Claims
- 1. A pharmaceutical composition comprising,
a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof wherein said piperidinoalkanol compound has a particle surface area of greater than about 1.0 m2/g; and b) at least one inert ingredient.
- 2. The pharmaceutical composition according to claim 1 wherein the inert ingredient is a disintegrant.
- 3. A pharmaceutical composition in solid unit dosage form, comprising;
a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and b) at least one inert ingredient.
- 4. The pharmaceutical composition in solid unit dosage form according to claim 3 wherein the inert ingredient is a disintegrant.
- 5. The pharmaceutical composition in solid unit dosage form according to claim 3, wherein said piperidinoalkanol compound is of the formula
- 6. The pharmaceutical composition in solid unit dosage form according to claim 5, wherein X is zero.
- 7. The pharmaceutical composition in solid unit dosage form according to claim 5, wherein at least one inert ingredient is selected from the group consisting of croscarmellose sodium, lactose, microcrystalline cellulose, pregelatinized starch, gelatin, calcium carbonate, magnesium stearate and sodium starch glycolate.
- 8. The pharmaceutical composition in solid unit dosage form according to claim 7 wherein said inert ingredients comprise croscarmellose sodium, lactose, microcrystalline cellulose, pregelatinized starch and gelatin.
- 9. The pharmaceutical composition in solid unit dosage form according to claim 8 wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch and gelatin are present in amounts of about 1% to about 10%, 20% to about 85%, 20% to about 85%, 1% to about 30% and 1% to about 15%, respectively, by weight of the composition.
- 10. The pharmaceutical composition in solid unit dosage form according to claim 8 wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch and gelatin are present in amounts of about 4.8%, 33.8%, 33.8%, 9.6% and 3.5%, respectively, by weight of the composition.
- 11. The pharmaceutical composition in solid unit dosage form according to claim 7 wherein said inert ingredients comprise microcrystalline cellulose, pregelatinized starch, gelatin, magnesium stearate, calcium carbonate and sodium starch glycolate.
- 12. The pharmaceutical composition in solid unit dosage form according to claim 11 wherein microcrystalline cellulose, pregelatinized starch, gelatin, magnesium stearate, calcium carbonate and sodium starch glycolate are present in amounts of about 20% to about 85%, 5% to about 50%, 1% to about 15%, 0.05% to about 3%, 5% to about 50% and 1% to about 15%, respectively, by weight of the composition.
- 13. The pharmaceutical composition in solid unit dosage form according to claim 11 wherein microcrystalline cellulose, pregelatinized starch, gelatin, magnesium stearate, calcium carbonate and sodium starch glycolate are present in amounts of about 34.9%, 29.4%, 3.3%, 0.5%, 15.6%, 5.6%, respectively, by weight of the composition.
- 14. The pharmaceutical composition in solid unit dosage form according to claim 7 wherein said inert ingredients comprise croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate.
- 15. The pharmaceutical composition in solid unit dosage form according to claim 14 wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are present in amounts of about 1% to about 10%, 20% to about 85%, 20% to about 85%, 1% to about 30%, 1% to about 15% and 0.05% to about 3.0%, respectively, by weight of the composition.
- 16. The pharmaceutical composition in solid unit dosage form according to claim 14 wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are present in amounts of about 4.8%, 33.7%, 33.7%, 9.6%, 3.5% and 0.5%, respectively, by weight of the composition.
- 17. The pharmaceutical composition in solid unit dosage form according to claim 14 wherein croscarmellose sodium, microcrystalline cellulose, lactose, pregelatinized starch, gelatin and magnesium stearate are present in amounts of about 4.8%, 25.7%, 25.7%, 9.6%, 3.5% and 0.75%, respectively, by weight of the composition.
- 18. The pharmaceutical composition in solid unit dosage form according to claim 7 wherein said inert ingredients comprise microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate.
- 19. The pharmaceutical composition in solid unit dosage form according to claim 18 wherein microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate are present in amounts of about 20% to about 85%, 5% to about 50%, 0.05% to about 3%, 5% to about 50% and 1% to about 15%, respectively, by weight of the composition.
- 20. The pharmaceutical composition in solid unit dosage form according to claim 18 wherein microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate are present in amounts of about 36.5%, 31.0%, 0.5%, 15.6%, and 5.6%, respectively, by weight of the composition.
- 21. The pharmaceutical composition in solid unit dosage form according to claim 18 wherein microcrystalline cellulose, pregelatinized starch, magnesium stearate, calcium carbonate and sodium starch glycolate are present in amounts of about 21.1%, 30.0%, 0.75%, 15.6%, and 10.0%, respectively, by weight of the composition.
- 22. The pharmaceutical composition in solid unit dosage form according to claim 7 wherein said inert ingredients comprise croscarmellose sodium, microcrystalline cellulose, pregelatinized starch, and magnesium stearate.
- 23. The pharmaceutical composition in solid unit dosage form according to claim 22 wherein croscarmellose sodium, microcrystalline cellulose, pregelatinized starch, and magnesium stearate are present in amounts of about 1% to about 10%, 20% to about 85%, 5% to about 50% and 0.05% to about 3%, respectively, by weight of the composition.
