IP Library › Patent Application 14619150
Patent Application
App. No. 14/619,150

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

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Patent No.
US None
App. No.
14/619,150
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.

Claims (18)

1 . 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.

2 . The tablet of claim 1 , which forms less than 0.5 or 0.4 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 three months.

3 . A tablet having a core consisting essentially of telotristat etiprate, lactose, hyrdroxy propyl cellulose, croscarmellose sodium, magnesium stearate, and silicon dioxide.

4 . A bottle comprising a tablet of any of claims 1 - 3 and a desiccant.

5 . A granule comprising telotristat etiprate, lactose, hydroxyl propyl cellulose, croscarmellose sodium, magnesium stearate, and silicon dioxide.

6 . The granule of claim 5 , wherein magnesium stearate is present in an amount greater than about 3, 4 or 5 weight percent.

7 . The granule of claim 5 , wherein the cellulose is hydroxyl propyl cellulose and/or microcrystalline cellulose.

8 . A granulate comprising granules of claim 5 , which has an average flow rate index of greater than about 0.3, 0.35, or 0.4 kg/sec.

9 . 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.

10 . The method of claim 9 , wherein the cellulose is hydroxyl propyl cellulose or microcrystalline cellulose.

11 . The method of claim 9 , wherein the intragranular ingredients further comprise croscarmellose sodium.

12 . The method of claim 9 , wherein the at least one extragranular ingredient further comprises one or more of croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate.

13 . The method of claim 9 , wherein the granules are prepared by milling a ribbon made by roller compaction of the intragranular ingredients.

14 . The method of claim 9 , which further comprises coating the tablet with an enteric coating.