Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-9737543-B2
Publication Date
2017-08-22
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 invention provides transdermal/topical compositions for erectile dysfunction that include a phosphodiesterase type 5 inhibitor and a nitric oxide donor, where the composition is applied as a cream, gel, or lotion to a genital region of a male subject. The composition produces an erection in less than 15 minutes after application, and the nitric oxide donor comprises L-arginine and/or L-arginine hydrochloride. Sildenafil and/or a salt thereof is included in the composition.
The formulation further includes an ionic salt at a concentration of at least about 0.25 M, and uses xanthan gum at no more than about 1 wt % together with propylene glycol at at least about 6% by weight. Polysorbate 20 is used at no more than about 3 wt %, and the composition is described as addressing a hostile biophysical environment with formulation stabilizers that provide improved performance.
The disclosed high ionic strength and pH optimization are used to ionize the inhibitor, and the topical composition is stated to provide rapid action versus oral dosing in the time-to-effect range described. The combination of ingredients provides unexpected high temperature stability, including stability at about 40°C for extended periods, compared to formulations missing one component.
Claims Coverage
The document contains two independent claims, each centered on applying a cream, gel, or lotion to a genital region. Across the independent claims, the inventive features consistently include a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, a high-ionic-strength ionic salt, limited xanthan gum, propylene glycol, limited Polysorbate 20, and sildenafil and/or a salt thereof.
Rapid erection after topical application
Applying a composition comprising a cream, gel, or lotion to the genital region of a male subject, wherein the composition produces an erection in less than 15 minutes after application.
Nitric oxide donor with L-arginine and/or L-arginine hydrochloride
The composition comprises a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride at a concentration of about 2.5% to about 15% by weight.
High ionic strength ionic salt
The composition comprises an ionic salt at a concentration of at least about 0.25 M.
Xanthan gum and propylene glycol with limited Polysorbate 20
The composition comprises xanthan gum at no more than about 1 wt %; propylene glycol at at least about 6% by weight; and Polysorbate 20 at no more than about 3 wt %.
Sildenafil for erectile dysfunction
The composition comprises sildenafil and/or a salt thereof.
Both independent claims are grounded on a method of applying a cream, gel, or lotion to a genital region using a formulation containing L-arginine and/or L-arginine hydrochloride, an ionic salt at high concentration, limited xanthan gum, sufficient propylene glycol, limited Polysorbate 20, and sildenafil or a salt thereof. Dependent claims further specify time-to-erection, stability at about 40°C, and optional excipients and packaged nitric oxide donor forms.
Stated Advantages
Provides an erection in less than 15 minutes after application.
Provides unexpected high temperature stability, including stability at about 40°C for extended periods.
Documented Applications
Topical/transdermal treatment of erectile dysfunction via applying a cream, gel, or lotion to a genital region of a male subject.
Topical use in a hostile biophysical environment, as described for the topical composition.
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