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1. (WO2007011349) NOVEL GRANULATION PROCESS AND GRANULATE PRODUCED THEREFROM
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/011349 International Application No.: PCT/US2005/025326
Publication Date: 25.01.2007 International Filing Date: 15.07.2005
IPC:
A61K 9/00 (2006.01) ,A61K 9/16 (2006.01) ,A61K 31/542 (2006.01) ,A61K 31/5415 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
16
Agglomerates; Granulates; Microbeadlets
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542
ortho- or peri-condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
5415
ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
Applicants:
TEVA PHARMACEUTICAL INDUSTRIES LTD. [IL/IL]; 5 Basel Street P.O. Box 3190 49131 Petah Tiqva, IL (AE, AG, AL, AM, AT, AU, AZ, BA, BE, BF, BG, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GW, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, SY, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, YU, ZA, ZM, ZW)
TEVA PHARMACEUTICAL USA, INC. [US/US]; 1090 Horsham Road P.O. Box 1090 North Wales, PA 19454-1090, US (BB)
ZALIT, Ilan [IL/IL]; IL (UsOnly)
HRAKOVSKY, Julia [IL/IL]; IL (UsOnly)
TENENGAUZER, Ruth [IL/IL]; IL (UsOnly)
SHALOM-KLEIN, Sagit [IL/IL]; IL (UsOnly)
Inventors:
ZALIT, Ilan; IL
HRAKOVSKY, Julia; IL
TENENGAUZER, Ruth; IL
SHALOM-KLEIN, Sagit; IL
Agent:
BRAINARD, Charles ; Kenyon & Kenyon One Broadway New York, NY 10004-1050, US
Priority Data:
Title (EN) NOVEL GRANULATION PROCESS AND GRANULATE PRODUCED THEREFROM
(FR) NOUVEAU PROCEDE DE GRANULATION ET GRANULE PRODUIT PAR CE PROCEDE
Abstract:
(EN) One of the objects of the invention relates to a pharmaceutical composition in the form of a granulate, wherein the granulates comprises an active pharmaceutical ingredient (API) having a poor water solubility intimately associated with at least one pharmaceutically acceptable sugar, and optionally or preferably at least one pharmaceutically acceptable excipient other than the at least one pharmaceutically acceptable sugar, wherein the active pharmaceutically ingredient has a water solubility less than about 20 mg/ml. The at least one pharmaceutically acceptable excipient other than the at least one pharmaceutically acceptable sugar is selected from the group consisting of disintegrants, wetting agents, diluents, binders, lubricants, glidants, coloring agents and flavoring agents. The at least one pharmaceutically acceptable sugar is preferably selected from pyranosyl pyranoses, such as lactose. Another object of the invention relates to a process for preparing a pharmaceutical granulate, comprising (a) combining an API having poor water solubility with a solution comprising at least one pharmaceutically acceptable sugar, for example a pyranosyl pyranose such as lactose, and a solvent, and optionally at least one pharmaceutically acceptable excipient other than the at least one pharmaceutically acceptable sugar to form a combined mixture; (b) drying the combined mixture of step (a); and (c) comminuting the product of step (b) to obtain the granulate.
(FR) La présente invention a trait, entre autres, à une composition pharmaceutique sous la forme d'un matière granulée, dans laquelle les granulés comportent un ingrédient pharmaceutique actif présentant une faible solubilité dans l'eau intimement associé à un sucre pharmaceutiquement acceptable, et éventuellement ou préférablement, au moins un excipient pharmaceutiquement acceptable, ledit ingrédient pharmaceutiquement actif présentant une solubilité dans l'eau inférieure à environ 20 mg/ml. Ledit au moins un excipient pharmaceutiquement acceptable autre que ledit au moins un sucre pharmaceutiquement acceptable est choisi parmi le groupe constitué d'agents de désintégration, d'agents de mouillage, de diluants, de liants, de lubrifiants, d'agents de glissement, d'agents colorants et d'aromatisants. Ledit un sucre pharmaceutiquement acceptable est choisi de préférence parmi les pyranoses de pyranosyle tels que le lactose. L'invention a également trait à un procédé pour la préparation d'un granulé pharmaceutique, comprenant: (a) la combinaison d'un ingrédient pharmaceutique actif présentant une faible solubilité dans l'eau avec une solution d'au moins un sucre pharmaceutiquement acceptable, par exemple un pyranose de pyranosyle telle que le lactose, et un solvant, et éventuellement au moins un excipient pharmaceutiquement acceptable autre que ledit au moins un sucre pharmaceutiquement acceptable pour former un mélange combiné; (b) le séchage du mélange combiné de l'étape (a); et (c) la fragmentation du produit de l'étape (b) pour obtenir le granulé.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
IL188177EP1793801JP2008540644CN101222911CA2614468IN89/DELNP/2008