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Details for Patent: 7,740,881

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Details for Patent: 7,740,881

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 LP (Stanford, CT)
Filing Date:Jul 24, 2000
Application Number:09/624,530
Claims:1. A method for treating pain in humans for a time period of about 24 hours, comprising administering to a human patient at a dosing interval of about 24 hours a solid, controlled-release oral dosage form comprising 8 to 64 mg of hydromorphone or a pharmaceutically acceptable salt thereof incorporated into a controlled-release formulation comprising a tablet overcoated with a controlled-release coating derived from an aqueous dispersion of a hydrophobic polymer selected from the group consisting of a cellulosic polymer, an acrylic polymer, and mixtures thereof, wherein the coating has been stabilized by curing for about 24 hours or more at a temperature greater than the glass transition temperature of the hydrophobic polymer and a relative humidity from about 60% to about 100% such that the dosage form attains a dissolution profile which is substantially unaffected by exposure to storage conditions of at least one month at a temperature of 40.degree. C. and a relative humidity of 75%, wherein (i) 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 pH 1.6 and 7.2 and at 37.degree. C., is such that from 12.5% to 42.5% (by wt) hydromorphone is released after 1 hour, from 25% to 65% (by wt) hydromorphone is released after 2 hours, from 45% to 85% (by wt) hydromorphone is released after 4 hours and greater than 60% (by wt) hydromorphone is released after 8 hours, and (ii) the in-vitro release rate is substantially independent of pH in that a difference, at any given time, between an amount of hydromorphone 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 dosage form providing a duration of therapeutic effect of at least 24 hours and a mean C.sub.max of hydromorphone from about 1070 pg/ml to about 1721 pg/ml and a T.sub.max of between 4.6 and 8 hours, based on a single dose administration of the dosage form comprising 8 mg of hydromorphone hydrochloride.

2. The method of claim 1, wherein said dosage form comprises a pharmaceutically acceptable salt of hydromorphone.

3. The method of claim 1, wherein said dosage form comprises hydromorphone hydrochloride.

4. The method of claim 1, wherein the controlled release formulation further comprises a polymer selected from the group consisting of a pharmaceutically acceptable gum, an alkylcellulose, a cellulose ether, an acrylic resin, and mixtures of the foregoing.

5. The method of claim 4, wherein the controlled release formulation further comprises a digestible substituted or unsubstituted C.sub.8-C.sub.50 hydrocarbon.

6. The method of claim 5, wherein said hydrocarbon is selected from the group consisting of fatty acids, fatty alcohols, mineral oils, vegetable oils, waxes and mixtures of any of the foregoing.

7. The method of claim 4, wherein said dosage form further comprises a polyalkyleneglycol.

8. A method for treating pain in humans for a time period of about 24 hours, comprising administering to a human patient at a dosing interval of about 24 hours a solid, controlled-release oral dosage form comprising an active agent consisting essentially of 8 to 64 mg of hydromorphone or a pharmaceutically acceptable salt thereof incorporated into a controlled-release formulation comprising a tablet overcoated with a controlled-release coating derived from an aqueous dispersion of a hydrophobic polymer selected from the group consisting of a cellulosic polymer, an acrylic polymer, and mixtures thereof, wherein the coating has been stabilized by curing for about 24 hours or more at a temperature greater than the glass transition temperature of the hydrophobic polymer and a relative humidity from about 60% to about 100% such that the dosage form attains a dissolution profile which is substantially unaffected by exposure to storage conditions of at least one month at a temperature of 40.degree. C. and a relative humidity of 75%, wherein (i) 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 pH 1.6 and 7.2 and at 37.degree. C., is such that from 12.5% to 42.5% (by wt) hydromorphone is released after 1 hour, from 25% to 65% (by wt) hydromorphone is released after 2 hours, from 45% to 85% (by wt) hydromorphone is released after 4 hours and greater than 60% (by wt) hydromorphone is released after 8 hours, and (ii) the in-vitro release rate is substantially independent of pH in that a difference, at any given time, between an amount of hydromorphone 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 dosage form providing a duration of therapeutic effect of at least 24 hours, a mean C.sub.max of hydromorphone from about 1070 pg/ml to about 1721 pg/ml and a T.sub.max of between 4.6 to 8 hours, based on a single dose administration of the dosage form comprising 8 mg of hydromorphone hydrochloride.

9. The method of claim 1, wherein the dosage form provides a peak plasma level of hydromorphone obtained in-vivo which occurs between 4.8 to 8 hours after administration of the dosage form.

