Bioavailability of a Poorly Water-Soluble Drug from Tablet and Solid Dispersion in Humans

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

“…The human bioavailability of the poorly soluble REV5901 from a solid dispersion in Gelucire 44/14 under a fasting regimen was much higher than that of a tablet formulation even though the micronized form of drug and a wetting agent were used in the tablet. 83 The bioavailability of ubidecarenone in dogs from solid dispersion in Gelucire 44/14 and the Gelucire 44/14-lecithin mixture were, respectively, two and three times higher than that of commercially available tablet. 63 The bioavailability of another poorly water-soluble drug, RP69698, in dogs was 4.5 times higher (27.6% versus 6%) from its solid dispersion in a PEG 3350-Labrasol-polysorbate 80 system than from an aqueous suspension in 0.5% methylcellulose.…”

Oral formulation of a novel antiviral agent, PG301029, in a mixture of Gelucire 44/14 and DMA (2∶1, wt/wt)

“…It enhances bioavailability of a poorly water soluble drug because it forms a very fine emulsion, improves the wettability of the drug, and increases the solubility of the drug when it contacts with gastrointestinal (GI) fluid at 37°C. [12][13][14][15][16] The mechanism for Gelucire 44/14 to improve the bioavailability of a poorly water soluble drug is related to its ability to act as a dispersing or emulsifying agent for the liberated drug. 17 This study proposes a PG301029 oral formulation produced by dissolving the drug into a vehicle of Gelucire 44/14 and DMA in a ratio of 2:1.…”

Solubility of Pharmaceutical Solids

“…Pharmaceutical applications of solid dispersions have become increasingly important over the last few decades in helping to overcome delivery challenges of poorly water soluble drugs (Chiou and Riegelman, 1971;Sheen et al, 1991;Serajuddin, 1999;Khoo et al, 2000;van Laarhoven et al, 2002;Verreck et al, 2004). The ideal type of solid dispersion for increasing dissolution is a glassy solution, in which the drug in the amorphous form has a lower thermodynamic barrier to dissolution and a maximally reduced particle size (Goldberg et al, 1965).…”