Process for the preparation of roflumilast
View Patent ↗A composition comprising: roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.
1. A composition comprising: roflumilast having a purity of greater than or equal to 99% by weight, and N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight.
2. The composition of claim 1 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
3. The composition of claim 1 , wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.
4. A pharmaceutical composition, comprising: roflumilast having a purity of greater than or equal to 99% by weight; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.
5. The pharmaceutical composition of claim 4 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
6. The pharmaceutical composition of claim 4 , wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.
7. A pharmaceutical dosage form, comprising: roflumilast having a purity of greater than or equal to 99% by weight; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount greater than zero and less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.
8. The pharmaceutical dosage form of claim 7 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
9. The pharmaceutical dosage form of claim 7 , wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.
10. The pharmaceutical dosage form of claim 7 , wherein said form is selected from the group consisting of tablets, coated tablets, capsules, caplets, suppositories, emulsions, suspensions, gels and solutions.
11. The pharmaceutical dosage form of claim 7 , wherein said dosage form includes from between 0.1% and 95% roflumilast.
12. The pharmaceutical dosage form of claim 7 , wherein the form is an oral dosage form.
13. The oral dosage form of claim 12 , containing from 0.05 mg to 2.5 mg of roflumilast.
14. The oral dosage form of claim 13 , containing from 0.1 to 0.5 mg of roflumilast.
15. The oral dosage form of claim 14 , containing 0.25 mg of roflumilast.
16. The oral dosage form of claim 14 , containing 0.5 mg of roflumilast.
17. A pharmaceutical tablet, comprising: 0.5 mg of roflumilast having a purity of greater than or equal to 99% by weight; N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide present (relative to roflumilast) in an amount less than 0.1% by weight; and pharmaceutically acceptable auxiliaries and/or excipients.
18. The pharmaceutical tablet of claim 17 , wherein said roflumilast has a purity of greater than or equal to 99.8% by weight.
19. The pharmaceutical tablet of claim 17 , wherein said N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-hydroxybenzamide is present (relative to roflumilast) in an amount greater than zero and less than 0.05% by weight.