The tolerability of multiple oral doses of Pulsincap™ capsules in healthy volunteers

Oral pulsatile delivery: Rationale and chronopharmaceutical formulations

“…Impermeable Bar-Shalom et al, 2009;Binns et al, 1996;Gohel and Sumitra, 2002;Hebden et al, 1999;Krögel andBodmeier, 1998, 1999b;Lee et al, 2000;Mastiholimath et al, 2007;McConville et al, 2004McConville et al, , 2005McConville et al, , 2009Nayak et al, 2009;Ross et al, 2000;Stevens et al, 2002;Sutch et al, 2003;Wilding et al, 1992Semi-permeable Crison et al, 1996Löbenberg et al, 2005 (d) Release controlling plug:…”

“…Swellable Binns et al, 1996;Hebden et al, 1999;Stevens et al, 2002;Wilding et al, 1992 Swellable/erodible Bar-Shalom et al, 2009;Gohel and Sumitra, 2002;Krögel andBodmeier, 1998, 1999b;Lee et al, 2000;Mastiholimath et al, 2007;McConville et al, 2004McConville et al, , 2005McConville et al, , 2009Nayak et al, 2009;Ross et al, 2000;Sutch et al, 2003Hydrophobic Crison et al, 1996Löbenberg et al, 2005 (e) Optional immediate-release drug dose Crison et al, 1996;Löbenberg et al, 2005 in delaying the drug liberation (McConville et al, 2004). Moreover, notable differences were found in the performance of such erosion-based capsular systems when the impermeable EC film was applied by aqueous rather than organic spray-coating to the drug-containing body (Sutch et al, 2003;McConville et al, 2005).…”

“…This was composed of cross-linked PEG 8000 hydrogel in the original Pulsincap TM device, the suitability of which for time-controlled release was extensively assessed by human imaging investigations (Wilding et al, 1992;Hebden et al, 1999;Stevens et al, 2002). Although regulatory concerns were raised by the use of the hydrogel polymer, the tolerability and patient compliance of a four-week placebo treatment that involved multiple daily dosing were established (Binns et al, 1996). However, erodible hydrophilic polymers, such as HPMC of various viscosity grades, PVA, PEO, guar gum and sodium alginate, were later employed as alternative matrix-forming agents to prepare the release-controlling plug Ross et al, 2000;Gohel and Sumitra, 2002;Mastiholimath et al, 2007;Nayak et al, 2009;McConville et al, 2009).…”

A pharmacoscintigraphic study of three time-delayed capsule formulations in healthy male volunteers

“…The simultaneous use of two different isotopes has been shown to aid the detection of pulsed release from an oral dosage form 22. Indium‐111 ( 111 In) and technetium‐99m ( 99m Tc) have different photopeak energies and hence can be used to visualise two separate components of complex pulsed release dosage forms 23. Both radiopharmaceuticals have suitable half‐lives, high water solubility and form nonabsorbable chelates when complexed with diethylenetriaminepentaacetic acid (DTPA).…”

An inulin and doxorubicin conjugate for improving cancer therapy

“…Inulin is a naturally occurring polysaccharide in many plants such as onion, garlic, and chicory and consists of a mixture of oligomers and polymers containing 2 to 60 β, 2–1 linked D-fructose molecules (Figure 1) [13]. Inulin’s average degree of polymerization is 12 and its short length gives rise to unique properties including fat reduction, dietary fiber, and prebiotic effects on colonic microflora [14].…”