Modified Release Dosage Forms of Skeletal Muscle Relaxants
OwnerGopi Venkatesh, James M. Clevengerinventors
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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.
Claims22
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.
A method for the preparation of an oral once-daily drug delivery system comprising a skeletal muscle relaxant, comprising the steps of:
- 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.
Dependencies are inferred from the claim text.