| 摘要 |
A formulation comprises: (a) one or more hydrophobic pharmaceutical agents being either quinazoline, nitrothiazole or indolinone based compounds; (b) one or more polyoxyhydrocarbyl compounds and (c) one or more pharmaceutically acceptable surfactants. The indolinone base compound, which is present in the composition in a concentration of 0.1 to 100 mg/ml, has the formula (VI) wherein: R1, R2, R3, and R4 are independently hydrogen, trihalomethyl, hydroxyl, amine, thioether, cyano, alkoxy, alkyl, amino, bromo, fluoro, chloro, iodo, mercapto, thio, cyanoamido, alkylthio, aryl, heteroaryl, carboxyl, ester, oxo, alkoxycarbonyl, alkenyl, alkoxy, nitro, alkoxyl, or amido moieties and R5 is an optionally substituted aryl or heteroaryl cyclic moiety. At least one of the surfactants for the indolinone based compound is PEG-400 present in a concentration of 0.01 to 10 g/ml and at least one of the polyoxyhydrocarbyl compounds for the indolinone based compound is ethoxylated castor oil present in a concentration of 0.01 to 10 g/ml. The quinazoline based compound has the formula (I) wherein: R1, R2, R3, R4, R5 and R6 are independently hydrogen or an optionally saturated alkyl, optionally substituted aryl, optionally substituted amine, halogen, trihalomethyl, ketone, carboxylic acid or ester, alcohol, alkoxy, amide, -SO2NX11X12, wherein X11 and X12 are as defined in the specification, optionally substituted homocyclic or heterocyclic ring moiety, aldehyde, sulphone or nitro. The nitrothiazole based compound has the formula IV wherein: R1, R2, and R3 are independently hydrogen or an optionally saturated alkyl, optionally substituted aryl, optionally substituted amine, halogen, trihalomethyl, ketone, carboxylic acid or ester, alcohol, alkoxy, halogen, trihalomethyl, ketone, carboxylic acid or ester, alcohol, alkoxy, amide, -SO2NX11X12, wherein X11 and X12 are as defined in the specification, optionally substituted homocyclic or heterocyclic ring moiety, aldehyde, sulphone or nitro.
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