Laureth-4 containing topical formulations
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.
1. A method for preparing a topical pharmaceutical composition comprising:
combining SHR0302, water, and at least one solvent with laureth-4, wherein the topical pharmaceutical composition does not contain an additional active ingredient.
2. The method of claim 1 , wherein the amount of laureth-4 is sufficient to improve the skin penetration of SHR0302 relative to the same topical pharmaceutical composition without laureth-4.
3. The method of claim 2 , wherein the SHR0302 is present in an amount of about 0.1 to about 1.0% w/w.
4. The method of claim 3 , wherein the laureth-4 is present in an amount of about 0.5 to about 5% w/w.
5. The method of claim 3 , wherein the laureth-4 is present in an amount of about 1% to about 4%.
6. The method of claim 4 , wherein the solvent is dimethyl sulfoxide.
7. The method of claim 6 , wherein said composition is selected from the group consisting of 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.
8. A method for preparing a topical SHR0302 pharmaceutical composition having improved skin penetration, comprising:
combining SHR0302, water, and at least one solvent with laureth-4,
wherein the amount of laureth-4 is sufficient to improve 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, wherein the topical pharmaceutical composition does not contain an additional active ingredient.
9. The method of claim 6 , wherein the SHR0302 is present in an amount of about 0.1 to about 1.0% w/w.
10. The method of claim 7 , wherein the laureth-4 is present in an amount of about 0.5 to about 5% w/w.
11. The method of claim 7 , wherein the laureth-4 is present in an amount of about 1% to about 4%.
12. The method of claim 8 , wherein the solvent is dimethyl sulfoxide.
13. The method of claim 10 , wherein said composition is selected from the group consisting of 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.
14. The method of claim 13 , wherein the amount of laureth-4 is sufficient to improve 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.