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Review

Oral pulsatile drug delivery systems

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Pages 855-871 | Published online: 16 Sep 2005

Bibliography

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  • •These authors describe the preparation and in vitro performances of a multiparticulate delivery system in pellets for pulsatile release, in which osmotic agents are exploited to induce mechanical disruption of the outer release-controlling film.
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  • •This work describes the first experiments reported in the literature on spray-coating based on high-viscosity HPMC aimed at the attainment of swellable/erodible delayed-release systems.
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  • •This paper points out the benefits, in terms of both process feasibility and in vitro/ in vivo performances, provided by low-viscosity HPMC employed as an aqueous spray-coating agent for the preparation of swellable/erodible pulsatile release systems.
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  • •An alternative technique, such as tangential spray-coating in rotary fluid bed, is explored for the application of swellable/erodible release-delaying coats onto solid dosage forms
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  • •This paper deals with the Time-Clock® technology, which envisages the unique utilisation of natural waxes and surfactant hydrophobic blends as the release-controlling material for the preparation of a single-unit pulsatile release system. Such a device has shown to correctly perform in vivo on humans as well.
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  • •In this paper, the SRS is introduced. This multiparticulate device relies on a peculiar working mechanism consisting in the permeability increase of an outer acrylic film brought about by its interaction with an organic acid contained in the inner layers.
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  • •This paper describes the in vivo performances of SRS in beagle dogs.
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  • •In this article, the design and in vivo behaviour of PulsincapTm are dealt with. The system represents the first capsular delivery system for time-controlled release.
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  • •In this paper, the tolerability related to repeated administrations of placebo PulsincapTm is assessed on volunteers over a 28-day period.
  • WILSON CG, BAKHSHAEE M, STEVENS HN et al.: Evaluation of a gastro-resistant pulsed release delivery system (PulsincapTm) in humans. Drug Del. (1997) 4(3):201–206.
  • HEBDEN JM, WILSON CG, SPILLER RC et al: Regional differences in quinine absorption from the undisturbed human colon assessed using a timed release delivery system. Pharm. Res. (1999) 16(7):1087–1092.
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  • STEVENS HNE, WILSON CG, WELLING PG et al: Evaluation of PulsincapTm to provide regional delivery of dofetilide to the human GI tract. Int. J. Pharm. (2002) 236(1-2):27–34.
  • ROSS AC, MACRAE RJ, WALTHER M, STEVENS HNE: Chronopharmaceutical drug delivery from a pulsatile capsule device based on programmable erosion. ./. Pharm. Pharmacol (2000) 52(8):903–909.
  • MCCONVILLE JT, ROSS AC, CHAMBERS AR et al: The effect of wet granulation on the erosion behaviour of an HPMC-lactose tablet, used as a rate-controlling component in a pulsatile drug delivery capsule formulation. Eur. Pharm. Biopharm. (2004) 57(3):541–549.
  • SUTCH JCD, ROSS AC, KOCKENBERGER W et al: Investigating the coating-dependent release mechanism of a pulsatile capsule using NMR microscopy. J. Control. Release (2003) 92(3):341–347.
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  • CRISON JR, SIERSMA PR, TAYLOR MD, ON GL: Programmable oral release technology, Port Systems®: a novel dosage form for time and site specific oral drug delivery. Proceedings of the 22nd International Symposium on Controlled Release of Bioactive Materials. Seattle, WA, USA (1995): 1126.
  • •The design and in vivo behaviour of the PORT system are dealt with in this work. Compared with other capsular devices, this system is based on the time-dependent expulsion of a lipid plug following osmotically-induced water influx into the body.
  • CRISON JR, SIERSMA PR, ON GL: A novel programmable oral release technology for delivering drugs: human feasibility testing using gamma scintigraphy. Proceedings of the 23rd International Symposium on Controlled Release of Bioactive Materials. Kyoto, Japan (1996): 128.
  • •This paper also details the design and in vivo behaviour of the PORT system.
  • LEE WW, O'MAHONY B, BAR-SHALOM D et al: Scintigraphic characterisation of a novel injection-moulded dosage form. Proceedings of the 27th International Symposium on Controlled Release of Bioactive Materials. Paris, France (2000) 8446.
  • •In this paper, the Egalet® technology is proposed in its Burst-Egalet® configuration for pulsatile release. The system envisages an alternative design comprising a cylindrical impermeable outer shell, an inner drug core and two swellable release-controlling plugs sealing each open end.
  • MAHONY B, KOBERLE M, WILSON CG et al: Scintigraphic assessment of a system (Egalet®) for pulsatile peptide delivery in marl. Proceedings of the 28th International Symposium on Controlled Release of Bioactive Materials. San Diego, CA, USA (2001): 6187.
  • •This work also discusses the Egalet® technology proposition in its Burst-Egalet® configuration for pulsatile release.
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  • •This research points out that the release of verapamil hydrochloride from an osmotic once-daily COER-24 formulation can occur over a period of several hours after a 4–5 h delay, thus ideally meeting ischaemic heart disease chronotherapeutic needs. The interest in the above article is augmented by the fact that Covera-HS®, a well-known anti-hypertensive medicinal product available on the US market, is merely based on COER-24 technology.
  • GLASSER SP: Circadian variations and chronotherapeutic implications for cardiovascular management: a focus on COER verapamil. Heart Dis. (1999) 1(4):226–232.
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