US2019201344A1PendingUtilityA1

Long acting opioid antagonists

61
Assignee: CONSEGNA PHARMA INCPriority: Dec 28, 2017Filed: Dec 28, 2018Published: Jul 4, 2019
Est. expiryDec 28, 2037(~11.4 yrs left)· nominal 20-yr term from priority
Inventors:Stephen L. HaywardLawrence J. Zana
A61K 31/485A61K 9/1647C07K 1/00
61
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Claims

Abstract

Sustained release formulations of opioid antagonists containing both free and encapsulated opioid antagonist are described herein.

Claims

exact text as granted — not AI-modified
1 . A composition comprising free opioid antagonist and microparticles of encapsulated opioid antagonist. 
     
     
         2 . The composition of  claim 1 , having a ratio of free opioid antagonist to encapsulated opioid antagonist of about 1:10 to about 1:50. 
     
     
         3 . The composition of  claim 1 , wherein the free opioid antagonist comprises about 0.4 milligrams (mg) to about 4 mg of opioid antagonist. 
     
     
         4 . The composition of  claim 1 , wherein the free opioid antagonist is selected from the groups consisting of naloxone (17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, naltrexone (17-(cyclopropylmethyl)-4,5α-epoxy-3, 14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, nalmefene (6-desoxy-6-methylenenaltrexone) in free base, salt, or hydrate form, and combinations thereof. 
     
     
         5 . The composition of  claim 1 , wherein the encapsulated opioid antagonist comprises about 10 mg to about 30 mg of encapsulated opioid antagonist. 
     
     
         6 . The composition of  claim 1 , wherein the encapsulated opioid antagonist is selected from the groups consisting of naloxone (17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, naltrexone (17-(cyclopropylmethyl)-4,5α-epoxy-3, 14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, nalmefene (6-desoxy-6-methylenenaltrexone) in free base, salt, or hydrate form, and combinations thereof. 
     
     
         7 . The composition of  claim 1 , wherein the microparticles have a mean particle diameter of about 40 μm to about 60 μm. 
     
     
         8 . The composition of  claim 1 , wherein the microparticles comprise a biodegradable polymer selected from the group consisting of PLGA, PLA, PGA, PBS, PHA, PCL, PHB, PHV, PHBV, PEG, PLEG, and copolymers thereof. 
     
     
         9 . The composition of  claim 8 , wherein the PLGA is capped. 
     
     
         10 . The composition of  claim 8 , wherein the PLGA comprises a ratio of PLA to PGA of 50:50 by weight to about 60:40 by weight. 
     
     
         11 . The composition of  claim 8 , wherein the biodegradable polymer comprises polymer units having molecular weights of about 5 kiloDalton (kDa) to about 150 kDa. 
     
     
         12 . The composition of  claim 1 , wherein opioid antagonist loading is about 0.5 wt. % to about 50 wt. %. 
     
     
         13 . A method for treating or preventing opioid overdose comprising administering to a subject in need of treatment a composition comprising free opioid antagonist and microparticles of encapsulated opioid antagonist. 
     
     
         14 . The method of  claim 13 , having a ratio of free opioid antagonist to encapsulated opioid antagonist of about 1:10 to about 1:50. 
     
     
         15 . The method of  claim 13 , wherein the free opioid antagonist comprises about 0.4 milligrams (mg) to about 4 mg of opioid antagonist. 
     
     
         16 . The method of  claim 13 , wherein the free opioid antagonist is selected from the groups consisting of naloxone (17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, naltrexone (17-(cyclopropylmethyl)-4,5α-epoxy-3, 14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, nalmefene (6-desoxy-6-methylenenaltrexone) in free base, salt, or hydrate form, and combinations thereof. 
     
     
         17 . The method of  claim 13 , wherein the encapsulated opioid antagonist comprises about 10 mg to about 30 mg of encapsulated opioid antagonist. 
     
     
         18 . The method of  claim 13 , wherein the encapsulated opioid antagonist is selected from the groups consisting of naloxone (17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, naltrexone (17-(cyclopropylmethyl)-4,5α-epoxy-3, 14-dihydroxymorphinan-6-one) in free base, salt, or hydrate form, nalmefene (6-desoxy-6-methylenenaltrexone) in free base, salt, or hydrate form, and combinations thereof. 
     
     
         19 . The method of  claim 13 , wherein administration results in a plasma concentration in the subject of greater than about 2 ng/ml for up to about 7 days. 
     
     
         20 . The method of  claim 13 , wherein administration is selected from the group consisting of depo injection, intramuscular injection, subcutaneous injection, oral, sublingual, and intranasal administration.

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