Encased Tamper Resistant Controlled Release Dosage Forms
First Claim
Patent Images
1. A solid controlled release dosage form comprising:
- a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and
a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material;
wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.
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Abstract
In certain embodiments, the present invention is directed to a solid controlled release dosage form comprising: a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37 C.
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Citations
136 Claims
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1. A solid controlled release dosage form comprising:
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a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 10, 14, 17, 20, 23, 24, 25, 28, 29, 30, 31, 32, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 70, 80, 81, 82, 87, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 129)
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9. (canceled)
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11-13. -13. (canceled)
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15-16. -16. (canceled)
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18-19. -19. (canceled)
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21-22. -22. (canceled)
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26-27. -27. (canceled)
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33-34. -34. (canceled)
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65-69. -69. (canceled)
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71-79. -79. (canceled)
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83-86. -86. (canceled)
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88-89. -89. (canceled)
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122. A solid controlled release dosage form comprising:
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a core comprising a first portion of an opioid analgesic dispersed in a first matrix material comprising polyethylene oxide; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material comprising polyethylene oxide.
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123. A solid controlled release dosage form comprising:
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a compressed core comprising a first portion of an opioid analgesic dispersed in a first matrix material comprising polyethylene oxide; and a compression coating encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material comprising polyethylene oxide.
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124. A solid controlled release dosage form comprising:
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a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and a shell encasing the core and comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form at 2 hours is less than about 25%; the amount of opioid analgesic released from the dosage form at 4 hours is from about 10% to about 30%; the amount of opioid analgesic released from the dosage form at 8 hours is from about 20% to about 60%; the amount of opioid analgesic released from the dosage form at 12 hours is from about 40% to about 90%; and the amount of opioid analgesic released from the dosage form at 18 hours is greater than about 70%; as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
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125. A solid controlled release dosage form comprising:
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a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a controlled release excipient; wherein the amount of hydrocodone or salt thereof released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.; andthe dosage form can be flattened without breaking, wherein the thickness of the dosage form after flattening corresponds to no more than about 20% of the thickness of the dosage form before flattening; and the amount of hydrocodone or salt thereof released at 0.5 hour from a flattened dosage form deviates no more than about 20% points from a non-flattened dosage form as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
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126. A solid controlled release dosage form comprising:
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a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a controlled release excipient; wherein the amount of hydrocodone or salt thereof released from the dosage form at 2 hours is less than about 25%; the amount of hydrocodone or salt thereof released from the dosage form at 4 hours is from about 10% to about 30%; the amount of hydrocodone or salt thereof released from the dosage form at 8 hours is from about 20% to about 60%; the amount of hydrocodone or salt thereof released from the dosage form at 12 hours is from about 40% to about 90%; and the amount of hydrocodone or salt thereof released from the dosage form at 18 hours is greater than about 70%; as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.; andthe dosage form can be flattened without breaking, wherein the thickness of the dosage form after flattening corresponds to no more than about 20% of the thickness of the dosage form before flattening; and the amount of hydrocodone or salt thereof released at 0.5 hour from a flattened dosage form deviates no more than about 20% points from a non-flattened dosage form as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
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127. A solid controlled release dosage form comprising:
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a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof dispersed in a controlled release excipient;
wherein the inner 60% of the dosage form contains at least 80% of the hydrocodone or salt thereof;wherein the amount of hydrocodone or salt thereof released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C. - View Dependent Claims (128)
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130. A method of preparing a solid controlled release dosage form comprising:
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preparing a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and encasing the core with a shell comprising a second portion of the opioid analgesic dispersed in a second matrix material; wherein the amount of opioid analgesic released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
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131. A method of preparing a solid controlled release dosage form comprising:
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preparing a core comprising a first portion of an opioid analgesic dispersed in a first matrix material comprising polyethylene oxide; and encasing the core in a shell comprising a second portion of the opioid analgesic dispersed in a second matrix material comprising polyethylene oxide.
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132. A method of preparing a solid controlled release dosage form comprising:
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preparing a compressed core comprising a first portion of an opioid analgesic dispersed in a first matrix material comprising polyethylene oxide; and encasing the core by compression coating a second portion of the opioid analgesic dispersed in a second matrix material comprising polyethylene oxide over the core.
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133. A method of preparing a solid controlled release dosage form comprising:
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preparing a core comprising a first portion of an opioid analgesic dispersed in a first matrix material; and encasing the core in a shell comprising a second portion of the opioid analgesic dispersed in a second matrix material over the core; wherein the amount of opioid analgesic released from the dosage form at 2 hours is less than about 25%; the amount of opioid analgesic released from the dosage form at 4 hours is from about 10% to about 30%; the amount of opioid analgesic released from the dosage form at 8 hours is from about 20% to about 60%; the amount of opioid analgesic released from the dosage form at 12 hours is from about 40% to about 90%; and the amount of opioid analgesic released from the dosage form at 18 hours is greater than about 70%. as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
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134. A method of preparing a solid controlled release dosage form comprising:
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combining a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a controlled release excipient; wherein the amount of hydrocodone or salt thereof released from the dosage form is proportional within 20% to elapsed time, at any two time points from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.; andthe dosage form can be flattened without breaking, wherein the thickness of the dosage form after flattening corresponds to no more than about 20% of the thickness of the dosage form before flattening; and the amount of hydrocodone or salt thereof released at 0.5 hour from a flattened dosage form deviates no more than about 20% points from a non-flattened dosage form as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.
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135. A method of preparing a solid controlled release dosage form comprising:
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combining a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a controlled release excipient; wherein the amount of hydrocodone or salt thereof released from the dosage form at 2 hours is less than about 25%; the amount of hydrocodone or salt thereof released from the dosage form at 4 hours is from about 10% to about 30%; the amount of hydrocodone or salt thereof released from the dosage form at 8 hours is from about 20% to about 60%; the amount of hydrocodone or salt thereof released from the dosage form at 12 hours is from about 40% to about 90%; and the amount of hydrocodone or salt thereof released from the dosage form at 18 hours is greater than about 70%; as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.; andthe dosage form can be flattened without breaking, wherein the thickness of the dosage form after flattening corresponds to no more than about 20% of the thickness of the dosage form before flattening; and the amount of hydrocodone or salt thereof released at 0.5 hour from a flattened dosage form deviates no more than about 20% points from a non-flattened dosage form as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.
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136. A method of preparing a solid controlled release dosage form comprising:
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dispersing a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof in a controlled release excipient;
wherein the inner 60% of the dosage form contains at least 80% of the hydrocodone or salt thereof;wherein the amount of hydrocodone or salt thereof released from the dosage form is proportional within 20% to elapsed time from 8 to 24 hours, as measured by an in-vitro dissolution in a USP Apparatus 1 (basket) at 100 rpm in 900 ml simulated gastric fluid without enzymes (SGF) at 37°
C.
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Specification