Modified release dosage forms of skeletal muscle relaxants
DCFirst Claim
1. A dosage form comprising a plurality of active-containing particles comprising cyclobenzaprine hydrochloride and a dissolution rate controlling polymer granulated together,wherein the dissolution rate controlling polymer is selected from the group consisting of ethers of cellulose and esters of cellulose;
- wherein the 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; and
after 8 hours, from about 60-85% of the total active is released; and
wherein the dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions.
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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.
67 Citations
73 Claims
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1. A dosage form comprising a plurality of active-containing particles comprising cyclobenzaprine hydrochloride and a dissolution rate controlling polymer granulated together,
wherein the dissolution rate controlling polymer is selected from the group consisting of ethers of cellulose and esters of cellulose; -
wherein the 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; and after 8 hours, from about 60-85% of the total active is released; and wherein the dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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19. A dosage form comprising a plurality of active-containing particles comprising cyclobenzaprine hydrochloride and a dissolution rate controlling polymer, granulated together;
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wherein the dissolution rate controlling polymer is selected from the group consisting of ethers of cellulose and esters of cellulose; wherein said dosage form comprises 30 mg of cyclobenzaprine hydrochloride and provides a maximum blood plasma concentration (Cmax) within the range of about 80% to 125% of about 20 ng/mL of cyclobenzaprine hydrochloride following oral administration of a single 30 mg cyclobenzaprine dose; and wherein said dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions. - View Dependent Claims (20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31)
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32. A dosage form comprising a plurality of active-containing particles comprising cyclobenzaprine hydrochloride and a dissolution rate controlling polymer surrounding the cyclobenzaprine hydrochloride,
wherein the dissolution rate controlling polymer is selected from the group consisting of ethers of cellulose and esters of cellulose; -
wherein the 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; and after 8 hours, from about 60-85% of the total active is released; and wherein the dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions. - View Dependent Claims (33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49)
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50. A dosage form comprising a plurality of active-containing particles comprising cyclobenzaprine hydrochloride and a dissolution rate controlling polymer surrounding the cyclobenzaprine hydrochloride;
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wherein the dissolution rate controlling polymer is selected from the group consisting of ethers of cellulose and esters of cellulose; wherein said dosage form comprises 30 mg of cyclobenzaprine hydrochloride and provides a maximum blood plasma concentration (Cmax) within the range of about 80% to 125% of about 20 ng/mL of cyclobenzaprine hydrochloride following oral administration of a single 30 mg cyclobenzaprine dose; and wherein said dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions. - View Dependent Claims (51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62)
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63. A dosage form comprising a plurality of active-containing particles comprising cyclobenzaprine hydrochloride and a dissolution rate controlling polymer, granulated together;
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wherein the dissolution rate controlling polymer is selected from the group consisting of ethers of cellulose and esters of cellulose; wherein said dosage form comprises 30 mg of cyclobenzaprine hydrochloride and provides a Tmax within the range of 80% to 125% of about 7 hours following oral administration of a single 30 mg cyclobenzaprine dose; and wherein said dosage form provides a therapeutically effective plasma concentration over a period of 24 hours to treat muscle spasm associated with painful musculoskeletal conditions. - View Dependent Claims (64, 65, 66, 67, 68, 69, 70, 71, 72, 73)
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Specification