.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 9,040,086

« Back to Dashboard

Details for Patent: 9,040,086

Title:Timed, sustained release systems for propranolol
Abstract: A unit dosage form, such as a capsule or the like for delivering drugs into the body in a circadian release fashion, is comprising of one or more populations of propranolol-containing particles (beads, pellets, granules, etc.). Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release cardiovascular drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need during the day, i.e., mimicking the circadian rhythm and severity/manifestation of a cardiovascular disease, predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro/in vivo correlations.
Inventor(s): Percel; Phillip J. (Troy, OH), Vishnupad; Krishna S. (Dayton, OH), Venkatesh; Gopi M. (Vandalia, OH)
Assignee: Aptalis Pharmatech, Inc. (Vandalia, OH)
Filing Date:Aug 09, 2006
Application Number:11/500,892
Claims:1. A timed, sustained-release (TSR) pharmaceutical formulation comprising timed, sustained release beads, wherein said TSR beads comprise: a) a core comprising propranolol or a pharmaceutically acceptable salt thereof; b) a first membrane comprising a first water insoluble polymer surrounding said core; c) a second outer membrane comprising a mixture of a second water insoluble polymer and an enteric polymer; wherein said formulation provides a lag time in propranolol blood plasma concentration of about 2 to about 6 hours, wherein said formulation comprises about 80 mg, about 120 mg, or about 160 mg of propranolol or a pharmaceutically acceptable salt thereof, wherein said formulation provides a maximum blood plasma concentration (C.sub.max) between about 10 and about 14 hours following administration.

2. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation comprises about 160 mg of propranolol or a pharmaceutically acceptable salt thereof, and provides a maximum blood plasma concentration (C.sub.max) within the range of 80% to 125% of about 177 ng/mL of propranolol between about 10 and about 14 hours following administration and an AUC.sub.0-T within the range of 80% to 125% of about 3417 nghr/mL.

3. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation comprises about 120 mg of propranolol or a pharmaceutically acceptable salt thereof, and provides a maximum blood plasma concentration (C.sub.max) within the range of 80% to 125% of about 130 ng/ml, of propranolol between about 10 and about 14 hours following administration and an AUC.sub.0-T within the range of 80% to 125% of about 2270 nghr/mL.

4. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation comprises about 80 mg of propranolol or a pharmaceutically acceptable salt thereof, and provides a maximum blood plasma concentration (C.sub.max) within the range of 80% to 125% of about 81 ng/mL of propranolol between about 10 and about 14 hours following administration and an AUC.sub.0-T within the range of 80% to 125% of about 1443 nghr/mL.

5. The pharmaceutical formulation of claim 1 wherein the first and second water insoluble polymers are independently selected from the group consisting of ethylcellulose, polyvinyl acetate, neutral copolymers based on ethyl acrylate and methylmethacrylate, and copolymers of acrylic and methacrylic acid esters with quaternary ammonium groups.

6. The pharmaceutical formulation of claim 1 wherein the enteric polymer is selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate, polyvinyl acetate phthalate, pH-sensitive methacrylic acid-methamethacrylate copolymers and shellac.

7. The pharmaceutical formulation of claim 1 whereby the first and second water insoluble polymers are ethylcellulose and the enteric polymer is a pH sensitive methacrylic acid-methamethacrylate copolymer.

8. A method of propranolol therapy which comprises administering orally to a human in need thereof the pharmaceutical formulation of claim 1.

9. A method of propranolol therapy which comprises administering orally to a human in need thereof the pharmaceutical formulation of claim 2.

10. A method of propranolol therapy which comprises administering orally to a human in need thereof the pharmaceutical formulation of claim 3.

11. A method of propranolol therapy which comprises administering orally to a human in need thereof the pharmaceutical formulation of claim 4.

12. A method of decreasing blood pressure during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 1.

13. A method of decreasing blood pressure during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 2.

14. A method of decreasing blood pressure during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 3.

15. A method of decreasing blood pressure during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 4.

16. A method of preventing angina during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 1.

17. A method of preventing angina during the early waking hours comprising orally administering once daily before bed time to a human in need thereof the pharmaceutical formulation of claim 2.

18. A method of preventing angina during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 3.

19. A method of preventing angina during the early waking hours comprising orally administering once daily before bedtime to a human in need thereof the pharmaceutical formulation of claim 4.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc