1,721,071 research outputs found

    Oral Colon Delivery: rationale and time-based drug design strategy

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    Increasing efforts have recently been spent onto the accomplishment of oral colon targeting. Indeed, this has been related to a number of local as well as systemic highly interesting applications, such as a more effective and tolerable therapy of inflammatory bowel disease (IBD), the pharmacological prevention of colorectal adenocarcinoma, and a possible improvement in the oral bioavailability of peptide and protein drugs. For the purpose of colon targeting, a variety of delivery technologies have been described, which rely on typical variation patterns shown by selected physiological parameters throughout the gastrointestinal tract. In particular, this article is focused on time-based formulation approaches that exploit the relative consistency in the small intestinal transit time (SITT) of dosage form

    Co-estrusione di una dispersione solida itraconazolo/Soluplus® ed eccipienti selezionati per favorire la disgregazione

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    Scopo del lavoro è valutare la possibilità di estrudere a caldo, in un unico processo, una dispersione solida costituita da un attivo poco solubile (itraconazolo) e un polimero idrofilo termoplastico (Soluplus®), con un composto in grado di favorire il processo di disgregazione. In un precedente studio si era infatti dimostrato che capsule di gelatina dura contenenti dispersioni solide (polveri ottenute per macinazione di prodotti di estrusione a caldo), a contatto con acqua, tendevano a formare una massa matriciale con ridotta velocità di liberazione dell’attivo. Il processo di co-estrusione della formulazione in toto qui proposto rappresenta un approccio innovativo alla produzione in continuo, fornendo al contempo buone potenzialità in termini di mixing dei componenti. Sono state prese in esame miscele contenenti il 20% (p/p) di croscarmellosa sodica, sodio bicarbonato come tale e tre diversi tipi di sistemi effervescenti. Prove preliminari di co-estrusione sono state effettuate su miscele di Soluplus® con ciascun eccipiente, per mettere a punto le condizioni di processo; in questa fase sono state evidenziate alcune criticità legate alle caratteristiche reologiche delle miscele, che contenevano materiali non termoplastici, e ad un certo grado di instabilità termica di alcuni fra gli eccipienti selezionati. Le formulazioni a base di croscarmellosa sodica e sodio bicarbonato, in particolare, si sono dimostrate adatte al tipo di lavorazione proposta; le capsule contenenti i corrispondenti prodotti di estrusione sono risultate caratterizzate da rapida disgregazione e da una pronta e completa dissoluzione dell’itraconazolo

    Retentive Drug Delivery Systems Based on Shape Memory Materials

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    Retentive drug delivery systems are intended for prolonged residence and release inside hollow organs of the body, in pursuit of either local or systemic therapeutic goals. Because of the relatively long-lasting period of time they could cover during operation, a primary advantage arising from their use would lie in reduced dosing frequency, thereby improving the overall adherence of patients to prescribed medication regimens. The treatment of numerous pathologies that affect the urinary bladder and the stomach could especially benefit from viability of such delivery technologies. Moreover, by making use of effective gastroretentive dosage forms, the bioavailability of drugs that are preferably absorbed from the upper gastrointestinal tract could be increased. Expansion of devices following administration is often exploited for retention purposes, and several formulation strategies have been proposed in this respect. Innovative applications of shape memory materials have also been explored, highlighting the great inherent potential for facing the challenges involved. (c) 2019 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019, 137, 48798

    Oral pulsatile delivery systems based on swellable hydrophilic polymers

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    Upon contact with aqueous fluids, swellable hydrophilic polymers undergo typical chain relaxation phenomena that coincide with a glassy-rubbery transition. In the rubbery phase, these polymers may be subject to swelling, dissolution and erosion processes or, alternatively, form an enduring gel barrier when cross-linked networks (hydrogels) are dealt with. Because of the peculiar hydration and biocompatibility properties, such materials are widely exploited in the pharmaceutical field, particularly as far as hydrophilic cellulose derivatives are concerned. In oral delivery, they have for long been employed in the manufacturing of prolonged release matrices and, more recently, for pulsatile (delayed) release devices as well. Pulsatile delivery, which is meant as the liberation of drugs following programmed lag phases, has drawn increasing interest especially in view of emerging chronotherapeutic approaches. In pursuit of pulsatile release, various design strategies have been proposed, chiefly including reservoir, capsular and osmotic formulations. In most cases, water-swellable polymers play a key role in the overall delivery mechanism after being activated by physiological media. Based on these premises, the aim of the present review is to survey the main oral pulsatile delivery systems, for which swelling, dissolution and/or erosion of hydrophilic polymers are primarily involved in the control of release
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