Granted Patent B2

US 8,889,736 · App. 13/232,905 · Granted Nov 18, 2014

Abstract

Claims (32)

1. A substantially nonaqueous therapeutic formulation for topical administration comprising a uniform liquid binary eutectic mixture of:

(a) a capsaicinoid having the structure of formula (I)

wherein R 1 is methoxy, R 2 is hydroxyl, X is

and R is —(CH 2 ) 4 —CH═CH—CH(CH 3 ) 2 , wherein the capsaicinoid represents about 40 wt. % to about 70 wt. % of the formulation; and

(b) a second active agent effective to decrease at least one side effect associated with capsaicin monotherapy, said second agent existing as a solid at 25° C., and wherein the second active agent is a local anesthetic selected from the group consisting of amylocaine, articaine, benzocaine, bupivacaine, butacaine, 2-chloroprocaine, cinchocaine, dexivacaine, diamocaine, dibucaine, etidocaine, ketocaine, lidocaine, mepivacaine, oxybuprocaine, parethoxycaine, prilocaine, procaine, propanocaine, proparacaine, propoxycaine, pyrrocaine, risocaine, rodocaine, ropivacaine, tetracaine, and combinations thereof; and

wherein the formulation contains less than 5 wt. % water.

2. The formulation of claim 1 , wherein the local anesthetic agent is lidocaine.

3. The formulation of claim 1 , wherein the local anesthetic agent is tetracaine.

4. A substantially nonaqueous therapeutic formulation for topical administration comprising a uniform liquid ternary eutectic mixture of:

(a) a capsaicinoid having the structure of formula (I)

wherein R 1 is methoxy, R 2 is hydroxyl, X is

and R is —(CH 2 ) 4 —CH═CH—CH(CH 3 ) 2 , wherein the capsaicinoid represents about 50 wt%. of the formulation; and

(b) a second active agent effective to decrease at least one side effect associated with capsaicin monotherapy, wherein the second active agent is a local anesthetic selected from the group consisting of amylocaine, articaine, benzocaine, bupivacaine, butacaine, 2-chloroprocaine, cinchocaine, dexivacaine, diamocaine, dibucaine, etidocaine, ketocaine, lidocaine, mepivacaine, oxybuprocaine, parethoxycaine, prilocaine, procaine, propanocaine, proparacaine, propoxycaine, pyrrocaine, risocaine, rodocaine, ropivacaine, tetracaine, and combinations thereof; and

(c) a third active agent effective to decrease at least one side effect associated with capsaicin monotherapy,

said second and third active agents both existing as a solid at 25° C.; and

wherein the formulation contains less than 5 wt. % water.

5. The formulation of claim 4 , wherein the local anesthetic agent is lidocaine.

6. The formulation of claim 4 , wherein the local anesthetic agent is tetracaine.

7. The formulation of claim 4 , wherein the third active agent is an anti-pruritic agent.

8. The formulation of claim 7 , wherein the anti-pruritic agent is selected from menthol, camphor, phenol, and combinations thereof.

9. The formulation of claim 4 , wherein the second and third active agents are present in a weight ratio of about 1:1.

10. A method for treating a patient suffering from pain, comprising topically administering to the patient a therapeutically effective amount of the formulation of claim 1 or claim 4 .

11. The method of claim 10 , wherein the pain is caused by inflammation of joints, tends, nerves, or muscle.

12. The method of claim 11 , wherein the pain is caused by arthritis.

13. The method of claim 10 , wherein the pain is back pain.

14. The method of claim 10 , wherein the pain is headache pain.

15. The method of claim 10 , wherein the pain is caused by cancer.

16. The method of claim 10 , wherein the pain is neuropathic pain.

17. The method of claim 16 , wherein the neuropathic pain is post-herpetic neuralgia.

18. The method of claim 16 , wherein the neuropathic pain is the result of HIV associated neuropathy.

19. The method of claim 16 , wherein the neuropathic pain is associated with diabetic neuropathy.

20. The method of claim 16 , wherein the neuropathic pain is trigeminal neuralgia.

Assignments (8)