| 主权项 |
1. A pharmaceutical composition in the form of a tablet comprising the following components
a) hot melt extrudate of 30-60% of a compound of formula I wherein R is lower alkyl, lower alkoxy, halogen or trifluoromethyl R1 is halogen or hydrogen; R2 and R2′ are each independently hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R4 is R5 is hydrogen, C3-6-cycloalkyl, benzyl, or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, —(CH2)nCOO—(R5), —N(R5)CO-lower alkyl, hydroxy-lower alkyl, —(CH2)nCN, —(CH2)nO(CH2)nOH, —CHO or a 5- or 6-membered heterocyclic ring containing from 1 to 4 heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur, and with one of the carbon atoms in said ring being unsubstituted or substituted with an oxo group, which heterocyclic ring is directly bonded or bonded via an alkylene group to the remainder of the molecule; is a cyclic tertiary amine which may contain one additional heteroatom selected from the group consisting of oxygen, nitrogen, or sulfur, wherein any sulfur present in the ring is thio or can be oxidized to sulfoxide or sulfur dioxide by which said cyclic tertiary amine is directly attached to the remainder of the molecule; X is —C(O)N(R5)— or —N(R5)C(O)—; n and p are each independently 1 to 4; or pharmaceutically acceptable acid addition salts thereof and 10-20% of a water soluble poloxamer;b) a filler20-30%;c) a disintegrant 1-10%;d) processing aid 0-5%;e) glidant 0-5%, and optionallyf) immediate release film coating system 2-5% of the tablet weight; andg) purified water, wherein the tablet contains 400 mg of the compound of Formula I. |
