The novel oral controlled-release drug delivery system TIMERx is a pregranulated blend composed of synergistic heterodisperse polysaccharides (usually xanthan gum and locust bean gum) together with a saccharide component (generally dextrose). The technology is capable of delivery a wide range of drugs and is customized to accommodate a variety of physicochemical and pharmacokinetic properties and release profiles. The material has uniform packing characteristics over a range of different particle size distributions and is capable of processing into tablets using either direct compression, following addition of drug and lubricant, or conventional wet granulation. The synergism between the homo- and heteropolysaccharide components of the system enables formulation manipulation of different rate-controlling mechanisms. The ultimate rate of drug release is controlled by the rate of water penetration into the matrix. The technology is well protected with over 90 patents issued worldwide.
Drug release from tablets containing the polysaccharide system is capable of control using a variety of different formulations and process methods to provide a variety of release modalities that are capable of matrix-dimension independence. Control of drug release is achieved by manipulation of the synergistic interactions of the heterodisperse polysaccharides to regulate the rate of water penetration into the tablet and subsequent diffusion of the drug across the gel layer.
Showing posts with label Drug Delivery System. Show all posts
Showing posts with label Drug Delivery System. Show all posts
Oral Modified-Release Delivery Systems
The oral route of drug delivery is typically considered the preferred and most patient-convenient means of drug administration. Consequently, much effort is directed during drug discovery to identify orally active candidates that will provide reproducible and effective plasma concentrations in vivo. The reality is that many compounds are either incompletely or ineffectively absorbed after oral administration (i.e., bioavailability is an issue), or that the required dosing frequency is too short to enable once- or twice-daily administration (i.e., pharmacokinetic half-life is an issue). Lead optimization typically addresses such shortcomings
during a discovery program; however, in many cases it is not possible to identify an appropriate clinical candidate with the requisite “ideal” physicochemical and/or pharmacokinetic properties. For clinical research phase drug candidates, or drugs already marketed, the opportunity for enhancing their clinical pharmacology profile after oral administration through attainment of more optimal blood drug concentration-time profiles should always be considered.
Modified-release formulation technologies offer an effective means to optimize the bioavailability and resulting blood concentration-time profiles of drugs that otherwise suffer from such limitations. Within the context of this chapter, the term “modified release” refers to both delayed- and extended-release systems for oral administration as well as oral delivery systems designed specifically to modify the release of poorly water-soluble drugs. Also included are the fastdissolving dosage forms for which absorption occurs primarily (but not exclu-sively) in the gastrointestinal (GI) tract. The chapters in this part describe a broad range of pharmaceutical formulation technologies that address various limiting features associated with oral drug bioavailability and dosing frequency. In planning this part, we invited technology-focused chapters from expert contributors who had direct experience with the individual systems. Our goal was to select relatively advanced technologies representative of the various contemporary approaches being taken in the field—our success in this endeavor is a direct consequence of the willingness of the contributing authors who graciously accepted our invitation. As with all written compilations of this nature, time, commercial, and intellectual property restrictions on the part of potential contributors unfortunately precluded the description of some highly relevant and successful technologies.
during a discovery program; however, in many cases it is not possible to identify an appropriate clinical candidate with the requisite “ideal” physicochemical and/or pharmacokinetic properties. For clinical research phase drug candidates, or drugs already marketed, the opportunity for enhancing their clinical pharmacology profile after oral administration through attainment of more optimal blood drug concentration-time profiles should always be considered.
Modified-release formulation technologies offer an effective means to optimize the bioavailability and resulting blood concentration-time profiles of drugs that otherwise suffer from such limitations. Within the context of this chapter, the term “modified release” refers to both delayed- and extended-release systems for oral administration as well as oral delivery systems designed specifically to modify the release of poorly water-soluble drugs. Also included are the fastdissolving dosage forms for which absorption occurs primarily (but not exclu-sively) in the gastrointestinal (GI) tract. The chapters in this part describe a broad range of pharmaceutical formulation technologies that address various limiting features associated with oral drug bioavailability and dosing frequency. In planning this part, we invited technology-focused chapters from expert contributors who had direct experience with the individual systems. Our goal was to select relatively advanced technologies representative of the various contemporary approaches being taken in the field—our success in this endeavor is a direct consequence of the willingness of the contributing authors who graciously accepted our invitation. As with all written compilations of this nature, time, commercial, and intellectual property restrictions on the part of potential contributors unfortunately precluded the description of some highly relevant and successful technologies.
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