Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-9498482-B2
Publication Date
2016-11-22
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 patent discloses a topical delivery composition for a subject. The composition is a cream, gel, or lotion that includes 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, together with a pharmaceutical agent and/or salt thereof for treating sexual dysfunction.
The formulation is characterized by an ionic salt and pH optimized to ionize the inhibitor within high salt environments, including chloride environments, and by stabilization of an emulsion using xanthan gum or KELTROL variants, propylene glycol, and Polysorbate 20. The disclosed composition is described as maintaining stability against phase separation and performance under thermal exposure.
The disclosed formulation is described as achieving unexpected high-temperature/thermal stability and enhanced transdermal migration. The documented pharmaceutical agents include a PDE5 inhibitor such as sildenafil and other named PDE5 inhibitors, with one example formulation treating sexual dysfunction using the specified topical components.
Claims Coverage
The document provides two independent claims. Each independent claim defines a topical cream, gel, or lotion composition with the same core formulation constraints for a nitric oxide donor, ionic salt, xanthan gum, propylene glycol, and Polysorbate 20, while differing in the specified scope of the pharmaceutical agent for sexual dysfunction.
Nitric oxide donor and hostile-ionic topical formulation with Polysorbate 20 and xanthan gum
A topical delivery composition for the skin comprising a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, an ionic salt, xanthan gum, propylene glycol, a polysorbate surfactant comprising Polysorbate 20, and a pharmaceutical agent and/or salt thereof for treating sexual dysfunction.
Topical nitric oxide donor cream, gel, or lotion with specified PDE5-class sexual dysfunction agents
A topical delivery composition for the skin comprising a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, an ionic salt, xanthan gum, propylene glycol, a polysorbate surfactant comprising Polysorbate 20, and a pharmaceutical agent for treating sexual dysfunction, the pharmaceutical agent comprising one or more of avanafil, lodenafil, mirodenafil, udenafil, acetildenafil, hydroxyacetildenafil, dimethylsildenafil, or thiomethisosildenafil.
Overall, the independent claims cover topical cream, gel, or lotion compositions that combine an L-arginine-based nitric oxide donor with an ionic salt, xanthan gum, propylene glycol, and Polysorbate 20, together with a sexual dysfunction pharmaceutical agent. One independent claim further specifies that the sexual dysfunction pharmaceutical agent includes one or more named PDE5-class agents.
Stated Advantages
Unexpected high-temperature/thermal stability.
Enhanced transdermal migration driven by high salt environments and pH optimized to ionize the inhibitor.
Documented Applications
Treatment of sexual dysfunction using a topical cream, gel, or lotion composition delivering a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride together with a pharmaceutical agent for sexual dysfunction.
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