# US 8,784,858 B2 · Degradable removable implant for the sustained release of an active compound

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- Number: US 8,784,858 B2
- Document ID: US8784858B2
- Status: Granted
- Kind: B2
- Application number: 13/515,380
- Filed: 2010-12-20
- Published: 2012-11-01
- Granted: 2014-07-22
- Earliest claimed: 2009-12-21
- Assignees: Janssen R&D Ireland
- Applicants: Deborah M. Schachter; Lieven Elvire Colette Baert; Guenter Kraus; Qiang Zhang; Iksoo Chun
- Inventors: Deborah M. Schachter; Lieven Elvire Colette Baert; Guenter Kraus; Qiang Zhang; Iksoo Chun
- Web page: https://patentgrep.com/patent/US8784858B2

## CPC

- A61L 31/148: {Materials at least partially resorbable by the body}
- A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)}
- A61K 9/0092: {Hollow drug-filled fibres, tubes of the core-shell type, coated fibres, coated rods, microtubules or nanotubes}
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)}
- A61K 31/34: having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61L 31/146: {Porous materials, e.g. foams or sponges}
- A61P 31/18: for HIV
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/5084: {Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs (tablets containing such a mixture A61K9/2077)}
- A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A degradable, removable, pharmaceutical implant for the sustained release of one or more drugs in a subject, wherein the pharmaceutical implant is composed of a tube comprising an outer wall made of a degradable polymer completely surrounding a cavity, wherein the outer wall has a plurality of openings and wherein the cavity contains one or more sets of micro-particles, which micro-particles contain an active agent or a combination of two or more active agents, and wherein the size of the microparticles is selected such that the majority of the microparticles cannot pass through the openings.

## Claims

### Claim 1

A degradable, removable, pharmaceutical subcutaneous implant for the sustained release of one or more drugs in a subject, wherein the pharmaceutical implant is composed of a tube comprising an outer wall made of a degradable polymer completely surrounding a cavity, wherein the outer wall has a plurality of openings and wherein the cavity contains one or more sets of micro-particles, which micro-particles are embedded in a hydrogel and contain at least one drug selected from an HIV inhibitor or an HCV inhibitor, and wherein the size of the microparticles is selected such that the majority of the microparticles cannot pass through the openings.

### Claim 2 (depends on 1)

The implant of claim 1, wherein the cavity contains two or more sets of micro-particles.

### Claim 3 (depends on 1)

The implant of claim 1, wherein the degradable polymer of the tube is selected from aliphatic polyesters, poly(amino acids), copoly(ether-esters), polyalkylene oxilates, polyamides, poly(iminocarbonates), poly(orthoesters), polyoxaesters, polyamidoesters, polyoxaesters containing amine groups, poly(anhydrides), polyphosphazenes, and blends thereof.

### Claim 4 (depends on 3)

The implant of claim 3, wherein the degradable polymer is selected from copolymers of lactide and glycolide.

### Claim 5 (depends on 3)

The implant of claim 3, wherein the degradable polymer is homopolymer of poly(dioxanone).

### Claim 6 (depends on 1)

The implant of claim 1, wherein the microparticles are fabricated from a biocompatible, biodegradable polymer selected from aliphatic polyesters, poly(amino acids), copoly(ether-esters), polyalkylene oxilates, polyamides, poly(iminocarbonates), poly(orthoesters), polyoxaesters, polyamidoesters, polyoxaesters containing amine groups, poly(anhydrides), polyphosphazenes, and blends thereof.

### Claim 7 (depends on 6)

The implant of claim 6, wherein the polymer used to fabricate the microparticles is a biocompatible, biodegradable polymer selected from homopolymers and copolymers of lactide, glycolide, epsilon-caprolactone, p-dioxanone (1,4-dioxin-2-one), and trimethylene carbonate (1,3-dioxan-2-one).

### Claim 8 (depends on 6)

The implant of claim 6, wherein the polymer used to fabricate the microparticles is a biocompatible, biodegradable polymer selected from copolymers of lactide and glycolide.

### Claim 9 (depends on 6)

The implant of claim 6, wherein the polymer used to fabricate the microparticles is a biocompatible, biodegradable polymer selected from a co-polymer of lactide and glycolide with a mole percent of lactide that ranges from 86% to 50%.

### Claim 10 (depends on 2)

The implant of claim 2, wherein one set of microparticles contains a NRTI and another set of microparticles contains a non-nucleoside reverse transcriptase inhibitor.

### Claim 11 (depends on 2)

The implant of claim 2, wherein one set of microparticles contains a non-nucleoside reverse transcriptase inhibitor and another set of microparticles contains a protease inhibitor.

### Claim 12 (depends on 1)

The implant of claim 1, containing rilpivirine.