MODIFIED RELEASE DOSAGE FORMS OF SKELETAL MUSCLE RELAXANTS
First Claim
1. A pharmaceutical dosage form of a skeletal muscle relaxant providing a modified release profile comprising a population of extended release (ER) beads,wherein said ER beads comprisean active-containing core particle (IR (immediate release) bead) comprising a skeletal muscle relaxant;
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C. exhibits a drug release profile substantially corresponding to the following pattern;
after 2 hours, no more than about 40% of the total active is released;
after 4 hours, from about 40-65% of the total active is releasedafter 8 hours, from about 60-85% of the total active is released; and
after 12 hours, from about 75-85% of the total active is released;
thereby providing therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions in humans.
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Accused Products
Abstract
A unit dosage form, such as a capsule or the like, for delivering a skeletal muscle relaxant, such as cyclobenzaprine hydrochloride, into the body in an extended or sustained release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. At least one bead population exhibits a pre-designed sustained release profile. Such a drug delivery system is designed for once-daily oral administration to maintain an adequate plasma concentration-time profile, thereby providing relief of muscle spasm associated with painful musculoskeletal conditions over a 24 hour period.
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Citations
22 Claims
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1. A pharmaceutical dosage form of a skeletal muscle relaxant providing a modified release profile comprising a population of extended release (ER) beads,
wherein said ER beads comprise an active-containing core particle (IR (immediate release) bead) comprising a skeletal muscle relaxant; - and
an ER (extended release) coating comprising a water insoluble polymer membrane surrounding said core, wherein said dosage form when dissolution tested using United States Pharmacopoeia Apparatus 2 (paddles @ 50 rpm) in 900 mL of 0.1N HCl at 37°
C. exhibits a drug release profile substantially corresponding to the following pattern;after 2 hours, no more than about 40% of the total active is released; after 4 hours, from about 40-65% of the total active is released after 8 hours, from about 60-85% of the total active is released; and after 12 hours, from about 75-85% of the total active is released; thereby providing therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions in humans. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 22)
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12. A method for the preparation of an oral once-daily drug delivery system comprising a skeletal muscle relaxant, comprising the steps of:
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a. preparing an active-containing core to form IR beads; b. coating the IR beads with an extended release coating comprising a plasticized water insoluble polymer to form ER (extended release) beads; and c. filling capsules with ER beads and optionally IR Beads at a ratio from about 70;
30 to 100;
0;wherein said dosage form when dissolution tested using United States Pharmacopoeia Apparatus 2 (paddles @ 50 rpm) in 900 mL of 0.1N HCl at 37°
C. exhibits a drug release profile substantially corresponding to the following pattern;after 2 hours, no more than about 40% of the total active is released; after 4 hours, from about 40-65% of the total active is released after 8 hours, from about 60-85% of the total active is released; and after 12 hours, from about 75-85% of the total active is released. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20, 21)
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Specification