ИТТЕР Джеффри Б. (US),ЛАЙ Мэй (US),БЕКСТРЕМ Джей Томас (US)
申请号：
RU2012147739/15
公开号：
RU2012147739A
申请日:
2012.11.09
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. A pharmaceutical composition for oral administration containing a therapeutically effective amount of 5-azacytidine, wherein the composition releases 5-azacytidine substantially in the stomach after oral administration to a subject. A composition according to claim 1, which is an immediate release composition. A composition according to claim 1, which is not coated with an enteric coating. The composition of claim 1, which is a tablet. The composition of claim 1, which is a capsule. 6. A composition according to claim 1, which further comprises an excipient selected from mannitol, microcrystalline cellulose, crospovidone and magnesium stearate. The composition of claim 1, further comprising a penetration enhancing agent. The composition of claim 7, wherein the penetration enhancing agent is d-alpha-tocopheryl polyethylene glycol 1000 succinate. The composition of claim 8, wherein d-alpha-tocopheryl polyethylene glycol 1000 succinate is present in the composition in an amount of about 2% by weight relative to the total weight of the composition. A composition according to claim 1, which essentially does not contain a cytidine deaminase inhibitor. A composition according to claim 1, which essentially does not contain tetrahydrouridin. A composition according to claim 1, which further comprises an additional therapeutic agent. The composition of claim 1, wherein the amount of 5-azacytidine is at least about 40 mg. The composition of claim 1, wherein the amount of 5-azacytidine is at least about 400 mg. The composition of claim 1, wherein the amount of 5-azacytidine is at least about 1000 mg. The composition according to claim 1, which reaches the value of the area under the curve at least1. Фармацевтическая композиция для перорального введения, содержащая терапевтически эффективное количество 5-азацитидина, где композиция высвобождает 5-азацитидин по существу в желудке после перорального введения субъекту.2. Композиция по п. 1, которая представляет собой композицию
