PDE5 inhibitor powder formulations and methods relating thereto
Inventors
Xu, Zhen • SMYTH, HUGH • Gibbons, Aileen • Shreeniwas, Revati • Soni, Pravin • Deaton, Dan • Hannon, James • Lermer, Stephen • Curtis, Robert • Donovan, Martin J.
Assignees
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Publication Number
US-11806314-B2
Publication Date
2023-11-07
Expiration Date
Abstract
Novel dry powder compositions comprising and methods relating thereto are provided. The dry powder compositions comprise PDE5 inhibitors, such as vardenafil, or pharmaceutically acceptable salts or esters thereof. The dry powder compositions may optionally include an carrier/excipient. The concentration of active agent may be at least about 2% by weight. Methods of aerosolizing the dry powder compositions and using them to treat various diseases are also disclosed.
Core Innovation
The disclosed invention provides a pharmaceutical composition in dry powder form suitable for oral inhalation. The composition comprises a micronized hydrochloride salt of vardenafil at about 2% to about 20% by weight of the total weight of the composition, and the micronized hydrochloride salt of vardenafil has a Dv50 of about 5 microns or less.
The composition further includes lactose having an average particle size between about 2 microns to about 250 microns. The lactose comprises a fine lactose fraction from about 2% to about 50% by weight of the total lactose component, and the fine lactose fraction has a particle size of less than 7 microns.
The disclosure also addresses pulmonary delivery of the vardenafil hydrochloride salt as inhalable aerosol from a dry powder inhaler. The inhaler includes a dispersion chamber with inlet and outlet channels configured to receive and deliver the composition to a subject.
Claims Coverage
The independent claims explicitly cover three inventive features: a dry powder oral inhalation composition with micronized vardenafil hydrochloride salt, controlled lactose particle size and fine fraction, and a dry powder inhaler with a dispersion chamber including inlet and outlet channels.
Micronized hydrochloride salt of vardenafil in dry powder inhalation composition
A pharmaceutical composition comprising at least about 2% to about 20% by weight of a micronized hydrochloride salt of vardenafil based on the total weight of the pharmaceutical composition, wherein the micronized hydrochloride salt of vardenafil has a Dv50 of about 5 microns or less, and wherein the pharmaceutical composition is in dry powder form suitable for oral inhalation.
Lactose with controlled fine lactose fraction
The pharmaceutical composition comprises lactose having an average particle size between about 2 microns to about 250 microns and comprising a fine lactose fraction from about 2% to about 50% by weight of the total lactose component, wherein the fine lactose fraction has a particle size of less than 7 microns.
Dry powder inhaler with dispersion chamber and channels
A dry powder inhaler for delivering the pharmaceutical composition, wherein the dry powder inhaler includes a dispersion chamber with an inlet channel to receive the composition and an outlet channel to deliver it to the subject.
Overall, the claim coverage centers on a dry powder oral inhalation composition defined by the vardenafil hydrochloride salt Dv50 limit and weight range, together with lactose having the stated particle-size range and fine fraction. The disclosure additionally ties delivery to pulmonary administration using a dry powder inhaler with a dispersion chamber including inlet and outlet channels.
Stated Advantages
Improved emitted/respirable fractions for lactose-blended formulations versus pure drug.
Documented Applications
Treating pulmonary arterial hypertension via pulmonary administration using a dry powder inhaler delivering an inhalable aerosol of the disclosed composition.
Treating cystic fibrosis via pulmonary administration using a dry powder inhaler delivering an inhalable aerosol of the disclosed composition.
Treating congestive heart failure via pulmonary administration using a dry powder inhaler delivering an inhalable aerosol of the disclosed composition.
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