PERCUTANEOUSLY ABSORBABLE PREPARATION

• US 20100010043A1
• Filed: 05/29/2009
• Published: 01/14/2010
• Est. Priority Date: 05/30/2008
• Status: Abandoned Application

• Current Assignee: Eisai R & D Management Company Limited (Eisai Medical Research Incorporated), Nitto Denko Corporation
• Original Assignee: Eisai R & D Management Company Limited (Eisai Medical Research Incorporated), Nitto Denko Corporation
• Inventors: Nishi, Sumiyo, Terashi, Sachiko, Sekiya, Junichi, Hanatani, Akinori, Akemi, Hitoshi
• Application Number:
  US12/475,249
• Publication Number:
  US 20100010043A1
• Time in Patent Office: Days
• US Class Current: 514/319
• CPC Class Codes: A61K 31/4465 only substituted in position 4
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The present invention provides a percutaneously absorbable preparation comprising 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one and/or a hydrochloride thereof wherein the percuneously absorbable preoaration is able to administer to a patient such that Cmax per unit surface area of the percutaneously absorbable preparation is 0.025 to 0.5 ng/ml·cm² in a plasma concentration profile.

Claims

1. A percutaneously absorbable preparation comprising 2-[(1-benzylpiperidin-4-yl) methyl]-5,6-dimethoxyindan-1-one and/or a hydrochloride thereof,

wherein the percutaneously absorbable preparation is able to administer to a patient such that Cmax per unit surface area of the percutaneously absorbable preparation is 0.025 to 0.5 ng/ml·

cm² in a plasma concentration profile.

2. The percutaneously absorbable preparation according to claim 1, wherein the Cmax is 0.025 to 0.45 ng/ml·

cm².

3. The percutaneously absorbable preparation according to claim 1, wherein the Cmax is 0.05 to 0.4 ng/ml·

cm².

4. The percutaneously absorbable preparation according to claim 1, wherein AUC per unit surface area of the percutaneously absorbable preparation is 7.5 to 75 ng·

hr/ml·

cm².

5. The percutaneously absorbable preparation according to claim 4, wherein the AUC is 10 to 62.5 ng·

hr/ml·

cm².

6. The percutaneously absorbable preparation according to claim 4, wherein the AUC is 12.5 to 50 ng·

hr/ml·

cm².

7. The percutaneously absorbable preparation according to claim 1, wherein Tmax is 12 to 192 hr.

8. The percutaneously absorbable preparation according to claim 7, wherein Tmax is 24 to 180 hr.

9. The percutaneously absorbable preparation according to claim 7, wherein the Tmax is 48 to 168 hr.

10. The percutaneously absorbable preparation according to claim 1, wherein AUC per unit surface area of the percutaneously absorbable preparation is 7.5 to 75 ng·

hr/ml·

cm², and Tmax is 12 to 192 hr.

11. The percutaneously absorbable preparation according to claim 10, wherein the Tmax is 24 to 180 hr.

12. The percutaneously absorbable preparation according to claim 10, wherein the Tmax is 48 to 168 hr.

13. The percutaneously absorbable preparation according to claim 1, wherein AUC per unit surface area of the percutaneously absorbable preparation is 10 to 62.5 ng·

hr/ml·

cm², and Tmax is 12 to 192 hr.

14. The percutaneously absorbable preparation according to claim 13, wherein the Tmax is 24 to 180 hr.

15. The percutaneously absorbable preparation according to claim 13, wherein the Tmax is 48 to 168 hr.

16. The percutaneously absorbable preparation according to claim 1, wherein AUC per unit surface area of the percutaneously absorbable preparation is 12.5 to 50 ng·

hr/ml·

cm², and Tmax is 12 to 192 hr.

17. The percutaneously absorbable preparation according to claim 16, wherein the Tmax is 24 to 180 hr.

18. The percutaneously absorbable preparation according to claim 16, wherein the Tmax is 48 to 168 hr.

28. The percutaneously absorbable preparation according to claim 1, which is applied to 5 to 150 cm² of a skin of the patient.

29. The percutaneously absorbable preparation according to claim 1, which is applied to the patient one to seven times per week.

19. A percutaneously absorbable preparation comprising 2-[(1-benzylpiperidin-4-yl) methyl]-5,6-dimethoxyindan-1-one and/or a hydrochloride thereof,

wherein the percutaneously absorbable preparation js able to administer to a patient such that AUC per unit surface area of the percutaneously absorbable preparation is 7.5 to 75 ng·

hr/ml·

cm² in a plasma concentration profile.

20. The percutaneously absorbable preparation according to claim 19, wherein the AUC is 10 to 62.5 ng·

hr/ml·

cm².

21. The percutaneously absorbable preparation according to claim 19, wherein the AUC is 12.5 to 50 ng·

hr/ml·

cm².

22. The percutaneously absorbable preparation according to claim 19, wherein Tmax is 12 to 192 hr.

23. The percutaneously absorbable preparation according to claim 22, wherein the Tmax is 24 to 180 hr.

24. The percutaneously absorbable preparation according to claim 22, wherein the Tmax is 48 to 168 hr.

25. A percutaneously absorbable preparation comprising 2-[(1-benzylpiperidin-4-yl) methyl]-5,6-dimethoxyindan-1-one and/or a hydrochloride thereof,

wherein the percutaneously absorbable preparation is able to administer to a patient such that Tmax of the plasma concentration profile is 12 to 192 hr.

26. The percutaneously absorbable preparation according to claim 25, wherein the Tmax is 24 to 180 hr.

27. The percutaneously absorbable preparation according to claim 25, wherein the Tmax is 48 to 168 hr.