# US 10,441,660 B2 · Pharmaceutical preparations containing highly volatile silicones

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- Number: US 10,441,660 B2
- Document ID: US10441660B2
- Status: Granted
- Kind: B2
- Application number: 15/688,728
- Filed: 2017-08-28
- Published: 2018-03-15
- Granted: 2019-10-15
- Earliest claimed: 2007-07-10
- Assignees: Egis Gyocyszergyar Nyilvanosan Mukodo Reszvenytarsasag
- Applicants: Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
- Inventors: Endre Mikulásik; Patrik Fazekas
- Web page: https://patentgrep.com/patent/US10441660B2

## CPC

- 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)
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/4164: 1,3-Diazoles
- A61K 31/4174: Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/5415: ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
- A61K 47/02: Inorganic compounds
- A61P 31/04: Antibacterial agents
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- 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 9/1611: {Inorganic compounds}
- 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

The subject of the present invention is a transdermal preparation containing pharmaceutically active ingredient, wherein the particles of the active ingredient are coated with highly volatile silicones or a mixture thereof, and these coated particles are dispersed in a gel or cream base. The volatile silicone component is hexamethyldisiloxane and/or octamethyltrisiloxane and/or decamethylpentacyclo-siloxane. A further subject of the present invention is a method for the preparation of such pharmaceutical compositions.

## Claims

### Claim 1

A process for the preparation of a pharmaceutical composition comprising a plurality of particles of an active pharmaceutical ingredient dispersed in a gel or cream base, the process comprising the steps of:
coating substantially all of the particles of active ingredient with a layer of highly volatile silicone or a mixture of highly volatile silicones;
mixing the coated particles of active ingredient with a gel or cream base;
wherein the layer of highly volatile silicone or mixture of highly volatile silicones substantially prevents contact between the active pharmaceutical agent and the gel or cream base at least until application; and
wherein the mass ratio of the layer of highly volatile silicone or mixture of highly volatile silicones to the active pharmaceutical agent is at least about 2:1.

### Claim 2 (depends on 1)

The process of claim 1, wherein the highly volatile silicone or mixture of highly volatile silicones is selected from the group consisting of hexamethyldisiloxane, octamethyltrisiloxane, decamethylpentacyclosiloxane and mixtures thereof.

### Claim 3 (depends on 1)

The process of claim 1, wherein the highly volatile silicone or mixture of highly volatile silicones comprises hexamethyldisiloxane.

### Claim 4 (depends on 1)

The process of claim 1, wherein the gel or cream base is a hydrated gel or cream base.

### Claim 5 (depends on 4)

The process of claim 4, wherein the hydrated gel or cream base is selected from the group consisting of hydrated carboxyvinyl polymer, hydrated hydroxypropyl-methyl cellulose and mixtures thereof.

### Claim 6 (depends on 1)

The process of claim 1, wherein the pharmaceutical composition comprises menthol.

### Claim 7 (depends on 6)

The process of claim 6, wherein the layer of highly volatile silicone or mixture of highly volatile silicones comprises menthol.

### Claim 8 (depends on 1)

The process of claim 1, wherein the mass ratio is no greater than about 6:1.

### Claim 9 (depends on 1)

The process of claim 1, wherein the mass ratio is no greater than about 5:1.

### Claim 10 (depends on 1)

The process of claim 1, wherein the mass ratio is at least about 6:1.