TONG PING,ZHOU DELIANG,ZHANG GEOFF G Z,HEEMSTRA KATHERINE,FISCHER CRISTINA M.,CATRON NATHANIEL,SCHMITT ERIC A.,SANZGIRI YESHWANT D.
申请号：
NZ59994110
公开号：
NZ599941A
申请日:
2010.12.21
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
Disclosed is a pharmaceutical capsule comprising a capsule shell having encapsulated therewithin, in an amount not greater than about 1000 mg per capsule, a liquid solution of navitoclax (ABT-263 / N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide) or a pharmaceutically acceptable salt thereof at a navitoclax free-base equivalent concentration of at least about 40 mg/ml in a substantially non-ethanolic carrier that comprises as pharmaceutically acceptable excipients (a) at least one phospholipid (such as phosphatidylcholine), (b) at least one solubilizing agent for the at least one phospholipid, selected from the group consisting of glycols, glycolides, glycerides and mixtures thereof (particularly mixtures of medium-chain triglycerides and one or more medium-chain mono- and/or diglycerides), (c) at least one non-phospholipid surfactant in an amount of 7% to 30% of the encapsulated liquid (such as polysorbate 80), and (d) at least one sulfur-containing antioxidant (such as sulfites, bisulfites, metabisulfites, thiosulfates and mixtures thereof) in an amount effective to reduce oxidative degradation of navitoclax upon storage.