10. The method of claim 8, wherein the dosage form provides a peak plasma level of hydromorphone obtained in-vivo which occurs between 4.8 to 8 hours after administration of the dosage form.

11. The method of claim 1, wherein the dosage form provides a peak plasma level of hydromorphone obtained in-vivo which occurs between 5.5 to 8 hours after administration of the dosage form.

12. The method of claim 8, wherein the dosage form provides a peak plasma level of hydromorphone obtained in-vivo which occurs between 5.5 to 8 hours after administration of the dosage form.

13. The method of claim 1, wherein the dosage form provides the mean C.sub.max of hydromorphone of 1211.+-.153 pg/ml.

14. The method of claim 1, wherein the dosage form provides a mean C.sub.24 of hydromorphone of about 600 pg/ml.

15. The method of claim 8, wherein the dosage form provides the mean C.sub.max of hydromorphone of 1211.+-.153 pg/ml.

16. The method of claim 8, wherein the dosage form provides a mean C.sub.24 of hydromorphone of about 600 pg/ml.

17. A method for treating pain in humans for a time period of about 24 hours, comprising administering to a human patient at a dosing interval of about 24 hours a solid, controlled-release oral dosage form comprising 8 to 64 mg of hydromorphone or a pharmaceutically acceptable salt thereof incorporated into a controlled-release formulation comprising a tablet overcoated with a controlled-release coating derived from an aqueous dispersion of a hydrophobic polymer selected from the group consisting of a cellulosic polymer, an acrylic polymer, and mixtures thereof, and a barrier coating separating hydromorphone from the controlled-release coating, wherein (i) 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 pH 1.6 and 7.2 and at 37.degree. C., is such that from 12.5% to 42.5% (by wt) hydromorphone is released after 1 hour, from 25% to 65% (by wt) hydromorphone is released after 2 hours, from 45% to 85% (by wt) hydromorphone is released after 4 hours and greater than 60% (by wt) hydromorphone is released after 8 hours, and (ii) the in-vitro release rate is substantially independent of pH in that a difference, at any given time, between an amount of hydromorphone 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 dosage form providing a duration of therapeutic effect of at least 24 hours, a mean C.sub.max of hydromorphone of from about 1070 pg/ml to about 1721 pg/ml and a T.sub.max of between 4.4 and 8 hours, based on a single dose administration of the dosage form comprising 8 mg of hydromorphone hydrochloride.

18. The method of claim 17, wherein the dosage form provides a mean C.sub.max of 1211.+-.153 pg/ml.

19. A method for treating pain in humans for a time period of about 24 hours, comprising administering to a human patient at a dosing interval of about 24 hours a solid, controlled-release oral dosage form comprising an active agent consisting essentially of 8 to 64 mg of hydromorphone or a pharmaceutically acceptable salt thereof incorporated into a controlled-release formulation comprising a tablet overcoated with a controlled-release coating derived from an aqueous dispersion of a hydrophobic polymer selected from the group consisting of a cellulosic polymer, an acrylic polymer, and mixtures thereof, wherein the coating has been stabilized by curing for about 24 hours or more at a temperature greater than the glass transition temperature of the hydrophobic polymer and at a relative humidity from about 60% to about 100% such that the dosage form attains a dissolution profile which is substantially unaffected by exposure to storage conditions of at least one month at a temperature of 40.degree. C. and a relative humidity of 75%, wherein (i) 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 pH 1.6 and 7.2 and at 37.degree. C., is such that from 12.5% to 42.5% (by wt) hydromorphone released after 1 hour, from 25% to 65% (by wt) hydromorphone released after 2 hours, from 45% to 85% (by wt) hydromorphone released after 4 hours and greater than 60% (by wt) hydromorphone released after 8 hours, and (ii) the in-vitro release rate is substantially independent of pH in that a difference, at any given time, between an amount of hydromorphone 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 dosage form providing a duration of therapeutic effect of at least 24 hours, a mean C.sub.max of hydromorphone from about 1070 pg/ml to about 1721 pg/ml and a T.sub.max of between 4.4 to 8 hours, based on a single dose administration of the dosage form comprising 8 mg of hydromorphone hydrochloride.

20. The method of claim 19, wherein the dosage form provides a mean C.sub.max of hydromorphone of 1211.+-.153 pg/ml.

21. The method of claim 1, wherein the controlled-release formulation further comprises a barrier coating separating hydromorphone from the controlled-release coating.

22. The method of claim 8, wherein the controlled-release formulation further comprises a barrier coating separating hydromorphone from the controlled-release coating.

23. The method of claim 19, wherein the controlled-release formulation further comprises a barrier coating separating hydromorphone from the controlled-release coating.
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