising dissolving aliskiren base in a solvent or mixture of solvents and contacting the solution with a substrate, removing the solvent or mixture of solvents, and optionally granulating the obtained mixture; (2) a pharmaceutical formulation containing aliskiren base in the form of an intermediate, and optionally pharmaceutical excipient(s); and (3) a tablet containing aliskiren base (50-500 mg) and having hardness of 50-250 N, friability of less than 5% and content uniformity of 95-105%. ACTIVITY : Hypotensive; Cardiant. No biological data given. MECHANISM OF ACTION : None given.

IPC 8 full level

A61K 9/14 (2006.01); A61K 9/20 (2006.01); A61K 31/165 (2006.01)

CPC (source: EP)

A61K 9/143 (2013.01); A61K 9/146 (2013.01); A61K 9/2077 (2013.01); A61K 31/165 (2013.01)

Citation (search report)

See references of WO 2011131348A1

Citation (examination)

  • J.M SONNERGAARD: "A critical evaluation of the Heckel equation", INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 193, no. 1, 1 December 1999 (1999-12-01), pages 63 - 71, XP055110937, ISSN: 0378-5173, DOI: 10.1016/S0378-5173(99)00319-1
  • ROBERTS R J ET AL: "Brittle/ductile behaviour in pharmaceutical materials used in tabletting", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL, vol. 36, no. 2-3, 1 May 1987 (1987-05-01), pages 205 - 209, XP025888794, ISSN: 0378-5173, [retrieved on 19870501], DOI: 10.1016/0378-5173(87)90157-8
  • CHATTERJEE L ET AL: "Mechanical properties of excipients do not affect polymer matrix formation", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL, vol. 384, no. 1-2, 15 January 2010 (2010-01-15), pages 87 - 92, XP026790373, ISSN: 0378-5173, [retrieved on 20091009]
  • SARSVATKUMAR PATEL ET AL: "Mechanistic investigation on pressure dependency of Heckel parameter", INTERNATIONAL JOURNAL OF PHARMACEUTICS, ELSEVIER BV, NL, vol. 389, no. 1, 10 January 2010 (2010-01-10), pages 66 - 73, XP028308322, ISSN: 0378-5173, [retrieved on 20100118], DOI: 10.1016/J.IJPHARM.2010.01.020

Designated contracting state (EPC)

AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

DOCDB simple family (publication)

EP 2382967 A1 20111102; CA 2807374 A1 20111027; EP 2590627 A1 20130515; WO 2011131348 A1 20111027

DOCDB simple family (application)

EP 10004251 A 20100421; CA 2807374 A 20110419; EP 11718287 A 20110419; EP 2011001990 W 20110419