Claims for Patent: 9,532,971

Summary for Patent: 9,532,971

Title:	Low-dose doxepin formulations and methods of making and using the same
Abstract:	The invention disclosed herein generally relates to low-dose oral doxepin pharmaceutical formulations and the use of these formulations to promote sleep.
Inventor(s):	Schioppi; Luigi (Escondido, CA), Dorsey; Brian Talmadge (Encinitas, CA), Skinner; Michael (San Diego, CA), Carter; John (Keswick, CA), Mansbach; Robert (San Diego, CA), Jochelson; Philip (San Diego, CA), Rogowski; Roberta L. (Rancho Santa Fe, CA), Casseday; Cara Baron (San Diego, CA), Perry; Meredith (San Diego, CA), Knox; Bryan (San Diego, CA)
Assignee:	Pernix Sleep, Inc. (Morristown, NJ)
Application Number:	13/898,364
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,532,971
Patent Claims:	1. A pharmaceutical composition comprising from about 0.5 to about 7 mg of doxepin, or a pharmaceutically acceptable salt thereof, and from about 92% to about 99.8% w/w silicified microcrystalline cellulose, the composition having one or more of the characteristics selected from the group consisting of: a hardness value of at least 2 Kp, a friability value of 1% or less, a disintegration time of about 1 minute as per USP protocols, at least an 80% release of doxepin within 15 minutes using compendial method for measuring dissolution of doxepin, at least an 85 percent release of doxepin within 30 minutes using U.S. Pharmacopeia (USP) Apparatus I at 100 rpm (or Apparatus II at 50 rpm) in 0.1 N HCl or Simulated Gastric Fluid USP without enzymes, at least an 85 percent release of doxepin within 30 minutes using U.S. Pharmacopeia (USP) Apparatus I at 100 rpm (or Apparatus II at 50 rpm) in a pH 4.5 buffer, and at least an 85 percent release of doxepin within 30 minutes using U.S. Pharmacopeia (USP) Apparatus I at 100 rpm (or Apparatus II at 50 rpm) in a pH 6.8 buffer or Simulated Intestinal Fluid USP without enzymes; and wherein the pharmaceutical composition has dissolution and bioavailablity characteristics such that after administration to a 70 kg human, the composition provides a plasma concentration of at least 0.05 ng/mL doxepin within a time frame of not more than about 90 minutes. 2. The composition of claim 1, further comprising from about 0.1 to about 1.5% w/w colloidal silicon dioxide. 3. The composition of claim 1, further comprising from about 0.25 to about 1.5% w/w magnesium stearate. 4. The composition of claim 1, wherein the doxepin is provided in an amount of about 2.5 to about 4 mg. 5. The composition of claim 4, wherein the doxepin is provided in an amount of about 3 mg. 6. The composition of claim 1, wherein the doxepin is provided in an amount of about 6 mg. 7. A pharmaceutical unit dosage form, comprising: doxepin or a pharmaceutically-acceptable salt thereof in an amount equivalent to about 3 or 6 mg doxepin hydrochloride; one or more pharmaceutically-acceptable excipients; and optionally, a capsule or coating; wherein the excipients and any capsule or coating are selected to provide a swallowable unit dosage that is at least externally solid and that has dissolution and bioavailablity characteristics such that after administration to a 70 kg human, the dosage form provides a plasma concentration of at least 0.1 ng/mL doxepin within a time frame of not more than about 60 minutes; and wherein the unit dosage form comprises about 92% to about 99.8% w/w silicified microcrystalline cellulose. 8. The unit dosage form of claim 7, wherein the time frame to provide a plasma concentration of at least 0.1 ng/mL is not more than about 50 minutes. 9. The unit dosage form of claim 7, wherein the doxepin or the pharmaceutically-acceptable salt thereof is in an amount equivalent to about 3 mg doxepin hydrochloride. 10. The unit dosage form of claim 7, wherein the doxepin or the pharmaceutically-acceptable salt thereof is in an amount equivalent to about 6 mg doxepin hydrochloride.