Solid dispersion with improved solubility comprising tetrazole derivative as an active ingredient
AssigneeHanmi Pharm. Co., Ltd.
InventorsYong Il Kim, Jun Young Choi, Young Keun Choi, Jae Hyun Park, Jong Soo Woo
Life of this patent
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Abstract
The present invention relates to an amorphous solid dispersion comprising a tetrazole derivative of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. The solid dispersion of the present invention comprises a water-soluble polymer or an acid so as to improve the solubility of its active ingredient, i.e., the tetrazole derivative of the formula (I), thereby improving its absorption rate, and thus can be effectively used to reduce multi-drug resistance (MDR) in cancer cells.
Claims20
An amorphous solid dispersion comprising a tetrazole compound of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient:
- wherein,
- R1 is quinoline, isoquinoline, quinoxaline, pyridine, pyrazine, naphthalene, phenyl, thiophene, furan, 4-oxo-4H-chromene or cinnoline, which is unsubstituted or substituted by C1-C5alkyl, hydroxyl, C1-5alkoxy, halogen, trifluoromethyl, nitro or amino;
- R2 to R5 and R8 to R11 are each independently H, hydroxyl, halogen, nitro, C1-C5alkyl or C1-5alkoxy;
- R6 and R7 are each independently H, hydroxyl, halogen, nitro, C1-5alkylene or C1-5 alkoxy;
- and R6 and R7 may be connected to form a 4- to 8-membered ring;
- m and n are each independently integers ranging from 0 to 4;
- and
- X is CH2, O or S.
A polymorph of a compound of formula (II), showing an X-ray power diffraction pattern comprising peaks at approximately 7.948, 12.936, 14.744, and 26.485 degree two-theta:
Dependencies are inferred from the claim text.