Pharmaceutical Forms with Improved Pharmacokinetic Properties

• US 20080249096A1
• Filed: 02/16/2006
• Published: 10/09/2008
• Est. Priority Date: 03/01/2005
• Status: Active Grant

• Current Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Original Assignee: Bayer Healthcare AG (Bayer AG)
• Inventors: Serno, Peter, Hayauchi, Yutaka, Heinig, Roland, Pauli, Kerstin
• Granted Patent: US 8,613,950 B2
• Time in Patent Office: Days
• US Class Current: 514/243
• CPC Class Codes: A61K 31/53 having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine melarsoprol A61K31/555 ; with four nitrogen atoms A61K31/495
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present application relates to novel drug formulations of vardenafil which dissolve rapidly in the mouth and lead to increased bioavailability and to a plateau-like plasma concentration profile, and to processes for their preparation.

Claims

1. A drug formulation of vardenafil which disintegrates rapidly in the mouth, wherein at least 80% of the vardenafil in the drug formulation dissolves at 25°

C. in 10 ml of physiological saline and the rate of release of the vardenafil from the drug formulation in 900 ml of physiological saline within the first 5 minutes in the USP pedal stirrer apparatus at 50 rotations per minute at 37°

C. is at least 70%.

2. The drug formulation according to claim 1, wherein the vardenafil is in the form of a salt with an acid or vardenafil with an acid.

3. The drug formulation according to claim 2, wherein the vardenafil is vardenafil hydrochloride or vardenafil hydrochloride trihydrate.

4. The drug formulation according to claim 3, wherein the vardenafil hydrochloride or vardenafil hydrochloride trihydrate is in micronized form with a mean particle size of less than 20 μ

m.

5. The drug formulation according to any one of claims 1 to 4, further comprising a sugar alcohol at about 40% to 99%.

6. A pharmaceutical package comprising the drug formulation according to any one of claims 1 to 4 instructions that the drug formulation is to be inserted into the oral cavity and, after its disintegration, to be swallowed.