Pharmaceutical compositions containing flibanserin
The invention relates to oral pharmaceutical compositions containing flibanserin, methods for the preparation thereof and use thereof as a medicament.
1 . A pharmaceutical composition for oral administration comprising a tablet core containing flibanserin polymorph A having an endothermic maximum at about 161° C., as determined using DSC, in admixture with at least one pharmaceutically acceptable excipient and further comprising a film coating comprising titanium dioxide and/or talc, enveloping said tablet core, wherein the pharmaceutical composition is a tablet.
2 . A pharmaceutical composition according to claim 1 , wherein the titanium dioxide is present in the amounts of 5-55 wt. % based on the total mass of the film coating of the film coated tablet.
3 . A pharmaceutical composition according to claim 1 , wherein the talc is present in the amounts of 5-50 wt. % based on the total mass of the film coating of the film coated tablet.
4 . A pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipient is a filler selected from lactose monohydrate, spray-dried lactose, agglomerated lactose, anhydrous lactose, microcrystalline cellulose, dibasic calcium phosphate, cornstarch, sugar alcohols and mixtures thereof.
5 . A pharmaceutical composition according to claim 4 , wherein the pharmaceutically acceptable excipient is lactose monohydrate.
6 . A pharmaceutical composition according to claim 4 , wherein the pharmaceutically acceptable excipient is a mixture of lactose monohydrate and microcrystalline cellulose.
7 . A pharmaceutical composition according to claim 4 , wherein the pharmaceutically acceptable excipient is a mixture of dibasic calcium phosphate and microcrystalline cellulose.
8 . A pharmaceutical composition according to claim 1 , wherein flibanserin polymorph A is present in an amount of 1 to 50 wt. % based on the total mass of the core.
9 . A pharmaceutical composition according to claim 1 , wherein flibanserin polymorph A is present in an amount of 15 to 35 wt. % based on the total mass of the core.
10 . A pharmaceutical composition according to claim 1 , wherein the core contains filler in an amount of 50 to 99 wt. % based on the total mass of the core.
11 . A pharmaceutical composition according to claim 1 , wherein the core contains filler in an amount of 65 to 85 wt. % based on the total mass of the core.
12 . A pharmaceutical composition according to claim 1 , wherein the core additionally contains a binding agent selected from povidone, copovidone, hydroxypropyl methylcellulose, hydroxypropylcellulose, corn starch and mixtures thereof.
13 . A pharmaceutical composition according to claim 12 , wherein the binding agent is hydroxypropyl methylcellulose.
14 . A pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipient is a mixture of lactose monohydrate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose.
15 . A pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipient is a mixture of dibasic calcium phosphate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose.
16 . A pharmaceutical composition according to claim 1 , wherein the core additionally contains a disintegrant selected from sodium starch glycolate, crospovidone, croscarmellose sodium, sodium-carboxymethylcellulose, dried corn starch and mixtures thereof.
17 . A pharmaceutical composition according to claim 16 , wherein the disintegrant is sodium-carboxymethylcellulose.
18 . A pharmaceutical composition according to claim 1 , wherein the core additionally contains one or more flow regulators, lubricants and mould release or antiadhesive agents selected from silicon dioxide, talc, magnesium stearate and mixtures thereof.
19 . A pharmaceutical composition according to claim 1 , wherein the film coating enveloping the core contains at least one film-forming agent selected from hydroxypropyl methylcellulose, hydroxypropylcellulose, methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose and poly(ethylacryate) methylmethacrylate.
20 . A pharmaceutical composition according to claim 19 , wherein the film coating enveloping the core contains hydroxypropyl methylcellulose.
21 . A pharmaceutical composition according to claim 1 , wherein the film coating enveloping the core contains one or more emulsifiers or plasticizers selected from polyethylene glycol, glycerol and propylene glycol.
22 . A pharmaceutical composition according to claim 21 , wherein the film coating enveloping the core contains polyethylene glycol.
23 . A pharmaceutical composition according to claim 1 , wherein the film coating enveloping the core contains hydroxypropyl methylcellulose and polyethylene glycol.
24 . A pharmaceutical composition according to claim 1 , wherein the film coating enveloping the core contains hydroxypropyl methylcellulose, polyethylene glycol and titanium dioxide.
25 . A pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipient is a mixture of lactose monohydrate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose and the film coating enveloping the core contains hydroxypropyl methylcellulose and polyethylene glycol.
26 . A pharmaceutical composition according to claim 1 , wherein the pharmaceutically acceptable excipient is a mixture of dibasic calcium phosphate and microcrystalline cellulose and the core additionally contains hydroxypropyl methylcellulose and the film coating enveloping the core contains hydroxypropyl methylcellulose and polyethylene glycol.