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PHARMACEUTICAL COMPOSITIONS CONTAINING A WATER-Insoluble ANTipsychotic PRODUCT AND SORBITE COMPLEXES

机译:包含水不溶性抗精神病药和山梨酸酯复合物的药物组合物

摘要

1. A pharmaceutical composition comprising (a) a water-insoluble antipsychotic agent; (b) esters of sorbitol and carboxylic acid, where the carboxylic acid contains 4-20 carbon atoms; (c) a polyoxyethylene derivative of esters of sorbitol and carboxylic acid, where the carboxylic acid contains 8 -14 carbon atoms; and (d) an aqueous filler; where the composition forms an aqueous, flocculated, injectable suspension. The pharmaceutical composition according to claim 1, wherein the water-insoluble antipsychotic is aripiprazole, a compound of formula 1 or a compound of formula II, or pharmaceutically acceptable salts thereof, hydrates or solvates of which R is absent and R is —CHOC (O) R, —CHOC (O) OR, —CHOC (O) N (R) or —C (O) R; or R is absent and R is —CHOC (O) R, —CHOC (O) OR, —CHOC (O) N (R) or —C (O) R; R is —CHOC (O) R, —CHOC (O) OR, —CHOC (O) N (R) or —C (O) R; where each R is independently selected from the group consisting of hydrogen, substituted or unsubstituted aliphatic groups and substituted or ezameschennogo aryl; where each R is selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; wherein is a pharmaceutically acceptable counterion; it is a single or double bond. 3. The pharmaceutical composition according to any one of the above items, wherein the water-insoluble antipsychotic agent is compound A-4 or compound A-74. The pharmaceutical composition according to claim 1, wherein the water-insoluble antipsychotic is olanzapine, a compound of formula III or a compound of formula IV, or pharmaceutically acceptable salts thereof, hydrates or solvates of which are R
机译:1.一种药物组合物,其包含(a)水不溶性抗精神病药; (b)山梨糖醇和羧酸的酯,其中该羧酸含有4-20个碳原子; (c)山梨糖醇和羧酸的酯的聚氧乙烯衍生物,其中该羧酸含有8 -14个碳原子; (d)水性填料;其中所述组合物形成水性的,絮凝的,可注射的悬浮液。 2.根据权利要求1所述的药物组合物,其中,所述水不溶性抗精神病药为阿立哌唑,式1的化合物或式II的化合物,或其药学上可接受的盐,不存在R且R为-CHOC的水合物或溶剂化物。 )R,-CHOC(O)OR,-CHOC(O)N(R)或-C(O)R;或R不存在且R为-CHOC(O)R,-CHOC(O)OR,-CHOC(O)N(R)或-C(O)R; R为-CHOC(O)R,-CHOC(O)OR,-CHOC(O)N(R)或-C(O)R;其中每个R独立地选自氢,取代或未取代的脂族基团和取代或ezameschennogo芳基;其中每个R选自取代或未取代的芳基和取代或未取代的杂芳基;其中是药学上可接受的抗衡离子;它是单键或双键。 3.根据上述项目中任一项的药物组合物,其中所述水不溶性抗精神病药是化合物A-4或化合物A-74。 2.根据权利要求1所述的药物组合物,其中,所述水不溶性抗精神病药为奥氮平,式III的化合物或式IV的化合物或其药学上可接受的盐,其水合物或溶剂化物为R。

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