Pain Therapeutics, Inc.

Cassava Sciences, Inc.

Zamloot, Michael

Remi Barbier

Michael S Zamloot

Stephen William Watt

Vijay Srirambhatla

Nadav Friedmann

Nadav Friedman

Sephen Watt

Vijay Sriranbhatla

Stephen Watt

This invention relates to cocrystals of naloxone and of naltrexone and their use as opioid antagonists. The cocrystals of the invention include naloxone isonicotinamide cocrystal, naloxone hydrochloride piperazine cocrystal, naltrexone menthol cocrystal, naltrexone thymine cocrystal, naltrexone 2,5-dihydroxybenzoic acid cocrystal, naltrexone salicylic acid cocrystal, naltrexone hydrochloride piperazine cocrystal and naltrexone hydrochloride sulfathiazole cocrystal. A drug-in&#xac; adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a cocrystal of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof. Also disclosed is an improved transdermal patch for administering fentanyl or an analog thereof, or for administering a mu opioid agonist, the improvement wherein the transdermal patch contains a cocrystal of the invention in an abuse limiting amount. The improved transdermal patch may be a drug-in-adhesive transdermal patch or a reservoir transdermal patch.

Cocrystals of naloxone and naltrexone

This invention relates to crystalline salts of naloxone and of naltrexone and their use as opioid antagonists. The crystalline salts of the invention include naloxone saccharinate, naltrexone succinate and a methanol solvate of naltrexone succinate. A drug-in-adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a crystalline salts of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof.

Crystalline salts of naloxone and naltrexone

A 4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal and its use as an opioid antagonist are disclosed. The invention also relates to a drug-in-adhesive transdermal patch containing the analgesic fentanyl, a mu opioid agonist, or an analog thereof and a 4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal, as an opioid antagonist. A transdermal patch of the invention is tamper-resistant and an abuse deterrent which protects against drug misuse or abuse. The invention also provides a method of treating pain, such as acute, chronic, or intermittent pain, by applying a drug-in-adhesive transdermal patch according to the invention to the skin of a patient in need thereof. Also disclosed is an improved transdermal patch for administering fentanyl or an analog thereof, or for administering a mu opioid agonist, the improvement wherein the transdermal patch contains a 4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal in an abuse limiting amount. The improved transdermal patch may be a drug-in-adhesive transdermal patch or a reservoir transdermal patch.

4:3 naltrexone: 5-methyl-2-furaldehyde cocrystal

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Austin, TX, United States of America

Remi Barbier