Solid dispersions of insoluble drug and preparation method thereof
AssigneeSK Biopharmaceuticals Co., Ltd.
InventorsMyoung Ki BAEK, Augustin PEGAN
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Abstract
The present invention relates to a solid dispersion characterized in that it comprises carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester as an active ingredient and a water-soluble polymer having a glass transition temperature lower than the melting point of the active ingredient as a carrier, and it is prepared via melt extrusion. The solid dispersion of the present invention remarkably increases the solubility and dissolution rate of the active ingredient which is an insoluble drug to efficiently improve the bioavailability when it is orally administered.
Claims18
1-16. (canceled)
A method for treating a disease of central nervous system, comprising
- administering to a patient in need thereof a pharmaceutically effective amount of a solid dispersion comprising:
- carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester, or a pharmaceutically acceptable salt or solvate thereof,
- a water-soluble polymer, and
- a plasticizer,
- wherein the solid dispersion is prepared by melt extrusion,
- wherein the water-soluble polymer is selected from polyvinylpyrrolidone, hypromellose acetate succinate and a combination thereof, and
- wherein the plasticizer is selected from the group consisting of D-alpha-tocopheryl polyethylene glycol 1000 succinate, polyethylene glycol 400, and a combination thereof.
A method for preparing a solid dispersion, comprising:
- mixing carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester and a water-soluble polymer, and
- melt-extruding the mixture at a temperature lower than the melting point of carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester.
Dependencies are inferred from the claim text.