# US 8,771,711 B2 · Sprayable gel-type skin/mucosa-adhesive preparation and administration system using the preparation

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- Number: US 8,771,711 B2
- Document ID: US8771711B2
- Status: Granted
- Kind: B2
- Application number: 12/226,287
- Filed: 2007-04-20
- Published: 2009-11-05
- Granted: 2014-07-08
- Earliest claimed: 2006-04-21
- Assignees: Toko Yakuhin Kogyo Kabushiki Kaisha
- Applicants: Taizou Kamishita
- Inventors: Taizou Kamishita
- Web page: https://patentgrep.com/patent/US8771711B2

## CPC

- A61K 9/0043: {Nose}
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/4174: Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
- A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61M 11/007: {Syringe-type or piston-type sprayers or atomisers}
- A61M 15/08: Inhaling devices inserted into the nose
- A61K 9/0031: {Rectum, anus}
- A61K 9/0046: {Ear}
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- 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 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61M 2005/31516: {reducing dead-space in the syringe barrel after delivery}
- B05B 11/028: {Pistons separating the content remaining in the container from the atmospheric air to compensate underpressure inside the container}
- B05B 11/1023: {having an outlet valve opened by deformation or displacement of the piston relative to its actuating stem}
- B05B 11/1026: {the piston being deformable and its deformation allowing opening of the outlet}
- 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)
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}
- B05B: SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES (spray-mixers with nozzles B01F25/72; processes for applying liquids or other fluent materials to surfaces by spraying B05D)

## Abstract

The present invention provides a sprayable gel-type skin/mucosa-adhesive preparation comprising a gel formulation which contains an active pharmaceutical ingredient in a gel base material comprising a skin/mucosa-adhesive agent and an administration system comprising the preparation.

## Claims

### Claim 1

A sprayable gel-type skin/mucosa-adhesive preparation that takes a particle form after spraying, comprising a gel formulation, which contains an active pharmaceutical ingredient in a gel base material comprising a skin/mucosa-adhesive agent,
wherein the skin/mucosa-adhesive agent comprises a carboxy vinyl polymer,
the skin/mucosa-adhesive agent is treated with an outside shearing force that adjusts viscosity of the skin/mucosa-adhesive agent to be in the range of 50 mPa·s to 5000 mPa·s, and
a particle of the sprayed formulation has a viscosity retention rate of about 100%.

### Claim 2 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the mucosa to which the preparation is applied is a mucosa of a nasal cavity, an eye, an ear, an oral cavity, a rectum, a vagina, or an urethra; or the skin to which the preparation is applied is skin of a hand, a finger, a leg, a body, a groin, a scalp, surroundings of an anus, or surroundings of a genitalium.

### Claim 3 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the mucosa to which the preparation is applied is a mucosa of a nasal cavity.

### Claim 4 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the skin/mucosa-adhesive agent contains the carboxy vinyl polymer in an amount of 0.1% (w/w) to 2.0% (w/w).

### Claim 5 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the skin/mucosa-adhesive agent contains the carboxy vinyl polymer and gellan gum in a total amount of 0.2% (w/w) to 4.0% (w/w).

### Claim 6 (depends on 4)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 4,
wherein the skin/mucosa-adhesive agent further comprises a viscosity modulating agent that adjusts the viscosity of the skin/mucosa-adhesive agent

### Claim 7 (depends on 6)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 6, wherein the viscosity modulating agent is selected from a group consisting of sodium chloride, potassium chloride and calcium chloride.

### Claim 8 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, further comprising a thickening agent for the carboxy vinyl polymer, which is selected from the group consisting of a neutral amino acid or basic water-soluble amino acid and is contained in a ratio of 1: 0.5 to 1: 3 relative to the carboxy vinyl polymer by weight.

### Claim 9 (depends on 8)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 8, wherein the thickening agent is at least one material selected from the group consisting of arginine, lysine, and ornithine.

### Claim 10 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the gel formulation contains an active pharmaceutical ingredient in an amount of 0.001-10% (w/w) in the gel formulation.

### Claim 11 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the active pharmaceutical ingredient is in a dissolved state.

### Claim 12 (depends on 1)

The sprayable gel-type skin/mucosa-adhesive preparation set forth in claim 1, wherein the skin/mucosa-adhesive agent further comprises gellan gum.