Timed, pulsatile release systems
First Claim
1. A solid oral multiparticulate drug delivery formulation comprising one or more populations of timed, pulsatile release (TPR) beads of one or more slightly acidic drug or a pharmaceutically acceptable salt thereof, wherein the timed, pulsatile release bead comprises:
- i. a core particle comprising a slightly acidic drug or a pharmaceutically acceptable salt thereof;
ii. an optional inner barrier coating comprising a water insoluble polymer that is optionally in combination with a water-soluble/pore-forming polymer;
iii. an outer lag-time coating comprising a water-insoluble polymer in combination with an enteric polymer;
wherein at least one population of timed, pulsatile release beads provides a lag time of at least 6 hours before onset of drug release; and
wherein the total amount of slightly acidic drug contained in the drug delivery formulation is sufficient and the resulting plasma concentration time profile is suitable for once- or twice-daily dosing regimens.
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Accused Products
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 (pharmocokinetics) 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.
263 Citations
27 Claims
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1. A solid oral multiparticulate drug delivery formulation comprising one or more populations of timed, pulsatile release (TPR) beads of one or more slightly acidic drug or a pharmaceutically acceptable salt thereof, wherein the timed, pulsatile release bead comprises:
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i. a core particle comprising a slightly acidic drug or a pharmaceutically acceptable salt thereof; ii. an optional inner barrier coating comprising a water insoluble polymer that is optionally in combination with a water-soluble/pore-forming polymer; iii. an outer lag-time coating comprising a water-insoluble polymer in combination with an enteric polymer; wherein at least one population of timed, pulsatile release beads provides a lag time of at least 6 hours before onset of drug release; and wherein the total amount of slightly acidic drug contained in the drug delivery formulation is sufficient and the resulting plasma concentration time profile is suitable for once- or twice-daily dosing regimens. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27)
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Specification