CHANDRASHEKAR GILIYAR,JOEL FRANK,MAHESH V. PATEL,NACHIAPPAN CHIDAMBARAM,SATISH KUMAR NACHAEGARI,SRINIVASAN VENKATESHWARAN
申请号：
BR112017004127
公开号：
BR112017004127A2
申请日:
2015.08.28
申请国别(地区):
BR
年份:
2018
代理人:
摘要：
a form of compositions and dosages that allows high drug loading for highly lipophilic drugs while maintaining excellent oral bioavailability. the pharmaceutical unit dosage and composition forms described herein may reduce the pill load for hydrophobic drugs such as (8r, 9s, 10r, 13s, 14s, 17s) -10,13-dimethyl-3-oxo-1, 2,6,7,8,9, 11,12,14,15,16,17-dodecahydrocyclopenta [a] phenanthrene-17-yl tridecanoate or (8r, 9s, 10r, 13s, 14s, 17s) -10,13 -dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta [a] phenanthrene-17-yl tetradecanoate, and may be formulated as drug fillers advantageous (e.g., greater than 23%) while providing adequate bioavailability (e.g., capable of treating a hypogonadal male subject with less than 10 unit dosage forms per day) allowing reduction in pill loading and consequent adherence or compliance improved patient care. In addition, the composition (e.g., dosage form) has a release profile that is suitable to provide bioavailable api and the release profile is stable over time (e.g. under storage conditions).uma forma de composições e dosagens que permite alto carregamento de fármaco para fármacos altamente lipofílicos enquanto mantém excelente biodisponibilidade oral. as formas de composições e de dosagem de unidade farmacêuticas descritas no presente documento podem reduzir a carga da pílula para fármacos hidrofóbicos como (8r,9s,10r,13s,14s,17s)-10,13-dimetil-3-oxo-1,2,6,7,8,9, 11,12,14,15,16,17-dodecahidrociclopenta[a]fenantren-17-il tridecanoato ou (8r,9s,10r,13s,14s,17s)-10,13-dimetil-3-oxo-l,2,6, 7,8,9,11,12,14,15,16,17- dodecahidrociclopenta[a]fenantren-17-il tetradecanoato, e podem ser formulados em cargas de fármaco vantajosas (por exemplo, maior que 23%) enquanto provê biodisponibilidade adequada (por exemplo, capaz de tratar um indivíduo masculino com hipogonadismo com menos que 10 formas de dosagem de unidade por dia) que permite redução na carga da pílula e consequentemente aderência ou complacência do paciente melho
