IP Library › Granted Patent US 10,596,103
Granted Patent B2
US 10,596,103 · App. 15/036,839 · Granted Mar 24, 2020

Drug delivery system for delivery of anti-virals

Inventors: Dennis Aarts (Etten-Leur, NL); Wouter de Graaff (Sprang-Capelle, NL); Johannes Antonius Hendrikus van Laarhoven (Vught, NL)
Assignee: Merek Sharp & Dohme B.V.
A61K9/0036A61K31/506A61K31/5025A61K31/567A61K31/57A61K45/06A61K47/32
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Quick Facts
Patent No.
US 10,596,103
App. No.
15/036,839
Granted
Mar 24, 2020
Kind
B2
Abstract

Described herein is a vaginal ring drug delivery system comprising (i) a core comprising a first thermoplastic polymer and a first therapeutic agent, wherein the first therapeutic agent is dissolved in the first thermoplastic polymer, and (ii) a skin surrounding the core comprising a second thermoplastic polymer and a second therapeutic agent, wherein the second therapeutic agent is in solid form.

Claims (7)

1. A vaginal ring drug delivery system comprising (i) a core comprising a first ethylene-vinylacetate copolymer and vicriviroc, wherein the vicriviroc is dissolved in the first ethylene-vinylacetate copolymer, and (ii) a skin surrounding the core comprising a second ethylene-vinylacetate copolymer wherein the second ethylene-vinylacetate copolymer is the only polymer in the skin, and wherein the first ethylene-vinylacetate copolymer has a higher vinylacetate content than the second ethylene-vinylacetate copolymer, and (S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino [1′,2′:1,5]pyrrolo [2,3-d]pyridazine-4-carboxamide, wherein the (S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino [1′,2′:1,5]pyrrolo[2,3-d]pyridazine-4-carboxamide is loaded in the skin in solid form, such that a depletion layer is preformed, and upon release, the (S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino[1′,2′:1,5]pyrrolo [2,3-d]pyridazine-4-carboxamide loaded in the skin displays a near zero order release profile.

2. The drug delivery system of claim 1 , wherein the first ethylene-vinylacetate copolymer has a vinylacetate content of 28% vinylacetate.

3. The drug delivery system of claim 1 , wherein the second ethylene-vinylacetate copolymer has a vinylacetate content of 15% vinylacetate.

4. A vaginal ring drug delivery system comprising (i) a core comprising an ethylene-vinylacetate copolymer having a vinylacetate content of equal to or greater than 28% and vicriviroc, wherein the vicriviroc is in dissolved form, and (ii) a skin surrounding the core, wherein the skin comprises an ethylene-vinylacetate copolymer having a vinylacetate content of less than 28% wherein the ethylene-vinylacetate copolymer having a vinylacetate content of less than 28% is the only polymer in the skin, and (S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino[1′,2′:1,5]pyrrolo [2,3-d]pyridazine-4-carboxamide, wherein the (S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino[1′,2′:1,5]pyrrolo [2,3-d]pyridazine-4-carboxamide is loaded in the skin in solid form, such that a depletion layer is preformed, and upon release the (S)-2-(3-chloro-4-fluorobenzyl)-8-ethyl-10-hydroxy-N,6-dimethyl-1,9-dioxo-1,2,6,7,8,9-hexahydropyrazino[1′,2′:1,5]pyrrolo [2,3-d]pyridazine-4-carboxamide loaded in the skin displays a near zero order release profile.

5. The drug delivery system of claim 4 , wherein the ethylene-vinylacetate copolymer in the core has a vinylacetate content between 28-33% vinylacetate.

6. The drug delivery system of claim 4 , wherein the ethylene-vinylacetate copolymer in the core has a vinylacetate content of 28% vinylacetate.

7. The drug delivery system of claim 4 , wherein the ethylene-vinylacetate copolymer in the skin has a vinylacetate content of 15% vinylacetate.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 16, 2016
From: AARTS, DENNIS; DE GRAAFF, WOUTER; HENDRIKUS VAN LAARHOVEN, JOHANNES ANTONIUS
To: MERCK SHARP & DOHME B.V.
Reel/Frame 038601/0175 →
Priority Claims (1)
EP 13196739.0 · Dec 11, 2013 · regional
Continuity (2)
Provisional Application 61914438 · Dec 11, 2013
Related Publication 20160296467A1 · Oct 13, 2016
Cited By (2)
US 12,472,148 US 12,502,360