.

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: 6,143,322

« Back to Dashboard

Details for Patent: 6,143,322

Title: Method of treating humans with opioid formulations having extended controlled release
Abstract:Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form.
Inventor(s): Sackler; Richard (Greenwich, CT), Kaiko; Robert (Weston, CT), Goldenheim; Paul (Wilton, CT)
Assignee: Purdue Pharma L.P. (Norwalk, CT)
Filing Date:Apr 08, 1997
Application Number:08/838,368
Claims:1. A method for treating pain in humans for a time period of about 24 hours, comprising

preparing a solid, controlled-release oral dosage form consisting of a plurality of inert pharmaceutical beads coated with an analgesically effective amount of an opioid analgesic or a mixture of opioid analgesics or a salt thereof, said inert pharmaceutical beads overcoated with a controlled release coating, wherein the dissolution rate in-vitro of the dosage form when measured by the USP Paddle Method of U.S. Pharmacopeia XXII(1990) at 100 rpm at 900 ml aqueous buffer at 1.6 and 7.2 pH and 37.degree. C. from about 16.8% to about 42.5% (by wt) opioid release after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid release after 8 hours, the in-vitro release rate being substantially independent of pH in that a difference, at any given time, between an amount of opioid released at one pH and an amount released at any other pH, when measured in-vitro using the USP Paddle Method of U.S. Pharmacopeia XXII (1990) at 100 rpm in 900 ml aqueous buffer, is no greater than 10%, the in-vitro release rate being chosen such that the peak plasma level of said opioid obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form; said dosage form providing an extended duration of therapeutic effect of about 24 hours; and

administering said dosage form to a human patient at a dosing interval of about 24 hours.

2. The method of claim 1, wherein said controlled release coating comprises a pharmaceutically acceptable hydrophobic polymer.

3. The method of claim 1, further comprising the step of placing a sufficient quantity of said dosage form into a capsule prior to said administering step.

4. The method of claim 1, wherein said opioid analgesic is selected from the group consisting of hydromorphone, oxycodone, dihydrocodeine, codeine, dihydromorphone, morphine, buprenorphine, salts of any of the foregoing, and mixtures of any of the foregoing.

5. The method of claim 1, wherein said dosage form provides a peak plasma of said opioid analgesic from about 4 to about 6 hours after administration.

6. The method of claim 2, where said hydrophobic polymer is selected from the group consisting of a plasticized acrylic polymer, a plasticized ethylcellulose and a mixture thereof.

7. The method of claim 2, wherein said hydrophobic polymer is applied to said beads as an aqueous dispersion.

8. The method of claim 1, wherein said controlled release coating comprises a copolymer of acrylic and methacrylic acid.

9. The method of claim 1, wherein said controlled release coating comprises a material selected from the group consisting of methyl methacrylate copolymer, ethoxyethyl methacrylate, cyanoethyl methacrylate, poly(acrylic acid), poly(methacrylic acid), methacrylic acid alkylamide copolymer, poly(methyl methacrylate), polymethacrylate, poly(methyl methacrylate) copolymer, polyacrylamide, aminoalkyl methacrylate copolymer, poly(methacrylic acid anhydride), and glycidyl methacrylate copolymer.

10. The method of claim 1, wherein said controlled release coating comprises an alkylcellulose.

11. The method of claim 1, wherein said controlled release coating comprises one or more ammonio methacrylate copolymers.

12. The method of claim 1, wherein the dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of U.S. Pharmacopeia XXII (1990) at 100 rpm at 900 ml aqueous buffer at 1.6 and 7.2 pH at 37.degree. C. is about 31.1% (by wt) opioid released after 1 hour, about 37% (by wt) opioid released after 2 hours, about 51.5% (by wt) opioid released after 4 hours and greater than about 60% (by wt) opioid released after 8 hours.

13. The method of claim 1, wherein the dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of U.S. Pharmacopeia XXII (1990) at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. is about 31.1% (by wt) opioid released after 1 hour, about 37% (by wt) opioid released after 2 hours, about 51.5% (by wt) opioid released after 4 hours and greater than about 60% (by wt) opioid released after 8 hours.
« 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