Pharmaceutical composition of taxoids

摘要

The present invention relates to a stable oral pharmaceutical composition with improved solubility and bioavailability; comprising a taxoid, a solubilizer, a stabilizing agent, a surfactant(s), a solvent(s), and an oil wherein the concentration of taxoid is in the range of 0.1 to 10%.

主权项

1. A stable oral pharmaceutical composition of taxoid with improved solubility and bioavailability for administration to a mammal, the composition comprising:
a taxoid selected from Paclitaxel or Docetaxel or a pharmaceutically acceptable salt thereof; a solubilizer selected from diethylene glycol monoethyl ether, glycofurol, and polyoxyl 40 hydrogenated castor oil; a stabilizing agent selected from piperine, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, polyvinyl pyrrolidone and hydroxypropyl methyl cellulose; a surfactant selected from capryl/caproyl macrogel glycerides, alpha-tochopherol polyethylene glycol 1000 succinate, polysorbate and PEG hydrogenated castor oil, and combinations thereof; a solvent selected from propylene glycol and ethyl alcohol, and combinations thereof; and an oil selected from: (1) medium chain fatty acid triglycerides selected from fractionated coconut oil, caprylic/capric triglyceride, (2) esters of fatty acids and monovalent alkanols selected from isopropyl myristate, isopropyl palmitate, ethyl linoleate and ethyl oleate and (3) propyleneglycol di-fatty acid esters selected from propyleneglycol dicaprylate, propyleneglycol dilaurate; wherein the ratio of solubilizer to taxoid and stabilizing agent to taxoid are in the range of 2.5 to 12.5 and 0.5 to 3.3, respectively.