Timed, pulsatile release systems
First Claim
1. A multiparticulate drug delivery formulation comprising a first and a second population of timed, pulsatile release (TPR) beads, wherein at least one of the first and the second population of TPR beads comprises:
- i. a core particle comprising an active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof; and
ii. an outer lag-time coating comprising a water-insoluble polymer in combination with at least one enteric polymer,wherein;
the first population of TPR beads provides a lag time of at least about 3 hours before onset of drug release and the second population of TPR beads provides a lag time of at least about 6 hours before onset of drug release,when tested for dissolution using Apparatus 1 (Baskets@ 100 rpm) or 2 (Paddles @ 50 rpm) and a two-stage dissolution medium (first two hours in 700 mL of 0.1 N HCl and thereafter in 900 mL of phosphate buffer at pH 6.8).
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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 (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
25 Claims
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1. A multiparticulate drug delivery formulation comprising a first and a second population of timed, pulsatile release (TPR) beads, wherein at least one of the first and the second population of TPR beads comprises:
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i. a core particle comprising an active pharmaceutical ingredient or a pharmaceutically acceptable salt thereof; and ii. an outer lag-time coating comprising a water-insoluble polymer in combination with at least one enteric polymer, wherein; the first population of TPR beads provides a lag time of at least about 3 hours before onset of drug release and the second population of TPR beads provides a lag time of at least about 6 hours before onset of drug release, when tested for dissolution using Apparatus 1 (Baskets@ 100 rpm) or 2 (Paddles @ 50 rpm) and a two-stage dissolution medium (first two hours in 700 mL of 0.1 N HCl and thereafter in 900 mL of phosphate buffer at pH 6.8). - 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)
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Specification