Stabilized, sprayable emulsion containing active agent particles

Inventors

Dann, Thomas • Nelson, Renee • Wagner, Brian • Walter, Mary

Assignees

FORMULATED SOLUTIONS LLC • Mission Pharmacal Co

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Publication Number

US-9700510-B2

Patent

Publication Date

2017-07-11

Expiration Date


Abstract

A sprayable emulsion is provided. The emulsion can be used in the treatment of various skin conditions. The emulsion includes a hydrofluoro-based propellant, an emulsification system, an oil phase, a water phase, and active agent particles. Further, the emulsification system includes at least one nonionic emulsifier. The emulsion has a viscosity ranging from about 500 centipoise to about 10,000 centipoise and a hydrophilic to lipophilic balance (HLB) value of from about 2 to about 12. The present inventors have found that by selectively controlling the nature of the emulsification system and the viscosity of the emulsion, the active agent particles resist settling such that a substantially homogeneous distribution of the active agent particles is maintained and can be evenly sprayed onto a surface without running once applied.

Core Innovation

The invention describes a sprayable emulsion comprising a hydrofluoro-based propellant, an emulsification system, an oil phase, a water phase, and active agent particles. The emulsion has a viscosity ranging from about 500 centipoise to about 10,000 centipoise and a hydrophilic to lipophilic balance (HLB) value from about 2 to about 12. The emulsification system comprises at least one nonionic emulsifier and includes a nonionic lipophilic emulsifier and a nonionic hydrophilic emulsifier.

The nonionic lipophilic emulsifier comprises a non-crosslinked dimethicone polyol, a sorbitan fatty acid ester, and an octyldodecanol, and the nonionic hydrophilic emulsifier comprises a sorbitan fatty acid ester modified with a polyoxyethylene. The emulsion maintains a substantially homogeneous distribution of active agent particles and prevents settling/caking and running upon application.

The disclosed compositions and formation approach include using a particulate-tolerant spray delivery system with a non-mechanical breakup actuator, where a base emulsion composition is formed and then a hydrofluoro-based propellant is injected into a spray container. Example formulations include HFO propellants such as HFO-1234ze with zinc oxide particles, where the zinc oxide particles have moisture barrier coatings.

Claims Coverage

The document provides two independent claims: one directed to a sprayable emulsion composition and one directed to a method of forming the sprayable emulsion. Each independent claim centers on an emulsification system using nonionic lipophilic and nonionic hydrophilic emulsifiers, and on emulsion property constraints (viscosity and HLB), with the method claim further defining formation of a base emulsion, introduction into a spray container, and injection of a hydrofluoro-based propellant.

Sprayable emulsion with hydrofluoro-based propellant and dual nonionic emulsifiers

A sprayable emulsion comprising a hydrofluoro-based propellant, an emulsification system, an oil phase, a water phase, and active agent particles, wherein the emulsification system comprises a nonionic lipophilic emulsifier and a nonionic hydrophilic emulsifier.

Specified emulsion viscosity and HLB range

The emulsion has a viscosity ranging from about 500 centipoise to about 10,000 centipoise and a hydrophilic to lipophilic balance (HLB) value of from about 2 to about 12.

Nonionic lipophilic emulsifier chemistry for the emulsification system

The nonionic lipophilic emulsifier comprises a non-crosslinked dimethicone polyol, a sorbitan fatty acid ester, and an octyldodecanol.

Nonionic hydrophilic emulsifier chemistry for the emulsification system

The nonionic hydrophilic emulsifier comprises a sorbitan fatty acid ester modified with a polyoxyethylene.

Method of forming by base emulsion and propellant injection

A method of forming a sprayable emulsion comprising forming a base emulsion composition with active agent particles, an emulsification system, an oil phase, and a water phase; introducing the base emulsion composition into a spray container; and injecting a hydrofluoro-based propellant into the container.

Across the independent claims, the coverage focuses on a sprayable hydrofluoro-based emulsion with an emulsification system using defined nonionic lipophilic and nonionic hydrophilic emulsifiers, while maintaining specified viscosity and HLB ranges. The method independent claim adds the formation sequence of preparing a base emulsion and injecting a hydrofluoro-based propellant into a spray container.

Stated Advantages

Maintains a substantially homogeneous distribution of active (particulate) agents.

Prevents settling/caking and running upon application.

Documented Applications

Topical skin treatment using a sprayable emulsion with active agent particles.

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