| 摘要 |
A spray-dried pharmaceutical composition of a naphthoquinone-based compound is provided to increase the solubility of the compound in water and minimize the solubility difference caused by pH change of a human body by spray-drying an insoluble naphthoquinone-based compound with a water-soluble polymer and a solubilizer. A spray-dried pharmaceutical composition comprises a therapeutically effective amount of at least one naphthoquinone-based compound having pharmacological efficacy on preventing or treating cancer and treating diseases caused by infection of bacteria, fungi, or parasite and skin diseases and represented by formulae(1) and (2) and is prepared by spray-drying a mixture solution of the naphthoquinone-based compound, a water soluble polymer, a solubilizer and a solvent. In the formulae(1) and (2), each R1 and R2 is independently H, halogen, alkoxy, hydroxy or C1-6 alkyl, or R1 and R2 may be coupled to each other to form a substituted or unsubstituted ring structure(wherein the ring structure is a saturated structure or a partial or a total unsaturated structure); each R3, R4, R5, R6, R7 and R8 is independently H, hydroxy, C1-20 alkyl, alkene or alkoxy, C4-20 cycloalkyl, heterocycloalkyl, aryl or heteroaryl, or two of the R3, R4, R5, R6, R7 and R8 are coupled to each other to form a ring structure(wherein the ring structure is a saturated structure or a partial or a total unsaturated structure); X is O, S or NR'(wherein R' is H or C1-6 alkyl); Y is C, S, or N, provided that R7 and R8 are nothing when Y is S, and R7 is H or C1-6 alkyl and R8 is nothing when Y is N; and each m and n is 0 or 1, provided that adjacent carbon atoms thereof are directly coupled to one another to form a ring structure when m or n is 0. In the composition, the naphthoquinone-based compound is in the form of a nano-particle through a pulverization, a spray-drying, a precipitation, a high-pressure emulsification or a super-critical nanoparticulation.
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