# US 9,872,829 B2 · Core sheath drug delivery devices

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- Number: US 9,872,829 B2
- Document ID: US9872829B2
- Status: Granted
- Kind: B2
- Application number: 14/855,187
- Filed: 2015-09-15
- Published: 2016-01-07
- Granted: 2018-01-23
- Earliest claimed: 2012-02-14
- Assignees: Chemo Research, S.L.
- Applicants: Chemo Research, S.L.
- Inventors: Andrew Loxley; Mark Mitchnick; Gonzalo Hernández Herrero; Celestino Ronchi
- Web page: https://patentgrep.com/patent/US9872829B2

## CPC

- A61K 9/0036: {Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms}
- A61F 6/142: {Wirelike structures, e.g. loops, rings, spirals}
- A61K 9/0002: {Galenical forms characterised by the drug release technique; Application systems commanded by energy}
- A61K 9/0092: {Hollow drug-filled fibres, tubes of the core-shell type, coated fibres, coated rods, microtubules or nanotubes}
- A61K 31/567: substituted in position 17 alpha, e.g. mestranol, norethandrolone
- A61K 31/569: substituted in position 17 alpha, e.g. ethisterone
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/18: Feminine contraceptives
- 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)
- A61F: FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS (dental prosthetics A61C)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

It relates to a device comprising (a) a core comprising polyurethane; (b) a sheath comprising ethylene vinyl acetate copolymer, said sheath substantially or completely surrounding said core; and (c) one or more active pharmaceutical ingredients dissolved or dispersed in said core and/or said sheath; and to a process for its preparation.

## Claims

### Claim 1

A device comprising:
(a) a core, said core comprising at least 90% of polyurethane,
wherein the polyurethane is selected from aliphatic polyether-based thermoplastic polyurethanes, aliphatic hydrophilic polyether-based thermoplastic polyurethanes, aromatic polyether-based thermoplastic polyurethanes, aliphatic polycarbonate-based thermoplastic polyurethanes, aromatic polycarbonate-based thermoplastic polyurethanes, aromatic polyether based polyurethane elastomers, thermoplastic polyether poly(urethanes), thermoplastic silicone polyether polyurethanes, thermoplastic silicone polycarbonate polyurethanes and hydrophilic thermoplastic polyurethane elastomers;
(b) a sheath, said sheath substantially or completely surrounding said core, said sheath comprising from 50 to 100% of ethylene vinyl acetate copolymer,
wherein the ethylene vinyl acetate copolymer has a vinyl acetate content from 1 to 50% w/w, and,
wherein said sheath has a thickness from 5 to 500 μm; and
(c) one or more active pharmaceutical ingredients dissolved or dispersed in said core and/or said sheath;
wherein the one or more active pharmaceutical ingredients are eluted at or near zero order.

### Claim 2 (depends on 1)

The device according to claim 1, wherein the active pharmaceutical ingredients are selected from the group consisting of antibacterial agents, antiviral agents, antifungal agents, chemotherapeutics, hormones, prohormones, anesthetics, analgesics, antibodies, antigens, muscle stimulants, psychoactive compounds, anti-cholinergic agents, and combinations thereof.

### Claim 3 (depends on 1)

The device according to claim 1, wherein the active pharmaceutical ingredients are present in the core.

### Claim 4 (depends on 3)

The device according to claim 3, wherein the active pharmaceutical ingredients are present in the core in a concentration below its saturation concentration.

### Claim 5 (depends on 1)

The device according to claim 1, which comprises an estrogen.

### Claim 6 (depends on 5)

The device according to claim 5, wherein the estrogen is ethinyl estradiol.

### Claim 7 (depends on 6)

The device according to claim 6, wherein ethinyl estradiol is present in the core in a concentration comprised from 0.10 to 0.30 wt % based on the total core weight.

### Claim 8 (depends on 1)

The device according to claim 1, which comprises a progestin.

### Claim 9 (depends on 8)

The device according to claim 8, wherein the progestin is etonogestrel.

### Claim 10 (depends on 9)

The device according to claim 9, wherein etonogestrel is present in the core in a concentration below its saturation concentration at 25° C. comprised from 0.20 to 1.00 wt % based on the total core weight.

### Claim 11 (depends on 8)

The device according to claim 8, wherein the progestin is levonorgestrel.

### Claim 12 (depends on 11)

The device according to claim 11, wherein levonorgestrel is present in the core in a concentration below its saturation concentration at 25° C. comprised from 0.20 to 1.00 wt % based on the total core weight.

### Claim 13 (depends on 1)

The device according to claim 1, which comprises a progestin and an estrogen.

### Claim 14 (depends on 13)

The device according to claim 13, wherein the progestin is etonogestrel and the estrogen is ethinyl estradiol.

### Claim 15 (depends on 14)

The device according to claim 14, wherein etonogestrel is present in the core in a concentration below its saturation concentration at 25° C. comprised from 0.20 to 1.00 wt % based on the total core weight; and ethinyl estradiol is present in the core in a concentration comprised from 0.10 to 0.30 wt % based on the total core weight.

### Claim 16 (depends on 1)

The device according to claim 1, wherein the ethylene vinyl acetate copolymer has a vinyl acetate content comprised from 10 to 40% w/w.

### Claim 17 (depends on 12)

The device according to claim 12, wherein the ethylene vinyl acetate copolymer has a vinyl acetate content comprised from 10 to 40% w/w.

### Claim 18 (depends on 15)

The device according to claim 15, wherein the ethylene vinyl acetate copolymer has a vinyl acetate content comprised from 10 to 40% w/w.

### Claim 19 (depends on 1)

The device according to claim 1, wherein the sheath has a thickness comprised from 50 to 200 μm.

### Claim 20 (depends on 12)

The device according to claim 12, wherein the sheath has a thickness comprised from 50 to 200 μm.

### Claim 21 (depends on 15)

The device according to claim 15, wherein the sheath has a thickness comprised from 50 to 200 μm.

### Claim 22 (depends on 1)

The device according to claim 1, wherein the device is a vaginal ring.

### Claim 23 (depends on 1)

The device according to claim 1, where the pharmaceutical ingredients are encapsulated prior to incorporation into the device.

### Claim 24 (depends on 1)

The device according to claim 1, where there is one or more active pharmaceutical ingredients contained in the sheath.
