Oral soluble film containing sildenafil citrate

Abstract

The present invention relates to an oral soluble film (OSF), methods of orally administering the same, and methods of manufacturing the same. The oral soluble film includes sildenafil citrate, and can further include a binder, filler, flavoring agent, plasticizer, sweetening agent, preservative, solvent, and optionally coloring agent. The active ingredient and excipients can be provided and present in an amount effective to achieve desired physical and performance characteristics of the OSF.

Description

RELATED U.S. APPLICATION DATA[0001]The present application is a continuation of U.S. patent application Ser. No. 17 / 236,054, filed on Apr. 4, 2021, which claims the benefit of U.S. provisional patent application No. 63 / 012,988, filed on Apr. 21, 2020; each of which is incorporated by reference herein in its entirety.BACKGROUND OF THE INVENTION[0002]Sildenafil, sold under the brand name Viagra® among others, is a medication used to treat erectile dysfunction (ED) and pulmonary arterial hypertension (PAH). It is taken by mouth, or injection into a vein. Sildenafil acts by blocking phosphodiesterase 5 (PDES), an enzyme that promotes breakdown of cGMP, which regulates blood flow in the penis. It requires sexual arousal, however, to work for ED. It also results in dilation of the blood vessels in the lungs.[0003]Pfizer originally discovered the medication in 1989 while looking for a treatment for heart-related chest pain. It was approved for medical use in the United States and in the Eu...

AI Technical Summary

Benefits of technology

[0011]Across multiple embodiments, the OSF described herein can independently possess one or more advantages relative to other OSFs and / or traditional dosage forms (e.g., tablets and capsules). The one or more advantages can relate to, e.g., physical characteristics and / or performance characteristics of the oral soluble film. For example, in specific embodiments, the OSF can be in the form of a unit dose having a requisite drug load, while having acceptable physical dimensions (e.g., length, width, and thickness), mass, and water content; and while also exhibiting a desired disintegration time and pharmacokinetic (PK) profile. In specific embodiments, the variation of active ingredient between two equally sized unit dosages is relatively small. In specific embodiments, accuracy in the administered dose can be assured from every strip or film. In specific embodiments, the unit dose has a suitable breaking strength, elongation strength, loss on drying (LOD), surface area, and / or density. In specific embodiments, the OSF is flexible, compliant, and not brittle. In specific embodiments, the OSF does not have an unpleasant taste (e.g., the bitter taste of the active ingredient is effectively masked). In specific embodiments, the OSF does not have an unpleasant mouth feel. In specific embodiments, upon administration to the subject, the oral soluble film exhibits a suitable pharmacokinetic (PK) profile that includes, e.g., AUC, Cmax, tmax, and / or t1 / 2. In specific embodiments, relative to an oral tablet having an equivalent amount of sildenafil citrate (e.g., Viagra®), administration of the oral soluble film results in a lower incidence, severity, and / or duration of one or more adverse reactions. In specific embodiments, a single dose of the oral soluble film is individually packaged and sealed with a primary packaging material. In specific embodiments, a single dose of strip can be individually packaged without requiring a secondary container. Individually packaged OSFs are typically more difficult to tamper with, compared to traditional packages for tablets and capsules, such as bottles or foil blister packs. Additionally, many consumers may prefer the convenience to carry individually packaged OSFs. In specific embodiments, the individually packaged OSF can be easily handled, stored, and transported. In further specific embodiments, the primary packaging material forms a primary package that protects the oral soluble film from light, protects the oral soluble film from microbial contamination, is child resistant, is a barrier to moisture and vapor, is airtight, and / or mitigates leachable(s) into the oral soluble film. In specific embodiments, the OSF can easily be titrated. In specific embodiments, the OSF can be discretely administered. In specific embodiments, the OSF can be administered in the absence of water or beverage. This makes the dosage form acceptable among pediatric and geriatric patients, as well as patients with a fear of choking (e.g., those suffering from dysphagia).

[0025]The present invention also provides for a single dose of the oral soluble film described herein, that is individually packaged and sealed with a primary packaging material. The primary packaging material includes multiple layers, wherein at least one layer is manufactured from metalized polyester. The primary packaging material forms a primary package that (i) protects the oral soluble film from light, (ii) protects the oral soluble film from microbial contamination, (iii) is child resistant, (iv) is a barrier to moisture and vapor, (v) is airtight, (vi) mitigates leachable(s) into the oral soluble film, (vii) identifies a logo and / or includes printed indicia, or (viii) any combination thereof.

Problems solved by technology

Individually packaged OSFs are typically more difficult to tamper with, compared to traditional packages for tablets and capsules, such as bottles or foil blister packs.

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