Patent application EP17164369A (EP), filed 2017-03-31
Publication number: EP3228324A1
Title: HYPROMELLOSE ACETATE SUCCINATE POWDER
Abstract: [0001]    Provided are HPMCAS powder having high solubility when dissolved in a solvent and being capable of suppressing generation of undissolved materials; and a method for producing the powder. More specifically, provided is hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively. Also provided is a method for producing a hypromellose acetate succinate, comprising the steps of: dissolving hypromellose powder in a solvent, esterifying the dissolved hypromellose with succinic anhydride and acetic anhydride in the presence of a catalyst to obtain a reaction mixture, and mixing the reaction mixture with water to precipitate hypromellose acetate succinate, wherein the reaction mixture just before being mixed with the water has a viscosity of from 100 to 200 Pa·s.
IPC codes: A61K  31/   525            A I
A61K  47/    38            A I
A61K   9/    28            A I
Claims: number: 1
text: Hypromellose acetate succinate powder having an average ratio of L to D of from 2.0 to 3.0, wherein L and D mean maximum and minimum diameters of each particle, respectively.
number: 2
text: The hypromellose acetate succinate powder according to claim 1, having a specific surface area of from 2.0 to 5.0 m<2> /g or more.
number: 3
text: The hypromellose acetate succinate powder according to claim 1 or 2, having a loose bulk density of from 0.10 to 0.25 g/mL.
number: 4
text: The hypromellose acetate succinate powder according to any one of claims 1 to 3, comprising 10% by weight or less of component not soluble at 20°C in such a weight of acetone as to be 10 times the weight of the powder.
number: 5
text: A method for producing a composition for solid dispersion, comprising the step of removing a solvent from a solution comprising the hypromellose acetate succinate powder as claimed in any one of claims 1 to 4, a drug and the solvent.
number: 6
text: A method for producing a coating composition, comprising the step of dissolving the hypromellose acetate succinate powder as claimed in any one of claims 1 to 4 in a solvent which is a mixed solution of water and an alcohol, or an aqueous ammonia solution.
number: 7
text: A method for producing a drug-containing particle, comprising:
number: 8
text: A method for producing a solid preparation, comprising:
number: 9
text: The method for producing a solid preparation according to claim 8, wherein the solid preparation is a tablet, a granule or a fine granule.
number: 10
text: A method for producing hypromellose acetate succinate powder, comprising the steps of:
Office action: search_report, dated 2017-10-11
Rejection reasons: novelty_epc_54
inventive_step_epc_56
Prior art cited: ref_id: JPH07109219A
ref_type: patent
severity: background
ref_id: JPH08245423A
ref_type: patent
severity: background
ref_id: - "Japanese Pharmacopoeia", article "Hypromellose"
ref_type: npl
severity: background
ref_id: - "Japanese Pharmacopoeia"
ref_type: npl
severity: background
ref_id: CA2934231A1
ref_type: patent
severity: background
ref_id: EP2837391A1
ref_type: patent
severity: background
ref_id: - ROWE R. ET AL: "Handbook of Pharmaceutical Excipients, fifth edition", 1 January 2006, PHARMACEUTICAL PRESS AND AMERICAN PHARMACISTS ASSOCIATION, London/Washington, ISBN: 0-85369-618-7, article "Hypromellose Acetate Succinate", pages: 350 - 353, XP002772538
ref_type: npl
severity: background
ref_id: - SARODE ASHISH L ET AL: "Stability assessment of hypromellose acetate succinate (HPMCAS) NF for application in hot melt extrusion (HME)", CARBOHYDRATE POLYMERS, vol. 101, 14 September 2013 (2013-09-14), pages 146 - 153, XP028790537, ISSN: 0144-8617, DOI: 10.1016/J.CARBPOL.2013.09.017
ref_type: npl
severity: background
ref_id: - ZIMMERMANN I.: "Pharmazeutische Technologie", 1998, SPRINGER VERLAG, Berlin, Heidelberg, NewYork, ISBN: 3-540-63944-6, article "Direkt abbildende optische Messverfahren", pages: 246 - 247, XP002772539
ref_type: npl
severity: background
ref_id: EP2837391
ref_type: patent
severity: obviousness
ref_id: CA2934231
ref_type: patent
severity: obviousness
ref_id: - "Hypromellose Acetate Succinate", Rowe R. et al, Handbook of Pharmaceutical Excipients, fifth edition, London/Washington, Pharmaceutical Press and American Pharmacists Association, (20060101), pages 350 - 353, ISBN 0-85369-618-7, XP002772538 [X] 1-10 * the whole document * [Y] 1-10
ref_type: npl
severity: novelty_destroying
ref_id: - SARODE ASHISH L ET AL, "Stability assessment of hypromellose acetate succinate (HPMCAS) NF for application in hot melt extrusion (HME)", CARBOHYDRATE POLYMERS, (20130914), vol. 101, doi:10.1016/J.CARBPOL.2013.09.017, ISSN 0144-8617, pages 146 - 153, XP028790537 [X] 1 * figure 7 *
ref_type: npl
severity: novelty_destroying
ref_id: - "Direkt abbildende optische Messverfahren", Zimmermann I., Pharmazeutische Technologie, Berlin, Heidelberg, NewYork, Springer Verlag, (1998), pages 246 - 247, ISBN 3-540-63944-6, XP002772539 [A] 1
ref_type: npl
severity: background
Final disposition: pending (2017-10-11)