Heterocyclic compounds and their uses
Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.
1. A pharmaceutical tablet formulation comprising:
a drug layer, comprising omecamtiv mecarbil dihydrochloride hydrate;
a sweller layer; and
a semi-permeable membrane coating having at least one delivery port,
wherein the semi-permeable membrane coating comprises 80% insoluble polymer and 20% pore forming polymer.
2. A pharmaceutical tablet formulation according to claim 1 , wherein the drug layer comprises:
omecamtiv mecarbil dihydrochloride hydrate;
a drug layer polymer; and
a lubricant.
3. A pharmaceutical tablet formulation according to claim 1 , wherein the sweller layer comprises:
a sweller layer polymer;
an osmotic agent;
a diluent; and
a lubricant.
4. A pharmaceutical tablet formulation according to claim 1 , where the
insoluble polymer comprises cellulose acetate.
5. A pharmaceutical tablet formulation according to claim 1 , wherein the pore forming polymer comprises polyethylene glycol.
6. A pharmaceutical tablet formulation comprising:
a drug layer comprising:
omecamtiv mecarbil dihydrochloride hydrate;
a drug layer polymer; and
a lubricant;
a sweller layer comprising:
a sweller layer polymer;
an osmotic agent;
a diluent; and
a lubricant; and
a semi-permeable membrane coating having at least one delivery port comprising:
an insoluble polymer comprising cellulose acetate; and
a pore forming polymer comprising polyethylene glycol,
wherein the semi-permeable membrane coating comprises 80% the insoluble polymer and 20% the pore forming polymer.
7. A pharmaceutical tablet formulation comprising
a drug layer comprising:
14-17 (w/w%) omecamtiv mecarbil dihydrochloride hydrate;
48-55 (w/w%) polyethylene oxide; and
0.1-0.5% (w/w%) lubricant;
a sweller layer comprising:
18-25 (w/w%) polyethylene oxide;
4-9 (w/w%) an osmotic agent;
3-6 (w/w%) microcrystalline cellulose; and
0.1-0.5 (w/w%) lubricant; and
a semi-permeable membrane having at least one delivery port comprising:
8-10 (w/w%) cellulose acetate;
0.5-3 (w/w%) polyethylene glycol.
8. The pharmaceutical tablet formulation of claim 7 , wherein the polyethylene glycol of the semi-permeable membrane has an average molecular weight of 3350.
9. The pharmaceutical tablet formulation of claim 7 , wherein the osmotic agent comprises sodium chloride.
10. The pharmaceutical tablet formulation of claim 7 , having one to 10 delivery ports.
11. The pharmaceutical tablet formulation according to claim 1 , wherein the tablet comprises 14-17 (w/w%) omecamtiv mecarbil dihydrochloride hydrate.
12. The pharmaceutical tablet formulation according to claim 1 , wherein the insoluble polymer comprises cellulose acetate and the pore forming polymer comprises polyethylene glycol.
13. The pharmaceutical tablet formulation according to claim 1 , having one to 10 delivery ports.
14. The pharmaceutical tablet formulation according to claim 12 , wherein the tablet comprises 14-17 (w/w%) omecamtiv mecarbil dihydrochloride hydrate.
15. The pharmaceutical tablet formulation according to claim 14 , wherein the polyethylene glycol of the semi-permeable membrane has an average molecular weight of 3350.