Pharmaceutical formulations comprising tenofovir alafenamide and emtricitabine
The invention provides a solid oral dosage form comprising tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.
1 .- 49 . (canceled)
50 . A tablet consisting of:
(a) 20 mg to 30 mg tenofovir alafenamide, or a pharmaceutically acceptable salt thereof;
(b) 150 mg to 250 mg emtricitabine or a pharmaceutically acceptable salt thereof; and
(c) one or more excipients comprising 20 mg to 35 mg croscarmellose sodium, 70 mg to 120 mg microcrystalline cellulose, and 1 mg to 7 mg magnesium stearate;
wherein the tablet comprises 7% to 9% by weight tenofovir alafenamide, or a pharmaceutically acceptable salt thereof; and
wherein the tablet does not comprise lactose.
51 . The tablet according to claim 50 , comprising about 8% by weight tenofovir alafenamide hemifumarate.
52 . The tablet according to claim 50 , wherein the tablet consists of about 200 mg emtricitabine, about 28 mg tenofovir alafenamide hemifumarate, about 28 mg croscarmellose sodium, about 88.70 mg microcrystalline cellulose, and about 5.25 mg magnesium stearate.
53 . A kit comprising the tablet according to claim 50 and a desiccant, wherein the desiccant is silica gel.
54 . The tablet of claim 50 , wherein the total weight of the tablet is 350 mg±25 mg.
55 . A tablet consisting of:
200 mg±20 mg emtricitabine;
28 mg±3 mg tenofovir alafenamide hemifumarate;
28 mg±3 mg croscarmellose sodium;
89 mg±9 mg microcrystalline cellulose; and
5.2 mg±1.1 mg magnesium stearate.
56 . The tablet of claim 55 , consisting of:
200 mg±10 mg emtricitabine;
28 mg±1.4 mg tenofovir alafenamide hemifumarate;
28 mg=1.4 mg croscarmellose sodium;
89 mg±4 mg microcrystalline cellulose; and
5.2 mg±0.5 mg magnesium stearate.
57 . The tablet of claim 55 , consisting of:
200 mg emtricitabine;
28 mg tenofovir alafenamide hemifumarate;
28 mg croscarmellose sodium;
89 mg microcrystalline cellulose; and
5.3 mg magnesium stearate.
58 . A tablet consisting of:
200 mg±20 mg emtricitabine;
28 mg±3 mg tenofovir alafenamide hemifumarate;
28 mg±3 mg croscarmellose sodium;
89 mg±9 mg microcrystalline cellulose;
5.2 mg±1.1 mg magnesium stearate; and
a polymeric film coating.
59 . The tablet of claim 58 , consisting of:
200 mg±10 mg emtricitabine;
28 mg±1.4 mg tenofovir alafenamide hemifumarate;
28 mg=1.4 mg croscarmellose sodium;
89 mg±4 mg microcrystalline cellulose;
5.2 mg±0.5 mg magnesium stearate; and
a polymeric film coating.
60 . The tablet of claim 58 , consisting of:
200 mg emtricitabine;
28 mg tenofovir alafenamide hemifumarate;
28 mg croscarmellose sodium;
89 mg microcrystalline cellulose;
5.3 mg magnesium stearate; and
a polymeric film coating.
61 . A tablet consisting of:
(a) 20 mg to 30 mg tenofovir alafenamide, or a pharmaceutically acceptable salt thereof;
(b) 150 mg to 250 mg emtricitabine or a pharmaceutically acceptable salt thereof;
(c) one or more excipients comprising 20 mg to 35 mg croscarmellose sodium, 70 mg to 120 mg microcrystalline cellulose, and 1 mg to 7 mg magnesium stearate; and
(d) a polymeric film coating;
wherein the tablet comprises 7% to 9% by weight tenofovir alafenamide, or a pharmaceutically acceptable salt thereof; and
wherein the tablet does not comprise lactose.
62 . The tablet according to claim 61 , comprising about 8% by weight tenofovir alafenamide hemifumarate.
63 . The tablet according to claim 61 , wherein the tablet consists of about 200 mg emtricitabine, about 28 mg tenofovir alafenamide hemifumarate, about 28 mg croscarmellose sodium, about 88.70 mg microcrystalline cellulose, about 5.25 mg magnesium stearate, and a polymeric film coating.
64 . A kit comprising the tablet according to claim 61 and a desiccant, wherein the desiccant is silica gel.
65 . The tablet of claim 61 , wherein the total weight of the tablet is 350 mg±25 mg.
66 . A tablet consisting of:
(a) 20 mg to 30 mg tenofovir alafenamide, or a pharmaceutically acceptable salt thereof;
(b) 150 mg to 250 mg emtricitabine or a pharmaceutically acceptable salt thereof; and
(c) one or more excipients comprising 20 mg to 35 mg croscarmellose sodium, 70 mg to 120 mg microcrystalline cellulose, and 1 mg to 7 mg magnesium stearate;
wherein the tablet comprises 7% to 9% by weight tenofovir alafenamide, or a pharmaceutically acceptable salt thereof; and
wherein the tablet does not comprise starch.
67 . The tablet according to claim 66 , comprising about 8% by weight tenofovir alafenamide hemifumarate.
68 . The tablet according to claim 66 , wherein the tablet consists of about 200 mg emtricitabine, about 28 mg tenofovir alafenamide hemifumarate, about 28 mg croscarmellose sodium, about 88.70 mg microcrystalline cellulose, and about 5.25 mg magnesium stearate.
69 . A kit comprising the tablet according to claim 66 and a desiccant, wherein the desiccant is silica gel.
70 . The tablet of claim 66 , wherein the total weight of the tablet is 350 mg±25 mg.
71 . A tablet consisting of:
(a) 20 mg to 30 mg tenofovir alafenamide, or a pharmaceutically acceptable salt thereof;
(b) 150 mg to 250 mg emtricitabine or a pharmaceutically acceptable salt thereof;
(c) one or more excipients comprising 20 mg to 35 mg croscarmellose sodium, 70 mg to 120 mg microcrystalline cellulose, and 1 mg to 7 mg magnesium stearate; and
(d) a polymeric film coating;
wherein the tablet comprises 7% to 9% by weight tenofovir alafenamide, or a pharmaceutically acceptable salt thereof; and
wherein the tablet does not comprise starch.
72 . The tablet according to claim 71 , comprising about 8% by weight tenofovir alafenamide hemifumarate.
73 . The tablet according to claim 71 , wherein the tablet consists of about 200 mg emtricitabine, about 28 mg tenofovir alafenamide hemifumarate, about 28 mg croscarmellose sodium, about 88.70 mg microcrystalline cellulose, about 5.25 mg magnesium stearate, and a polymeric film coating.
74 . A kit comprising the tablet according to claim 71 and a desiccant, wherein the desiccant is silica gel.
75 . The tablet of claim 71 , wherein the total weight of the tablet is 350 mg±25 mg.