Timed, pulsatile release systems
First Claim
1. A pharmaceutical composition comprising one or more populations of timed, pulsatile release beads, wherein at least one population of time-pulsatile release beads comprises:
- a) a core particle comprising a basic active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof;
b) an inner barrier coating comprising a water-insoluble polymer that is optionally in combination with a water-soluble/pore-forming polymer; and
c) an outer lag-time coating comprising a water-insoluble polymer in combination with an enteric polymer;
wherein the population of timed, pulsatile release beads provides a lag time greater than 6 hours before onset of drug release.
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Abstract
A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described. The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating. Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics. The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications.
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Citations
43 Claims
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1. A pharmaceutical composition comprising one or more populations of timed, pulsatile release beads, wherein at least one population of time-pulsatile release beads comprises:
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a) a core particle comprising a basic active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof; b) an inner barrier coating comprising a water-insoluble polymer that is optionally in combination with a water-soluble/pore-forming polymer; and c) an outer lag-time coating comprising a water-insoluble polymer in combination with an enteric polymer; wherein the population of timed, pulsatile release beads provides a lag time greater than 6 hours before onset of drug release. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41)
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13. A method for the preparation of a pharmaceutical composition, the method comprising:
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a) preparing immediate release beads comprising a basic active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof; b) optionally applying an inner barrier coating on said immediate release beads, said inner barrier coating comprising a water-insoluble polymer that is optionally in combination with a water-soluble/pore-forming polymer; and c) applying an outer lag-time coating comprising a water-insoluble polymer in combination with an enteric polymer onto inner barrier coated beads of step b) or onto said immediate release beads of step a) to form a population of timed, pulsatile release beads; and d) combining one or more populations of timed, pulsatile release beads and immediate release beads in the form of a capsule or a tablet. - View Dependent Claims (42, 43)
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Specification