JP2012500788A5 - - Google Patents

Claims (15)

A solid pharmaceutical composition for oral administration comprising a substantially amorphous taxane, a hydrophilic carrier and a surfactant, wherein the taxane , the carrier and the surfactant are in the form of a solid dispersion. The solid pharmaceutical composition, wherein the solid dispersion is prepared by a spray drying method. The taxane is selected from docetaxel, paclitaxel, BMS-275183, and functional derivatives thereof, and pharmaceutically acceptable salts or esters thereof , preferably docetaxel, paclitaxel, and functional groups thereof The composition according to claim 1, which is selected from derivatives, and pharmaceutically acceptable salts or esters thereof. The composition according to claim 1 or 2 , wherein the carrier is polymeric. The composition according to any one of claims 1 to 3 , wherein the carrier is selected from PVP, PVP-VA and PEG. The carrier is PVP , preferably the PVP is selected from 1) PVP-K12, PVP-K15, PVP-K17, PVP-K25, PVP-K30, PVP-K60 and PVP-K90. The composition according to any one of claims 1 to 4 , which is or is selected from 2) PVP-K30, PVP-K60 and PVP-K90 . The surfactant is 1) sodium dodecyl sulfate (SDS), sorbitan esters (sorbitan fatty acid esters), polyoxyethylene stearates, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene castor oil derivatives, polyoxy Selected from ethylene alkyl ethers, poloxamers, glyceryl monooleate, sodium docusate, cetrimide, benzyl benzoate, benzalkonium chloride, benzethonium chloride, hypromellose, nonionic emulsifying wax, anionic emulsifying wax and triethyl citrate 2) Is it selected from SDS, sorbitan esters (sorbitan fatty acid esters), polyoxyethylene sorbitan fatty acid esters and CPC? Or 3) The composition according to any one of claims 1 to 5 , which is SDS . The weight ratio of the taxane to the carrier is about 0.01: 99.99 (w / w) to about 75:25 (w / w) , preferably about 0.01: 99.99 (w / w). ) is about 30:70 (w / w), composition according to any one of claims 1 to 6. The weight ratio of surfactant to combined taxane and carrier is from about 1:99 (w / w) to about 50:50 (w / w) , preferably from about 2:98 (w / w) to 8. The composition according to any one of claims 1 to 7 , which is about 17:83 (w / w) . 9. The composition according to any one of claims 1 to 8 , further comprising one or more additional pharmaceutically active ingredients. 10. The composition of claim 9 , wherein the one or more additional pharmaceutically active ingredients is a CYP3A4 inhibitor , preferably the CYP3A4 inhibitor is ritonavir . 11. A composition according to claim 9 or 10 , wherein the taxane, the carrier, the surfactant and the one or more additional pharmaceutically active ingredients are in the form of a solid dispersion. The composition according to claim 11 , wherein the solid dispersion is prepared by a spray drying method. 13. A composition according to any one of claims 1 to 12 for use in therapy. Use of a composition according to any one of claims 1 to 12 in the preparation of a medicament for the treatment of neoplastic diseases. Using a spray drying method, amorphous Takisa down, including as engineering of preparing a solid dispersion comprising a hydrophilic carrier and a surfactant, a method for preparing the composition of claim 1.