首页> 外国专利> Pharmaceutical compositions of 5,7,14-triazatetracyclo 10.3.1.0(2,11).0(4,9)-hexadeca-2(11)3,5,7,9-pentaene

Pharmaceutical compositions of 5,7,14-triazatetracyclo 10.3.1.0(2,11).0(4,9)-hexadeca-2(11)3,5,7,9-pentaene

机译:5,7,14-三氮杂三环[10.3.1.0(2,11).0(4,9)]-十六碳-2(11)3,5,7,9-戊烯的药物组合物

摘要

Disclosed is a controlled release dosage form suitable for administration to a subject comprising 5,8,14-triazatetra-cyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene, and a means for administering the compound to the subject at a rate of less than about 6 mg/hour, whereby the controlled release dosage form is formulated such that at least about 0.1 mg of the compound is administered over a 24 hour period. Also disclosed is a controlled release dosage form formulated such that, when dosed to a subject the dosage form results in a time for maximum plasma concentration (Tmax) that is increased for the drug in an initial administration to the subject by an average of 50% of the corresponding Tmax determined for an equal does of the pentaene in the form of an immediate release bolus. Also disclosed is a controlled release dosage form formulated such that the dosage releases the pentaene at a rate of less than 6 mgA/hr in vitro when dissolution tested in a USP-2 apparatus, such that the time for dissolution of 50 w/w% of the drug is between 1 and 15 hours.
机译:公开了一种适于向包含5,8,14-三氮杂双环[10.3.1.02,11.04,9]-十六碳-2(11),3,5,7,9-戊烯的受试者给药的控释剂型,以及以小于约6mg /小时的速率向受试者施用化合物的方式,由此配制控释剂型,使得在24小时内施用至少约0.1mg的化合物。还公开了控制释放剂型,其被配制为使得当给药于受试者时,该剂型导致最大血浆浓度(Tmax)的时间,该时间对于药物在最初给予受试者中增加了平均50%。以速释推注的形式确定与戊烯相同剂量的相应Tmax的平均值。还公开了一种控释剂型,其配制使得当在USP-2装置中进行溶出度试验时,该剂量以低于6 mgA / hr的速率在体外释放戊烯,以使溶出时间为50 w / w%药物的使用时间为1到15小时。

著录项

相似文献

  • 专利
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号