| 摘要 |
Provided are solid stable pharmaceutical dosage forms comprising (S)-ethyl 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)propanoate (telotristat). In an embodiment the dosage form is a tablet comprising (S)-ethyl 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)propanoate, lactose, hydroxy propyl cellulose, croscarmellose sodium, magnesium stearate, and silicon dioxide; wherein the tablet forms less than 1.0 percent (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 40°C and 75% relative humidity for six months; and wherein the tablet has a disintegration time of less than 5.5 minutes in water. |
