【正文】
(德溫特領(lǐng)域) PA (LIPH ) LIPHA LYONNAISE IND PHARM (MERE ) MERCK PATENT GMBH (專利權(quán)人) IN GIET P; HULOT T; MICHEL D; SASLAWSKI O (發(fā)明人) PN FR2775188 A1 19990827 DW199943 A61K47/36 058pp (專利號) WO9942086 A1 19990826 DW199943 A61K9/16 Eng 000pp DS BE CY EA FR GR IE IT MC NL OA SZ (EP指定國) PR FR19980002143 19980223 (優(yōu)先項) IC A61K9/16 。 A61K9/20 。 A61K9/22 。 A61K9/48 。 A61K9/52 。 A61K31/155 。 A61K31/19 。 A61K47/14 。 A61K47/26 。 A61K47/36 (IPC號) MC A10E07C A10E08A A12V01 B04C03C B05A01A B05B01E B05B01F B05B01G B12M11C (手工代碼) A01 [001] 018 。 R00351 G1558 D01 D23 D22 D31 D42 D50 D73 D82 F47 。 P8004 P0975 P0964 D01 D10 D11 D50 D82 F34 。 P0055 。 H0000 。 M9999 M2153R 。 M9999 M2200 。 M9999 M2186 (塑料代碼)(以下略) M1 [03] H4 H402 H482 H5 H589 H8 M280 M312 M323 M332 M342 M383 M393 M423 M431 M510 M520 M530 M540 M620 M782 M904 M905 M910 Q120 R031。 R02044K R02044M。 2044U (化學(xué)代碼)(以下略) DR 2044U (德溫特登記號) AP FR19980002143 19980223。 WO1999EP00994 19990216 (申請項) XIC A61K009/16 。 A61K009/20 。 A61K009/22 。 A61K009/48 。 A61K009/52 。 A61K031/155 。 A61K031/19 。 A61K047/14 。 A61K047/26 。 A61K047/36 (交叉檢索用IPC號) IW ORAL COMPOSITION IMPROVE ABSORB GASTRO TRACT CONTAIN ABSORB PROMOTE BALANCE (標引詞) AB FR2775188 NOVELTY Medicaments for oral administration having hydrophilic or ionizable active ingredients, an absorption promoter having an HLB (hydrophilelipophile balance) of over 8 that is a lipidic material. (新穎性) DETAILED DESCRIPTION The lipidic material is selected from one or more of the following: polysorbates, alkylethers, polyoxyethylene ethers, fatty acid polyoxyethylene esters, fatty acids, fatty alcohols, biliary acids and their salts, 16C alkanol esters with fatty acids, fatty acid 26 OH polyol esters, and polyglycosylated glycerides, in association with one or more pharmaceutical excipients, except for pharmaceutical forms containing captopril. The active material is preferably calcium acamprosate, metformin or metformin hydrochloride. The positions preferably contain 10 % by weight of the absorption promoter, especially 2 %. The positions may further contain an agent to control the kinetic liberation of the active material, especially glycerol palmostearates, glycerol behenates, hydrogenated castor oil, and their mixtures. (發(fā)明詳述) ACTIVITY The bioavailability of calcium acetylhomotaurinate (calcium acamprosate) was determined in beagle dogs using various formulations containing 333 mg of active material. For control purposes, a standard coated tablet formulation was used. Compositions of the invention contained 1 % soya lecithin, or 34 % lactose, together with Gelucire 44/14 (RTM). Taking the control as 100 %, the positions of the invention gave maximum values of plasmatic acamprosate of 138 % and 146 % respectively. (化學(xué)活度) USE Oral positions for absorption in the gastrointestinal tract. (用途) ADVANTAGE The positions give improved transmembrane and paracellular absorption in the gastrointestinal tract. (進步) ( /9) CN RA04V6K RA04V6M R02044K R02044M RA014CK RA014CM RA0MPQK RA0MPQM R14399K R14399M RA0GVGK RA0GVGM 000655501K 000655501M RA013OK RA013OM (化合物登記號) DN AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZW (WO指定國) TI Oral positions having improved absorption in the gastrointestinal tract containing an absorption promoter with a hydrophile (標題)20 / 2