Treatment of erectile dysfunction and other indications
Inventors
Assignees
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Publication Number
US-10682357-B2
Publication Date
2020-06-16
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 transdermal/topical compositions for treating erectile dysfunction that include a phosphodiesterase type 5 inhibitor and, optionally, a nitric oxide donor. The composition is provided as a cream, gel, or lotion for topical delivery to the skin of a subject and is formulated to create an ionic hostile biophysical environment characterized by high chloride/ionic strength and pH-related ionization behavior that affect inhibitor performance.
The core formulation approach uses a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride together with sildenafil and/or a salt thereof. It further specifies formulation components including xanthan gum, propylene glycol, and a polysorbate surfactant comprising Polysorbate 20, while setting an ionic strength of at least 1 M.
The document addresses enhanced and rapid onset of topical action with reduced systemic exposure compared with oral dosing, and it reports high temperature stability. The temperature stability is achieved by combining a stabilization polymer, propylene glycol, and polysorbate, with stability reported at elevated temperatures. The document further includes example manufacturing/formulation tables and emulsion formulation concepts, including oil-in-water emulsion and water-in-oil emulsion.
Claims Coverage
The provided partial content includes two independent claims that cover topical skin compositions (cream, gel, or lotion) containing a nitric oxide donor based on L-arginine and/or L-arginine hydrochloride, sildenafil and/or a salt thereof, and a formulation with xanthan gum, propylene glycol, and polysorbate surfactant, where the composition has an ionic strength of at least 1 M. Across both independent claims, the main inventive features are the same, with dependent claims adding additional quantitative and packaging limitations, including heat stability requirements and ionic-salt concentration and identity constraints.
Hostile biophysical environment topical cream with high ionic strength and nitric oxide donor plus sildenafil
A cream, gel, or lotion composition for topical delivery to the skin that includes a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, xanthan gum, propylene glycol, and a polysorbate surfactant comprising Polysorbate 20, together with sildenafil and/or a salt thereof, wherein the composition has an ionic strength of at least 1 M.
Hostile biophysical environment topical cream with high ionic strength and nitric oxide donor plus sildenafil
A cream, gel, or lotion composition for topical delivery to the skin that includes a nitric oxide donor comprising L-arginine and/or L-arginine hydrochloride, xanthan gum, propylene glycol, and a polysorbate surfactant, together with sildenafil and/or a salt thereof, wherein the composition has an ionic strength of at least 1 M.
Both independent claims require a topical skin composition (cream, gel, or lotion) containing a nitric oxide donor based on L-arginine and/or L-arginine hydrochloride, sildenafil and/or a salt thereof, and a formulation defined by xanthan gum, propylene glycol, and polysorbate surfactant, combined with an ionic strength of at least 1 M. The claim set further narrows stability under heat exposure and can specify ionic-salt concentration and identity.
Stated Advantages
Improved transdermal migration with high-salt environments.
Enhanced and rapid onset of topical action.
Reduced systemic exposure compared with oral dosing.
High temperature stability at elevated temperatures.
Documented Applications
Treatment of erectile dysfunction using transdermal/topical compositions delivered to skin as a cream, gel, or lotion including phosphodiesterase type 5 inhibitors and, optionally, a nitric oxide donor.
Use in an erectile dysfunction scenario in the examples, including formulation concepts and hostile biophysical environment definition.
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