Solid dosage forms of (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
OwnerJinling CHEN, Matthew S. DEAVER +2inventors
InventorsJinling CHEN, Matthew S. DEAVER, Richard J. HOLL, Kalyan NUGURU
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Abstract
Solid 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) are disclosed, as well as methods of making them and compositions useful in their manufacture.
Claims14
A tablet comprising telotristat or a pharmaceutically acceptable salt thereof, which forms less than 1.0, 0.8 or 0.5 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 about 40° C. and about 75% relative humidity for six months.
A tablet having a core consisting essentially of telotristat etiprate, lactose, hyrdroxy propyl cellulose, croscarmellose sodium, magnesium stearate, and silicon dioxide.
A granule comprising telotristat etiprate, lactose, hydroxyl propyl cellulose, croscarmellose sodium, magnesium stearate, and silicon dioxide.
A method of making a tablet, which comprises:
- combining granules comprising intragranular ingredients with at least one extragranular ingredient, and
- compressing the granules to provide a tablet;
- wherein the intragranular ingredients comprise telotristat or a pharmaceutically acceptable salt thereof, magnesium stearate, and lactose;
- and
- the at least one extragranular ingredient is lactose.
Dependencies are inferred from the claim text.