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Claims for Patent: 8,729,085

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Claims for Patent: 8,729,085

Title:Pharmaceutical composition
Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethyle- ne-butyl]-(1'R,2'S,3'R,4'S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.
Inventor(s): Fujihara; Kazuyuki (Ibaraki, JP)
Assignee: Dainippon Sumitomo Pharma Co., Ltd. (Osaka, JP)
Application Number:11/919,678
Patent Claims: 1. An oral preparation which comprises N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethyle- ne-butyl]-(1'R,2'S,3'R,4'S)-2,3-bicyclo[2,2,1]heptanedicarboxylmide hydrochloride (lurasidone) of the formula (1): ##STR00003## a pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder; wherein a content of lurasidone in the preparation is 20 to 45% (wt/wt), and the pregelatinized starch is incorporated in an amount of 20 to 50% (wt/wt) based on the weight of the preparation.

2. The oral preparation of claim 1 wherein the water-soluble excipient is mannitol or lactose.

3. The oral preparation of claim 1 wherein the pregelatinized starch is incorporated in an amount of 20 to 30% (wt/wt) based on the weight of the preparation.

4. The oral preparation of claim 1 wherein a content of lurasidone per tablet is 10 to 160 mg.

5. The oral preparation of claim 1 wherein a content of lurasidone per tablet is 20 to 120 mg.

6. The oral preparation of claim 1 wherein a content of lurasidone per tablet is 40 to 120 mg.

7. The oral preparation of claim 1 wherein the water-soluble excipient is mannitol or lactose and a content of lurasidone in the preparation is 25 to 40% (wt/wt).

8. The oral preparation of claim 1 wherein the water-soluble excipient is mannitol or lactose, the pregelatinized starch is incorporated in an amount of 20 to 30% (wt/wt) based on the weight of the preparation and a content of lurasidone per tablet is 40 to 120 mg.

9. The oral preparation of claim 1 wherein a pregelatinizing ratio of the pregelatinized starch is 50 to 95%.

10. The oral preparation of claim 1 wherein a 50 by volume particle size of lurasidone is 0.1 to 8 .mu.m.

11. The oral preparation of claim 1 wherein the pregelatinized starch contains water soluble matter of 30% or less.

12. The oral preparation of claim 1 wherein the water-soluble excipient is mannitol or lactose, the pregelatinized starch is incorporated in an amount of 20 to 30% (wt/wt) based on the weight of the preparation, and a content of lurasidone per tablet is 20 to 120 mg.

13. The oral preparation of claim 3 wherein the water-soluble excipient is mannitol or lactose.

14. The oral preparation of claim 1 wherein the water-soluble polymer binder is hydroxypropyl methylcellulose, polyvinyl alcohol, polyvinylpyrrolidone or hydroxypropylcellulose.

15. The oral preparation of claim 1 wherein a content of the water-soluble polymer binder per tablet is 0.5 to 10% (wt/wt).

16. The oral preparation of claim 1, further comprising a disintegrant wherein a content of the disintegrant per tablet is 0.5 to 5% (wt/wt).

17. The oral preparation of claim 1, further comprising a disintegrant wherein a content of the disintegrant per tablet is 0.5 to 5% (wt/wt); the pregelatinized starch is incorporated in an amount of 20 to 30% (wt/wt) based on the weight of the preparation; a content of lurasidone per tablet is 40 to 120 mg; a pregelatinizing ratio of the pregelatinized starch is 50 to 95%; 50% by volume particle size of lurasidone is 0.1 to 8 .mu.m; the pregelatinized starch contains water soluble matter of 30% or less; the water-soluble excipient is mannitol or lactose; the water-soluble polymer binder is hydroxypropyl methylcellulose, polyvinyl alcohol, polyvinylpyrrolidone or hydroxypropylcellulose; and a content of the water-soluble polymer binder per tablet is 0.5 to 10% (wt/wt).

18. The oral preparation of claim 1 wherein a content of lurasidone per tablet is 20 to 160 mg.

19. The oral preparation of claim 1, wherein a similarity factor f2 of each preparation is in the range of 50.ltoreq.f2.ltoreq.100 when a content of lurasidone per tablet changes over a range of 20 to 120 mg.

20. An oral preparation which comprises N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethyle- ne-butyl]-(1'R,2'S,3'R,4'S)-2,3-bicyclo[2,2,1]heptanedicarboxylmide hydrochloride (lurasidone) of the formula (1): ##STR00004## a pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder, wherein the oral preparation contains 20 to 45% (wt/wt) of lurasidone, the oral preparation contains 20 mg to 120 mg of lurasidone, the pregelatinized starch is incorporated in an amount of 20 to 50% (wt/wt) based on the weight of the oral preparation, and the oral preparation exhibits an equivalent dissolution profile across the range of lurasidone per oral preparation.

21. The oral preparation of claim 1, wherein the water-soluble excipient is one or more selected from the group of mannitol, lactose, saccharose, sorbitol, D-sorbitol, erythritol and xylitol.

22. The oral preparation of claim 16, wherein the disintegrant is one or more selected from the group of corn starch, crystalline cellulose, low substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, carboxymethyl starch sodium and crospovidone.

23. The oral preparation of claim 1, further comprising a lubricant, wherein a content of the lubricant per tablet is 1.0% (wt/wt) to 1.43% (wt/wt).

24. The oral preparation of claim 23, wherein the lubricant is selected from the group of magnesium stearate, talc, polyethylene glycol, silica and hydrogenated vegetable oil.

25. The oral preparation of claim 1, wherein the oral preparation is a tablet.

26. An oral preparation which comprises N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethyle- ne-butyl]-(1'R,2'S,3'R,4'S)-2,3-bicyclo[2,2,1]heptanedicarboxylmide hydrochloride (lurasidone), a pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder, wherein a content of lurasidone in the preparation is 20 to 45% (wt/wt), the pregelatinized starch is incorporated in an amount of 20 to 30% (wt/wt) based on the weight of the preparation, the water-soluble excipient is mannitol or lactose, and the water-soluble polymer binder is one or more agents selected from the group of hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone and polyvinyl alcohol.

27. An oral preparation which comprises N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethyle- ne-butyl]-(1'R,2'S,3'R,4S)-2,3-bicyclo[2,2,1]heptanedicarboxylmide hydrochloride (lurasidone), a pregelatinized starch, a water-soluble excipient and a water-soluble polymer binder, and further comprises a disintegrant and a lubricant, wherein a content of lurasidone in the preparation is 20 to 45% (wt/wt), the pregelatinized starch is incorporated in an amount of 20 to 30% (wt/wt) based on the weight of the preparation, the water-soluble excipient is mannitol, the water-soluble polymer binder is hydroxypropylmethylcellulose, and the oral preparation is a tablet.
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