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oral dosage forms of bendamustine and its therapeutic use
专利权人:
ASTELLAS DEUTSCHLAND GMBH
发明人:
TAOUFIK OUATAS,ULRICH PATZAK
申请号:
BR112012030658
公开号:
BR112012030658A2
申请日:
2011.06.01
申请国别(地区):
BR
年份:
2016
代理人:
摘要:
oral dosage forms of bendamustine and therapeutic use thereof. In the present invention there is provided a pharmaceutical composition for oral administration comprising bendamustine or a pharmaceutically acceptable ester, salt, or solvate as an active ingredient, and a pharmaceutically acceptable excipient and having a bendamustine dissolution of at least 60% within 20 minutes. % in 40 minutes and 80% in 60 minutes, as measured with a paddle apparatus at 50rpm according to the European Pharmacopoeia, in 500 ml of a dissolution medium at a pH of 1.5 and wherein the pharmaceutically acceptable excipient. is either a pharmaceutically acceptable nonionic surfactant selected from the group consisting of a polyethoxylated castor oil or a derivative thereof and a block copolymer of ethylene oxide and propylene oxide or a pharmaceutically acceptable saccharide from the group comprising: consists of one or more of a monosaccharide, a disaccharide, an oligosaccharide, a cyclic oligosaccharide, a polysaccharide o is a saccharide alcohol, wherein the weight ratio of active ingredient to excipet (s) is in the range 1: 1-5. The invention further relates to the above pharmaceutical composition for use in the oral treatment of a medical condition that is selected from chronic lymphocytic leukemia, acute lymphocytic leukemia, chronic myelocytic leukemia, acute myelocytic leukemia, hodgkin's disease, non-hodgkin's lymphoma. multiple myeloma, breast cancer, ovarian cancer, small cell lung cancer and non-small cell lung cancer. The invention furthermore relates to the above pharmaceutical composition for the above use wherein the dosage regimen comprises at least the administration of a dose of 100 to 600 mg / m2 per person of bendamustine on day 1; day 2, optionally a dose of 50 to 150 mg / m 2 / iv or orally of a corticosteroid on days 1 to 5, and optionally a suitable dose of an additional active agent selected from the group consisting of a dc20 specific antibody, an anthracycline
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