- 24. The pharmaceutical composition in solid unit dosage form according to claim 22 wherein croscarmellose sodium, microcrystalline cellulose, pregelatinized starch, and magnesium stearate are present in amounts of about 6%, 33.3%, 30% and 0.75%, respectively, by weight of the composition.
- 25. The pharmaceutical composition in solid unit dosage form as in either claims 10, 13, 16, 17, 20, 21 or 24 wherein said piperidinoalkanol compound is 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylbenzeneacetic acid hydrochloride.
- 26. The pharmaceutical composition in solid unit dosage form according to claim 25 wherein 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylbenzeneacetic acid hydrochloride is present in an amount of about 5 mg to about 180 mg.
- 27. A pharmaceutical composition prepared by a wet granulation process comprising, preparing the wet granulation wherein a compound of formula;
- 28. A pharmaceutical composition prepared by a wet granulation process comprising, preparing the wet granulation wherein a compound of formula;
- 29. A pharmaceutical composition in solid unit dosage form prepared by a process comprising, blending together a compound of the formula;
- 30. A pharmaceutical composition in solid unit dosage form according to claim 29 wherein the resulting mixture is filled into capsules.
- 31. A pharmaceutical composition in solid unit dosage form according to claim 29 wherein the microcrystalline cellulose, lactose, pregelatinized starch, gelatin and croscarmellose sodium are combined in amounts of about 33.8%, 33.8%, 9.6%, 3.5% and 4.8%, respectively, by weight of the composition.
- 32. A pharmaceutical composition in solid unit dosage form according to claim 29 wherein the microcrystalline cellulose, lactose, pregelatinized starch, gelatin, croscarmellose sodium and magnesium stearate are combined in amounts of about 33.7%, 33.7%, 9.6%, 3.5%, 4.8% and 0.5%, respectively, by weight of the composition.
- 33. A pharmaceutical composition in solid unit dosage form prepared by a process comprising blending together a compound of the formula;
- 34. A pharmaceutical composition in solid unit dosage form according to claim 33 wherein the final mixture is pressed into tablets.
- 35. A pharmaceutical composition in solid unit dosage form according to claim 33 wherein the microcrystalline cellulose, lactose, pregelatinized starch, gelatin, croscarmellose sodium and magnesium stearate are combined in amounts of about 33.7%, 33.7%, 9.6%, 3.5%, 4.8% and 0.5%, respectively, by weight of the composition.
- 36. A pharmaceutical composition in solid unit dosage form prepared by a process comprising blending together a compound of the formula;
- 37. A pharmaceutical composition in solid unit dosage form according to claim 36 wherein the final mixture is pressed into tablets.
- 38. A pharmaceutical composition in solid unit dosage form according to claim 36 wherein the microcrystalline cellulose, calcium carbonate, pregelatinized starch, gelatin, sodium starch glycolate and magnesium stearate are combined in total amounts of about 34.9%, 15.6%, 29.4%, 3.3%, 5.6% and 0.5%, respectively, by weight of the composition.
- 39. A pharmaceutical composition in solid unit dosage form prepared by a process comprising blending together a compound of the formula;
- 40. A pharmaceutical composition in solid unit dosage form according to claim 39 wherein the final mixture is pressed into tablets.
- 41. A pharmaceutical composition in solid unit dosage form according to claim 39 wherein the microcrystalline cellulose, calcium carbonate, pregelatinized starch, sodium starch glycolate and magnesium stearate are combined in total amounts of about 336.5%, 15.6%, 31.0%, 5.6% and 0.5%, respectively, by weight of the composition.
- 42. A pharmaceutical composition in solid form according to claim 16 wherein the final mixture is pressed into a tablet from which the quantity of compound of the formula;
- 43. A pharmaceutical composition in solid form according to claims 17, 21 or 24 wherein the final mixture is pressed into a tablet from which the quantity of compound of the formula;
CROSS-REFERENCE TO RELATED APPLICATION
[0001] This is a continuation-in-part of application Ser. No. 08/395,952 filed Feb. 28, 1995.
Divisions (1)
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Number |
Date |
Country |
Parent |
08943460 |
Oct 1997 |
US |
Child |
09157841 |
Sep 1998 |
US |
Continuations (5)
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Date |
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Parent |
10039798 |
Jan 2002 |
US |
Child |
10347953 |
Jan 2003 |
US |
Parent |
09845966 |
Apr 2001 |
US |
Child |
10039798 |
Jan 2002 |
US |
Parent |
09586743 |
Jun 2000 |
US |
Child |
09845966 |
Apr 2001 |
US |
Parent |
09157841 |
Sep 1998 |
US |
Child |
09586743 |
Jun 2000 |
US |
Parent |
08552287 |
Dec 1995 |
US |
Child |
08943460 |
Oct 1997 |
US |
Continuation in Parts (1)
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Number |
Date |
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Parent |
08395952 |
Feb 1995 |
US |
Child |
08552287 |
Dec 1995 |
US |