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Claims for Patent: 6,344,212

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Claims for Patent: 6,344,212

Title: Method of providing sustained analgesia with buprenorphine
Abstract:A method of effectively treating pain in humans is achieved by administering buprenorphinein accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.
Inventor(s): Reder; Robert F. (Greenwich, CT), Kaiko; Robert F. (Weston, CT), Goldenheim; Paul D. (Wilton, CT)
Assignee: Euro-Celtique S.A. (Luxembourg, LU)
Application Number:09/756,419
Patent Claims: 1. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients by applying a transdermal delivery system to the skin of said patient, and maintaining said transdermal delivery system in contact with said patient's skin for at least 5 days such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 0.3 to about 113 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 3 to about 296 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 7 to about 644 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 13 to about 753 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 16 to about 984 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 20 to about 984 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 21 to about 1052 pg/ml at about 72 hours after initiation of the dosing interval; and

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 19 to about 1052 pg/ml over at least the next 48 hours.

2. The method of claim 1, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 23 to about 1052 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 23 to about 1052 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 22 to about 970 pg/ml at about 144 hours after initiation of the dosing interval; and

a mean plasma concentration from about 19 to about 841 pg/ml at about 168 hours after initiation of the dosing interval.

3. The method of claim 2, further comprising maintaining a mean relative release rate from about 3 ug/hr to about 86 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate from about 0.3 ug/hr to about 9 ug/hr from about 72 hours after the initiation of the dosing interval until the end of dosing interval.

4. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients by applying a transdermal delivery system to the skin of said patient, and maintaining said transdermal delivery system in contact with said patient's skin for at least 5 days such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 1 to about 28 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 14 to about 74 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 30 to about 161 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 51 to about 188 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 62 to about 246 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 79 to about 246 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 85 to about 263 pg/ml at about 72 hours after initiation of the dosing interval; and

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 77 to about 263 pg/ml over at least the next 48 hours.

5. The method of claim 4, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 92 to about 263 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 94 to about 263 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 86 to about 243 pg/ml at about 144 hours after initiation of the dosing interval; and

a mean plasma concentration from about 77 to about 210 pg/ml at about 168 hours after initiation of the dosing interval.

6. The method of claim 5, further comprising maintaining a mean relative release rate of from about 13 ug/hr to about 21 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate of about 1 ug/hr to about 2 ug/hr from about 72 hours after the initiation of the dosing interval until the end of the seven-day dosing interval.

7. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients by applying a transdermal delivery system to the skin of said patient, and maintaining said transdermal delivery system in contact with said patient's skin for at least 5 days such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 0.3 to about 7 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 4 to about 19 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 7 to about 40 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 13 to about 47 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 16 to about 62 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 20 to about 62 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 21 to about 66 pg/ml at about 72 hours after initiation of the dosing interval; and

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 19 to about 66 pg/ml over at least the next 48 hours.

8. The method of claim 1, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 23 to about 66 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 23 to about 66 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 22 to about 61 pg/ml at about 144 hours after initiation of the dosing interval; and

a mean plasma concentration from about 19 to about 53 pg/ml at about 168 hours after initiation of the dosing interval.

9. The method of claim 8, further comprising maintaining a mean relative release rate of from about 3 ug/hr to about 5 ug/hr from the initiation of the seven-day dosing interval until about 72 hours after the initiation of the seven-day dosing interval; and

a mean relative release rate of about 0.3 ug/hr to about 0.6 ug/hr from about 72 hours after the initiation of the dosing interval until the end of the dosing interval.

10. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients by applying a transdermal delivery system to the skin of said patient, and maintaining said transdermal delivery system in contact with said patient's skin for at least 5 days such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 0.7 to about 14 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 7 to about 37 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 15 to about 80 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 25 to about 94 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 31 to about 123 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 40 to about 123 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 42 to about 132 pg/ml at about 72 hours after initiation of the dosing interval; and

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 38 to about 132 pg/ml over at least the next 48 hours.

11. The method of claim 10, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 46 to about 132 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 47 to about 132 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 43 to about 121 pg/ml at about 144 hours after initiation of the dosing interval; and

a mean plasma concentration from about 38 to about 105 pg/ml at about 168 hours after initiation of the dosing interval.

12. The method of claim 11, further comprising maintaining a mean relative release rate of from about 6 ug/hr to about 11 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate of about 0.7 ug/hr to about 1 ug/hr from about 72 hours after the initiation of the dosing interval until the end of the dosing interval.

13. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients by applying a transdermal delivery system to the skin of said patient, and maintaining said transdermal delivery system in contact with said patient's skin for at least 5 days such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 3 to about 57 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 28 to about 148 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 59 to about 322 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 102 to about 377 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 124 to about 492 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 159 to about 492 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 169 to about 526 pg/ml at about 60 hours after initiation of the dosing interval;

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 153 to about 526 pg/ml over at least the next 48 hours.

14. The method of claim 13, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 184 to about 526 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 187 to about 526 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 173 to about 485 pg/ml at about 144 hours after initiation of the dosing interval;

a mean plasma concentration from about 153 to about 420 pg/ml at about 168 hours after initiation of the dosing interval.

15. The method of claim 14, further comprising maintaining a mean relative release rate of from about 26 ug/hr to about 43 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate of about 2 ug/hr to about 4 ug/hr from about 72 hours after the initiation of the dosing interval until the end of the dosing interval.

16. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients by applying a transdermal delivery system to the skin of said patient, and maintaining said transdermal delivery system in contact with said patient's skin for at least 5 days such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 4 to about 85 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 42 to about 222 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 89 to about 483 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 152 to about 565 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 186 to about 738 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 238 to about 738 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 254 to about 789 pg/ml at about 60 hours after initiation of the dosing interval;

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 230 to about 789 pg/ml over at least the next 48 hours.

17. The method of claim 16, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 276 to about 789 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 281 to about 789 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 259 to about 727 pg/ml at about 144 hours after initiation of the dosing interval;

a mean plasma concentration from about 230 to about 630 pg/ml at about 168 hours after initiation of the dosing interval.

18. The method of claim 17, further comprising maintaining a mean relative release rate of from about 38 ug/hr to about 64 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate of about 4 ug/hr to about 7 ug/hr from about 72 hours after the initiation of the dosing interval until the end of the dosing interval.

19. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients in a manner such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 5 to about 113 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 55 to about 296 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 118 to about 644 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 203 to about 753 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 247 to about 984 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 317 to about 984 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 339 to about 1052 pg/ml at about 72 hours after initiation of the dosing interval; and thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 306 to about 1052 pg/ml over at least the next 48 hours.

20. The method of claim 19, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 369 to about 1052 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 374 to about 1052 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 346 to about 970 pg/ml at about 144 hours after initiation of the dosing interval;

a mean plasma concentration from about 306 to about 841 pg/ml at about 168 hours after initiation of the dosing interval.

21. The method of claim 20, further comprising maintaining a mean relative release rate of from about 51 ug/hr to about 86 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate of about 5 ug/hr to about 9 ug/hr from about 72 hours after the initiation of the dosing interval until the end of the dosing interval.

22. A method of effectively treating pain in humans, comprising administering buprenorphine to human patients in a manner selected from the group consisting of parenteral, sublingual, oral, buccal and rectal administration such that the following mean plasma concentrations are achieved over a 72 hour dosing interval:

a mean plasma concentration from about 0.3 to about 113 pg/ml at about 6 hours after initiation of the dosing interval;

a mean plasma concentration from about 3 to about 296 pg/ml at about 12 hours after initiation of the dosing interval;

a mean plasma concentration from about 7 to about 644 pg/ml at about 24 hours after initiation of the dosing interval;

a mean plasma concentration from about 13 to about 753 pg/ml at about 36 hours after initiation of the dosing interval;

a mean plasma concentration from about 16 to about 984 pg/ml at about 48 hours after initiation of the dosing interval;

a mean plasma concentration from about 20 to about 984 pg/ml at about 60 hours after initiation of the dosing interval;

a mean plasma concentration from about 21 to about 1052 pg/ml at about 72 hours after initiation of the dosing interval; and

thereafter administering the buprenorphine in a manner such that the mean plasma concentrations are maintained from about 19 to about 1052 pg/ml over at least the next 48 hours.

23. The method of claim 22, further comprising administering the buprenorphine in a manner such that the mean plasma concentrations are maintained as follows:

a mean plasma concentration from about 23 to about 1052 pg/ml at about 96 hours after initiation of the dosing interval;

a mean plasma concentration from about 23 to about 1052 pg/ml at about 120 hours after initiation of the dosing interval;

a mean plasma concentration from about 22 to about 970 pg/ml at about 144 hours after initiation of the dosing interval; and

a mean plasma concentration from about 19 to about 841 pg/ml at about 168 hours after initiation of the dosing interval.

24. The method of claim 23, further comprising maintaining a mean relative release rate from about 3 ug/hr to about 86 ug/hr from the initiation of the dosing interval until about 72 hours after the initiation of the dosing interval; and

a mean relative release rate from about 0.3 ug/hr to about 9 ug/hr from about 72 hours after the initiation of the dosing interval until the end of dosing interval.
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