IP Library › Patent Application 16235021
Patent Application
App. No. 16/235,021

LONG ACTING OPIOID ANTAGONISTS

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Quick Facts
Patent No.
US None
App. No.
16/235,021
Abstract

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

Claims (20)

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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 23, 2019
From: HAYWARD, STEPHEN L; ZANA, LAWRENCE
To: CONSEGNA PHARMA, INC.
Reel/Frame 050148/0248 →