Laureth-4 containing topical formulations
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Publication Number
US-12083122-B2
Publication Date
2024-09-10
Expiration Date
Abstract
The present invention is a method and composition comprising laureth-4 in topical formulations, wherein the laureth-4 increases the penetration of active ingredients across the skin. In a particularly preferred embodiment, the active ingredient is SHR0302.
Core Innovation
The invention relates to topical pharmaceutical compositions containing the JAK1 inhibitor SHR0302 (ARQ-250) and laureth-4 as a skin-penetration enhancer. The compositions include SHR0302 combined with water and at least one solvent with laureth-4, and the topical pharmaceutical composition does not contain an additional active ingredient.
A key aspect is that laureth-4 improves skin penetration of SHR0302. The document discusses in vitro permeation testing (IVPT) using excised human cadaver skin dermatomed to a target thickness of 500 microns, including identification and discussion of finite dose versus infinite dose IVPT artifacts.
Laureth-4 is reported to increase SHR0302 permeation relative to the same topical pharmaceutical formulation without laureth-4. Example prototype formulations and tabulated or cited permeation data are included, including references to tables and figures comparing the presence versus absence of laureth-4.
Claims Coverage
The partial content includes two independent claims. The claims center on topical SHR0302 compositions with laureth-4 as a skin-penetration enhancer, without an additional active ingredient, and require IVPT-based skin-penetration improvement on excised human cadaver skin dermatomed to 500 microns.
Topical pharmaceutical composition without additional active ingredient
The composition does not contain an additional active ingredient.
Combining SHR0302, water, solvent, and laureth-4
Combining SHR0302, water, and at least one solvent with laureth-4.
Five-fold to thirty-fold skin penetration improvement by IVPT
Improving the skin penetration of SHR0302 by 5-fold to 30-fold relative to the same topical pharmaceutical formulation without laureth-4 as measured by in vitro permeation testing in excised human cadaver skin dermatomed to a target thickness of 500 microns.
Improving skin penetration by 10-fold to thirty-fold by IVPT
Improving the skin penetration of SHR0302 by 10-fold to 30-fold relative to the same topical pharmaceutical formulation without laureth-4 as measured by in vitro permeation testing in excised human cadaver skin dermatomed to a target thickness of 500 microns.
SHR0302 concentration range
SHR0302 is present in an amount of about 0.1 to about 1.0% w/w.
Laureth-4 concentration range
Laureth-4 is present in an amount of about 0.5 to about 5% w/w.
Solvent specified as dimethyl sulfoxide
The solvent is dimethyl sulfoxide.
Topical dosage/formulation type selected from listed forms
The topical pharmaceutical composition is selected from an oil-in-water emulsion, a water-in-oil emulsion, a microemulsion, a nanoemulsion, a foam, a spray, a hydrophilic ointment, or a hydrophobic ointment.
The claims are directed to topical SHR0302 compositions using laureth-4 as a skin-penetration enhancer without an additional active ingredient, with IVPT-based skin-penetration improvement on excised human cadaver skin dermatomed to 500 microns. Dependent refinements specify concentration ranges, dimethyl sulfoxide as solvent, and listed formulation types.
Stated Advantages
Increased skin penetration of SHR0302 using laureth-4, reported as 5-fold to 30-fold, and in a refinement 10-fold to 30-fold, relative to the same formulation without laureth-4 as measured by IVPT.
Documented Applications
Treatment of inflammatory skin diseases, including atopic dermatitis, rosacea, psoriasis, seborrheic dermatitis, vitiligo, eczema, and alopecia areata.
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