ЧЭНЬ Цзиньлин (US),ДИВЕР Мэттью С. (US),ХОЛЛ Ричард Дж. (US),НУГУРУ Калиан (US)
申请号：
RU2014119866/15
公开号：
RU2014119866A
申请日:
2012.10.16
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. A tablet containing telotristate or a pharmaceutically acceptable salt thereof, in which less than 1.0 is formed； 0.8 or 0.5% (S) -2-amino-3- (4- (2-amino-6 - ((R) -1- (4-chloro-2- (3-methyl-1H-pyrazole -1-yl) phenyl) -2,2,2-trifluoroethoxy) pyrimidin-4-yl) phenyl) propanoic acid when stored at a temperature of about 40 ° C and a relative humidity of about 75% for six months. The tablet according to claim 1, wherein less than 0.5 or 0.4% of (S) -2-amino-3- (4- (2-amino-6 - ((R) -1- (4- chloro-2- (3-methyl-1H-pyrazol-1-yl) phenyl) -2,2,2-trifluoroethoxy) pyrimidin-4-yl) phenyl) propanoic acid when stored at a temperature of approximately 40 ° C and relative humidity of approximately 75% for three months. 3. A tablet containing a core consisting mainly of etiprate telotristate, lactose, hydroxypropyl cellulose, croscarmellose sodium, magnesium stearate and silicon dioxide. 4. A vial containing tablets according to any one of paragraphs. 1-3 and moisture absorber. 5. Granules containing telotristate etiprate, lactose, hydroxypropyl cellulose, croscarmellose sodium, magnesium stearate and silicon dioxide. 6. The granules of claim 5, wherein the magnesium stearate is present in an amount of more than about 3, 4, or 5 weight percent. The granules according to claim 5, wherein the cellulose is hydroxypropyl cellulose and / or microcrystalline cellulose. A granulate containing granules according to claim 5, which has an average flow rate coefficient of more than about 0.3； 0.35 or 0.4 kg / s. 9. A method for producing tablets, which comprises: mixing granules containing intragranular ingredients with at least one extragranular ingredient, compressing granules to obtain tablets； wherein the intragranular ingredients include telotristate or a pharmaceutically acceptable1. Таблетка, содержащая телотристат или его фармацевтически приемлемую соль, в которой образуется менее, чем 1,0； 0,8 или 0,5% (S)-2-амино-3-(4-(2-амино-6-((R)-1-(4-хлор-2-(3-метил-1H-пиразол-1-ил)фенил)-2,2
