Formulations Of Indanylamines And The Use Thereof As Local Anesthetics And As Medication For Chronic Pain
AssigneeBridge Pharma, Inc.
InventorsA.K. Gunnar Aberg, Keith Johnson
Life of this patent
Estimating the term…
Abstract
Internal-dermal formulations of RS—, S—, or R-2-[2-(N-phenyl-N-2-indanyl)aminoethyl]piperidine causing intradermal accumulation of said piperidine and intended for the treatment of neuropathic pain are provided, as well as a method of inducing the relief of pain using the compounds.
Claims13
An intradermal formulation for inducing relief of neuropathic pain, comprising a therapeutically effective amount of the compound 2-[2-(N-phenyl-N-2-indanyl)aminoethyl]piperidine, or an optically active isomer thereof or pharmaceutically acceptable salt thereof, dissolved in one or more solvents, at least one of which is volatile, in which said compound, isomer or salt is soluble, together with an anti-solvent in an amount sufficient to reduce the solubility of said compound, isomer or salt in said one or more solvents such that upon application of said formulation to the skin of a patient, said volatile solvent evaporates to form a saturated solution of said compound, isomer or salt, facilitating the penetration of said compound, isomer or salt into the skin and accumulation of said compound, isomer or salt in the epidermis and dermis of the skin in an amount effective for inducing relief of neuropathic pain.
A method of inducing relief of neuropathic pain in a patient in need thereof, comprising applying to the skin of said patient a therapeutically effective amount of the compound 2-[2-(N-phenyl-N-2-indanyl)aminoethyl]piperidine, or an optically active isomer thereof or a pharmaceutically acceptable salt thereof, dissolved in one or more solvents in which said compound, isomer or salt is soluble, together with an anti-solvent in an amount sufficient to reduce the solubility of said compound, isomer or salt in said one or more solvents, wherein upon application of said formulation to the skin of said patient, said solvent evaporates to form a saturated solution of said compound, isomer or salt, causing said compound, isomer or salt to penetrate the stratum corneum and to accumulate in the epidermis and dermis of the skin in an amount effective for inducing relief of neuropathic pain.
A method of down-regulating the up-regulated sodium channels in thin dermal afferent nerve fibers and in dermal nerve endings of the skin of a patient suffering from neuropathic pain, comprising applying to the skin of said patient a therapeutically effective amount of the compound, or an optically active isomer thereof or pharmaceutically acceptable salt thereof, dissolved in one or more solvents in which said compound, isomer or salt is soluble, together with an anti-solvent in an amount sufficient to reduce the solubility of said compound, isomer or salt in said one or more solvents at least one of which is a volatile solvent, wherein upon application of said formulation to the skin of said patient, said volatile solvent evaporates to form a saturated solution of said compound, isomer or salt, causing said compound, isomer or salt to accumulate in the epidermis and dermis of the skin.
Dependencies are inferred from the claim text.