| 摘要 |
A composition comprising a naphthoquinone-based compound as an active ingredient is provided to increase the in vivo absorption amount of the active ingredient and enhance the in vivo duration time by formulating the compound into an intestine delivery system, thereby improving the in vivo availability and kinetic characteristics of the compound. An oral administering pharmaceutical composition is characterized in that a naphthoquinone-based compound represented by a formula(1), a pharmaceutically acceptable salt thereof, a solvate thereof or an isomer thereof as an active ingredient is formulated into an intestine delivery system. In the formula(1), 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 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, 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 C(R)(R'), N(R"), O or S(wherein each R, R' and R" is independently H or C1-6 alkyl); and n is 0 or 1, provided that adjacent carbon atoms thereof are directly coupled to one another to form a ring structure when n is 0. In the composition, the intestine delivery system is formulated by adding a pH sensitive polymer or a bio-degradable polymer by an intestine-specific bacteria enzyme and the active ingredient has an amorphous crystalline structure.
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