Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-9492458-B2
Publication Date
2016-11-15
Expiration Date
Abstract
The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising a phosphodiesterase type 5 inhibitor and/or a salt thereof, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.
Core Innovation
The invention relates to a composition for topical delivery to the skin of a subject. The composition is a cream, gel, or lotion comprising a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, an ionic salt, xanthan gum, propylene glycol, and a polysorbate surfactant comprising Polysorbate 20. The formulation further includes a pharmaceutical agent and/or salt thereof for treating sexual dysfunction.
The disclosed compositions position the L-arginine-based nitric oxide donor together with high concentrations of ionic salt and defined levels of xanthan gum, propylene glycol, and Polysorbate 20. The background/problem context described in the provided material is the presence of a hostile biophysical environment, typically created by high chloride/ionic strength.
A stabilization system is disclosed as unexpected improvement for temperature stability and sustained efficacy in high-salt emulsions. The system includes xanthan gum, propylene glycol, and a polysorbate surfactant including Polysorbate 20.
Claims Coverage
The partial claim set includes two independent claims. Both independently define a topical skin-delivery cream, gel, or lotion with an L-arginine-based nitric oxide donor combined with defined ionic salt, xanthan gum, propylene glycol, and a Polysorbate 20 surfactant, together with a specified class of sexual dysfunction therapeutic agents; one independent claim further restricts the PDE5 inhibitor selection to exclude sildenafil.
Topical skin-delivery composition with L-arginine nitric oxide donor and high ionic salt
A cream, gel, or lotion comprising a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, an ionic salt, xanthan gum, propylene glycol, and a polysorbate surfactant comprising Polysorbate 20.
Sexual dysfunction agent selection for topical delivery
The topical composition further includes a pharmaceutical agent and/or salt thereof for treating sexual dysfunction, comprising one or more of yohimbe, alprostadil, tadalafil, apomorphine, and vardenafil.
PDE5 inhibitor topical delivery excluding sildenafil
A cream, gel, or lotion comprising the L-arginine nitric oxide donor, ionic salt, xanthan gum, propylene glycol, and Polysorbate 20, together with a phosphodiesterase type 5 inhibitor and/or a salt thereof that is not sildenafil.
Across the independent claims, the inventive core is a topical cream, gel, or lotion that combines an L-arginine or L-arginine hydrochloride nitric oxide donor with defined excipients and pairs this with a sexual dysfunction therapeutic agent set; one independent claim specifically requires a PDE5 inhibitor that is not sildenafil.
Stated Advantages
Unexpected improvement in temperature stability and sustained efficacy in high-salt emulsions.
Temperature stability at 40°C for at least about 4 weeks.
Documented Applications
Treating erectile dysfunction (sexual dysfunction) via topical delivery to the skin using the disclosed compositions comprising PDE5 inhibitors and/or other sexual dysfunction agents together with an L-arginine-based nitric oxide donor.
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