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Injectable capsaicin

a technology of capsaicin and injection, which is applied in the direction of biocide, plant/algae/fungi/lichens, biocide composition, etc., can solve the problems of poor patient compliance, high dropout rate during clinical trials, and limited effectiveness of topically administered capsaicin in general arthritis, so as to minimize the potential adverse effects of c-fiber, reduce or eliminate pain, and localize the effect of destruction or incapacitation

Inactive Publication Date: 2005-01-27
ALGORX PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0013] It is another object of the present invention to provide compositions and methods for relieving pain at an intra-articular site or at a body space by administering an injectable or implantable single dose of capsaicin or capsaicin analogue to the intra-articular site or body space.
[0025] The invention is further directed in part to a method of treating acute traumatic pain associated with an injury, comprising injecting a capsaicinoid in a physiologically compatible vehicle through the skin of a patient in proximity to an injury, said dose of capsaicinoid being sufficient to attenuate the dull, aching pain associated with C-fibers in proximity to the injury and such that the patient continues to have sensation in proximity to the injury and without affecting sharp protective pain associated with A-delta fibers in proximity to the site, the dose of capsaicinoid being therapeutically equivalent to a dose of capsaicin in an amount from about 300 to about 1500 μg and being effective to attenuate dull, aching pain in proximity to the injury for at least about 48 hours.
[0027] The single injectable or implantable dose of a capsaicinoid administered at a discrete painful site in accordance with the present invention is preferably in an amount effective to a) produce a selective, highly-localized destruction or incapacitation of C-fibers and / or A-delta fibers in a discrete, localized area responsible for the initiation of pain for the purpose of reducing or eliminating pain arising from a discrete locus, and b) minimize potential adverse consequences of C-fiber and / or A-delta activation and or damage outside of the locus of pain.

Problems solved by technology

However the efficacy of topically administered capsaicin in arthritis in general has proven to be limited.
However, since the application of capsaicin itself frequently causes burning pain and hyperalgesia apart from the neuropathic pain being treated, patient compliance has been poor and the drop out rates during clinical trials have exceeded fifty percent.

Method used

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  • Injectable capsaicin
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Examples

Experimental program
Comparison scheme
Effect test

example i

Osteoarthritis of the Knee Safety Study

[0141] The following clinical study was carried out in order to evaluate the safety, tolerability, systemic pharmacokinetics, and efficacy of purified capsaicin administered by intra-articular infiltration together with a local anesthetic administered by intra-articular infiltration in subjects with osteoarthritis of the knee.

[0142] The primary objective of the study was to evaluate the safety and tolerability of intra-articular capsaicin, when co-administered with intra-articular local anesthetic, compared to placebo, in subjects with end-stage osteoarthritis of the knee, already scheduled to receive knee replacements.

[0143] Purified capsaicin was supplied in vials containing 5 mL of purified capsaicin at a concentrations of 500 μg / mL. Study drug was stored at a temperature between 15° C. and 25° C. Within four hours prior to injection, vehicle was used to dilute the drug to final concentrations of purified capsaicin, as follows:

TABLE 1Do...

example ii

Osteoarthritis of the Knee Efficacy Study

[0160] The following clinical study evaluates the efficacy of purified capsaicin administered by intra-articular infiltration together with a local anesthetic injected by intra-articular infiltration in subjects with osteoarthritis of the knee.

[0161] The primary objective of the study is to evaluate the efficacy of intra-articular capsaicin, when co-administered with intra-articular local anesthetic, compared to placebo, in subjects with end-stage osteoarthritis of the knee, already scheduled to receive knee replacements (21 and 42 days after injection of study medication).

[0162] Purified capsaicin is supplied in vials containing 5 mL of purified capsaicin at a concentrations of 500 μg / mL. Study drug was stored at a temperature between 15° C. and 25° C. Within four hours prior to injection, vehicle is used to dilute the drug to final concentrations of purified capsaicin, as follows:

TABLE 2Dose LevelConcentrationTotal Volume of Dose1000 μ...

example iii

Bunionectomy Efficacy Study

[0169] The following study was carried out in order to evaluate the safety, tolerability, systemic pharmacokinetics, and efficacy of intra-operative (infiltration) capsaicin when co-administered with a local anesthetic in patients scheduled to undergo transpositional osteotomy (bunionectomy).

[0170] The primary objective of the study was to evaluate the safety and tolerability of capsaicin, when co-administered by intra-articular infiltration with a local anesthetic, compared to placebo, in subjects with hallux valgus deformity, already scheduled to undergo transpositional osteotomy (bunionectomy). The secondary objective of the study was to evaluate the safety, tolerability and systemic pharmacokinetics of purified capsaicin following intra-operative administration. The primary efficacy endpoint was the proportion of subjects in each treatment group requiring opioid analgesia in the first 24 hours post-operatively. The proportions were compared amongst t...

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Abstract

The present invention provides compositions and methods for relieving pain at a site in a human or animal in need thereof by administering at a discrete site in a human or animal in need thereof a dose of capsaicin in an amount effective to denervate a discrete site without eliciting an effect outside the discrete location, the dose of capsaicin ranging from 1 μg to 3000 μg.

Description

[0001] This application claims the benefit of U.S. Provisional Patent Application No. 60 / 434,453, filed Dec. 18, 2002, U.S. Provisional Patent Application No. 60 / 434,530, filed Dec. 18, 2002, U.S. Provisional Patent Application No. 60 / 434,500, filed Dec. 18, 2002, U.S. Provisional Patent Application No. 60 / 434,828, filed Dec. 18, 2002, U.S. Provisional Patent Application No. 60 / 434,452, filed Dec. 18,.2002, U.S. Provisional Patent Application No. 60 / 434,501, filed Dec. 18, 2002, and U.S. Provisional Patent Application No. 60 / 461,164, filed Apr. 8, 2003, the disclosures of which is hereby incorporated by reference in their entirety.FIELD OF THE INVENTION [0002] This application is directed to compositions and methods for relieving pain at a specific site, for example, associated with inflammation of joints, tendons, nerves, muscle, and other soft tissues, nerve injury and neuropathies, and pain from tumors in soft tissues or bone. BACKGROUND OF THE INVENTION [0003] Capsaicin, a punge...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/05A61K31/16A61K31/165A61K31/5415A61K31/551A61K36/81A61K45/06A61K47/10C07C231/02C07C233/20
CPCA61K9/0019A61K31/05A61K31/16A61K31/165A61K31/5415A61K31/551A61K36/81A61K45/06A61K47/10C07C231/02A61K2300/00C07C233/20A61P19/02A61P23/00A61P23/02A61P25/00A61P25/02A61P25/04A61P29/00A61P29/02A61P43/00
Inventor BURCH, RONALD M.CARTER, RICHARD B.LAZAR, JEFF
Owner ALGORX PHARMA INC
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