Pharmaceutical composition
Provided is a pharmaceutical composition which contains pemafibrate, a salt thereof or a solvate thereof and one or more selected from the group consisting of a metal oxide, a dihydric alcohol, an ester species and a silicic acid compound and which has excellent storage stability. The pharmaceutical composition includes the following components (A) and (B):(A) pemafibrate, a salt thereof or a solvate thereof; and (B) one or more selected from the group consisting of the following components (B-1) to (B-4):(B-1) a metal oxide; (B-2) a dihydric alcohol; (B-3) an ester species; and (B-4) a silicic acid compound, with component (A) and component (B) being substantially in non-contact with each other.
1 . A solid pharmaceutical composition, comprising:
an active component comprising pemafibrate, a salt thereof or a solvate thereof; and
at least one ester species selected from the group consisting of acetyltriethyl citrate, acetyltributyl citrate, triethyl citrate, tributyl citrate and triacetin,
wherein the active component and the at least one ester species are formulated substantially in non-contact with each other such that the pemafibrate is substantially in non-contact with the at least one ester species, and
wherein a total content of the at least one ester species with respect to 1 part by mass of a free form of pemafibrate is from 1 to 10 parts by mass.
2 . The pharmaceutical composition according to claim 1 , wherein the pharmaceutical composition has a dosage form that is a tablet, a capsule, a granule, a powder or a pill.
3 . The pharmaceutical composition according to claim 1 , wherein the at least one ester species is at least one selected from the group consisting of triethyl citrate and triacetin.
4 . The pharmaceutical composition according to claim 1 , further comprising:
at least one component incorporated such that the active component and the at least one ester species are formulated substantially in non-contact with each other by the at least one component and the pemafibrate is substantially in non-contact with the at least one ester species.
5 . The pharmaceutical composition according to claim 4 , wherein the at least one component comprises an additive component.
6 . The pharmaceutical composition according to claim 1 , further comprising:
a plurality of components incorporated such that the active component and the at least one ester species are formulated substantially in non-contact with each other by the components and the pemafibrate is substantially in non-contact with the at least one ester species.
7 . The pharmaceutical composition according to claim 6 , wherein the plurality of components comprises an additive component.
8 . A pharmaceutical composition, comprising:
a film-coated tablet comprising a core tablet and a film coating layer,
wherein the core tablet comprising an active component comprising pemafibrate, a salt thereof or a solvate thereof, and the film coating layer comprising at least one ester species selected from the group consisting of acetyltriethyl citrate, acetyltributyl citrate, triethyl citrate, tributyl citrate and triacetin are formulated such that the pemafibrate in the core tablet is substantially in non-contact with the at least one ester species, and
wherein a total content of the at least one ester species with respect to 1 part by mass of a free form of pemafibrate is from 1 to 10 parts by mass.
9 . The pharmaceutical composition of claim 8 , wherein the core table comprises the active component and at least one binder selected from the group consisting of methylcellulose, hydroxypropyl cellulose, hypromellose, carmellose sodium, a starch selected from the group consisting of wheat starch, rice starch, corn starch, and partially pregelatinized starch dextrin, pullulan, acacia, agar, gelatin, tragacanth, sodium alginate, povidone and polyvinyl alcohol.
10 . The pharmaceutical composition according to claim 8 , wherein the core tablet comprises at least one component such that the active component in the core tablet and the at least one ester species in the film coating layer are formulated substantially in non-contact with each other by the at least one component and the pemafibrate is substantially in non-contact with the at least one ester species.
11 . The pharmaceutical composition according to claim 10 , wherein the at least one component comprises an additive component.
12 . The pharmaceutical composition according to claim 8 , wherein the core tablet comprises a plurality of components such that the active component in the core tablet and the at least one ester species in the film coating layer are formulated substantially in non-contact with each other by the components and the pemafibrate is substantially in non-contact with the at least one ester species.
13 . The pharmaceutical composition according to claim 12 , wherein the plurality of components comprises an additive component.
14 . A pharmaceutical composition, comprising:
a film-coated tablet comprising a core tablet and a film coating layer,
wherein the core tablet comprising an active component comprising pemafibrate, a salt thereof or a solvate thereof, and the film coating layer comprising at least one of a metal oxide, a dihydric alcohol and a silicic acid compound, and at least one ester species selected from the group consisting of acetyltriethyl citrate, acetyltributyl citrate, triethyl citrate, tributyl citrate and triacetin are formulated such that the pemafibrate is not in contact with the at least one of the metal oxide, the dihydric alcohol and the silicic acid compound, and the at least one ester species, and
wherein a total content of the at least one ester species with respect to 1 part by mass of a free form of pemafibrate is from 1 to 10 parts by mass.
15 . The pharmaceutical composition according to claim 14 , wherein the core tablet comprises at least one component such that the active component in the core tablet and the at least one ester species and the at least one of the metal oxide, the dihydric alcohol, the silicic acid compound in the film coating layer are formulated substantially in non-contact with each other by the at least one component and the pemafibrate is substantially in non-contact with the at least one ester species.
16 . The pharmaceutical composition according to claim 15 , wherein the at least one component comprises an additive component.
17 . The pharmaceutical composition according to claim 14 , wherein the core tablet comprises a plurality of components such that the active component in the core tablet and the at least one ester species and the at least one of the metal oxide, the dihydric alcohol and the silicic acid compound in the film coating layer are formulated substantially in non-contact with each other by the components and the pemafibrate is substantially in non-contact with the at least one ester species.
18 . The pharmaceutical composition according to claim 17 , wherein the plurality of components comprises an additive component.
19 . A method for stabilizing pemafibrate, a salt thereof or a solvate thereof in a pharmaceutical composition, comprising:
incorporating an active component comprising pemafibrate, a salt thereof or a solvate thereof, and at least one ester species selected from the group consisting of acetyltriethyl citrate, acetyltributyl citrate, triethyl citrate, tributyl citrate and triacetin such that the active component and the at least one ester species are formulated substantially in non-contact with each other such that the pemafibrate is substantially in non-contact with the at least one ester species, and
wherein a total content of the at least one ester species with respect to 1 part by mass of a free form of pemafibrate is from 1 to 10 parts by mass.
20 . The pharmaceutical composition according to claim 19 , wherein the at least one ester species is at least one selected from the group consisting of triethyl citrate and triacetin.