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Claims for Patent: 8,216,604

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Claims for Patent: 8,216,604

Title:Method of managing or treating pain
Abstract: A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (C.sub.max) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
Inventor(s): Watts; Peter James (Nottingham, GB), Castile; Jonathan David (Nottingham, GB), Lafferty; William Columbus Ian (Leicestershire, GB), Smith; Alan (Nottingham, GB)
Assignee: Archimedes Development Limited (Nottingham, GB)
Application Number:12/047,388
Patent Claims: 1. A method of treating or managing pain by intranasally administering to an animal in need thereof in a single dosage regimen having a practical dose volume to provide rapid absorption in combination with a lower peak plasma concentration than that provided using a simple aqueous solution and in an amount to effectively treat or manage pain, a pharmaceutical composition comprising an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof in an amount to effectively treat or manage pain that is from 0.1 to 30 mg/ml of fentanyl or a pharmaceutically acceptable salt thereof (expressed as fentanyl base) and a pectin having a degree of esterification (DE value) of less than 30%, provided that the composition is substantially free of divalent metal ions; wherein the animal administered the composition in the single dosage regimen is provided with a peak plasma concentration of fentanyl (C.sub.max) that is from 20 to 75% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose; and wherein the intranasal administration of the composition provides a time to achieve peak plasma concentration (T.sub.max) of fentanyl in the animal's plasma of 5 to 30 minutes.

2. A method according to claim 1, wherein the animal administered the composition by the single dosage regimen is provided with a peak plasma concentration of fentanyl (C.sub.max) that is from 30 to 70% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose.

3. A method according to claim 1, wherein the pectin has a DE value of from 7 to 30%.

4. A method according to claim 3, wherein the pectin has a DE value of from 10 to 25%.

5. A method according to claim 1, wherein the pectin has a DE value of from 5 to 25%.

6. A method according to claim 1, wherein the animal administered the composition by the single dosage regimen is provided with a peak plasma concentration of fentanyl (C.sub.max) that is from 30 to 70% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose, and wherein the pectin has a DE value of from 5 to 25%.

7. A method according to claim 1, wherein the composition comprises a pharmaceutically acceptable salt of fentanyl.

8. A method according to claim 7, wherein the pharmaceutically acceptable salt of fentanyl is fentanyl citrate.

9. A method according to claim 1, wherein the composition has a concentration of pectin from 5 to 25 mg/ml of the composition.

10. A method according to claim 1, wherein the composition is at least 99% free of divalent metal ions.

11. A method according to claim 1, wherein the composition has an osmolality of from 0.25 to 0.35 osmol/kg.

12. A method according to claim 1, wherein the composition has a pH of from 3.4 to 5.0.

13. A method according to claim 1, wherein the composition is administered by the single dosage regimen in the form of drops or as a spray.

14. A method according to claim 1 for treating acute or chronic pain.

15. A method according to claim 1, wherein the animal is a human.

16. A method according to claim 1, wherein the composition comprises from 0.1 to 20 mg/ml of the composition of fentanyl or a pharmaceutically acceptable salt thereof (expressed as fentanyl base).

17. A method according to claim 16, wherein the composition comprises from 0.2 to 16 mg/ml of the composition of fentanyl or a pharmaceutically acceptable salt thereof (expressed as fentanyl base) of the composition.

18. A method of treating or managing pain by intranasally administering to an animal in need thereof in a single dosage regimen having a practical dose volume to provide rapid absorption in combination with a lower peak plasma concentration than that provided using a simple aqueous solution and in an amount to effectively treat or manage pain, a pharmaceutical composition comprising an aqueous solution of 0.2 to 16 mg/ml (expressed as fentanyl base) of fentanyl or a pharmaceutically acceptable salt thereof and 5 to 25 mg/ml of a pectin having a DE value of 10 to 25%; the composition having a pH of 3.4 to 5.0 and an osmolality of 0.2 to 0.4 osmol/kg and being substantially free of divalent metal ions; so as to provide in the animal administered the composition a peak plasma concentration of fentanyl (C.sub.max) that is from 20 to 75% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose and a time to achieve peak plasma concentration (T.sub.max), of fentanyl in the animal's plasma of 5 to 30 minutes.

19. A method according to claim 18, wherein the animal is a human.

20. A method according to claim 19, wherein the single dosage regimen of the method further comprises administering the composition to the human via a maximum of two intranasal sprays to each nostril of the human where the maximum volume of each spray is 0.15 ml of the composition.

21. A method according to claim 15, wherein the single dosage regimen of the method further comprises administering the composition to the human via a maximum of two intranasal sprays to each nostril of the human where the maximum volume of each spray is 0.15 ml of the composition.

22. A method of treating or managing pain by intranasally administering to an animal in need thereof in a single dosage regimen having a practical dose volume to provide rapid absorption in combination with a lower peak plasma concentration than that provided using a simple aqueous solution and in an amount to effectively treat or manage pain, a pharmaceutical composition comprising an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof in an amount to effectively treat or manage pain that is from 0.1 to 30 mg/ml of fentanyl or a pharmaceutically acceptable salt thereof (expressed as fentanyl base); a pectin having a degree of esterification (DE value) of less than 30%; and a non-metal ion osmolality adjusting agent in an amount to ensure that the osmolality of the composition is from 0.2 to 0.8 osmol/kg; provided that the composition is substantially free of divalent metal ions; wherein the animal administered the composition is provided with a peak plasma concentration of fentanyl (C.sub.max) that is from 20 to 75% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose; and wherein the intranasal administration of the composition provides a time to achieve peak plasma concentration (T.sub.max) of fentanyl in the animal's plasma of 5 to 30 minutes.

23. The method of claim 22, wherein the non-metal ion osmolality adjusting agent is selected from one or more in the group consisting of mannitol, sorbitol, dextrose, sucrose and trehalose.

24. The method of claim 22, wherein the osmolality of the composition is from 0.2 to 0.4 osmol/kg.

25. The method of claim 24, wherein the osmolality of the composition is from 0.25 to 0.35 osmol/kg.

26. The method of claim 18, wherein the osmolality of the composition is from 0.25 to 0.35 osmol/kg.
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