OXYMORPHONE CONTROLLED RELEASE FORMULATIONS
First Claim
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1. A controlled release oxymorphone formulation, comprising:
- a. about 5 mg to about 80 mg of oxymorphone or a pharmaceutically acceptable salt of oxymorphone;
b. a hydrophilic material; and
c. a filler, wherein upon oral administration of the formulation to a subject in need of an analgesic effect;
(i) the formulation provides detectable blood plasma levels of 6-OH oxymorphone and oxymorphone;
(ii) the blood plasma levels of 6-OH oxymorphone and oxymorphone peak within about 1 hour to about 8 hours after administration;
(iii) the blood plasma levels of 6-OH oxymorphone and oxymorphone exhibit a ratio of area under the curve (AUC(O to inf)) of blood plasma level versus time for 6-OH oxymorphone compared to oxymorphone in a range of about 0.5 to about 1.5; and
(iv) the duration of the analgesic effect is through at least about 12 hours after administration.
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Abstract
The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.
110 Citations
20 Claims
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1. A controlled release oxymorphone formulation, comprising:
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a. about 5 mg to about 80 mg of oxymorphone or a pharmaceutically acceptable salt of oxymorphone;
b. a hydrophilic material; and
c. a filler, wherein upon oral administration of the formulation to a subject in need of an analgesic effect;
(i) the formulation provides detectable blood plasma levels of 6-OH oxymorphone and oxymorphone;
(ii) the blood plasma levels of 6-OH oxymorphone and oxymorphone peak within about 1 hour to about 8 hours after administration;
(iii) the blood plasma levels of 6-OH oxymorphone and oxymorphone exhibit a ratio of area under the curve (AUC(O to inf)) of blood plasma level versus time for 6-OH oxymorphone compared to oxymorphone in a range of about 0.5 to about 1.5; and
(iv) the duration of the analgesic effect is through at least about 12 hours after administration. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
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13. A pharmaceutical tablet prepared by:
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a. mixing oxymorphone or a pharmaceutically acceptable salt of oxymorphone and granules comprising a hydrophilic material, a filler and one or more optional excipients; and
b. directly compressing the mixture of (a) to form the tablet. - View Dependent Claims (14, 15, 16, 17, 18, 19, 20)
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Specification