A review of drug solubility in human intestinal fluids: Implications for the prediction of oral absorption

Dissolution behavior of co-amorphous amino acid-indomethacin mixtures: The ability of amino acids to stabilize the supersaturated state of indomethacin

“…To overcome this challenge, fluids that simulate gastric or intestinal fluids, and are easy to prepare in the laboratory, have been introduced [5,6]. These include for example fasted state simulated intestinal fluid (FaSSIF) and fed state simulated intestinal fluid (FeSSIF) which have been found to predict drug solubility in actual human intestinal fluid with sufficient accuracy in the early stages of drug development [6].…”

Increasing the biorelevance of simulated intestinal fluids for better predictions of drug equilibrium solubility in the fasted upper small intestine

“…Estimated degradation half-life is 1.44h. Interestingly, solubility of cinnarizine has been previously reported to be 32.011.8 μg/ml and 47.317.4 μg/ml in HIFs and FaSSIF, respectively [16]. After reaching equilibrium in plain phosphate and plain maleate buffers filtrates were incubated at 37 °C for 48h at which time their cinnarizine content was measured to be zero.…”

Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

“…It is also known that different drugs interact uniquely with physiological surfactants, depending on the physicochemical properties of both entities. Physiological surfactants in the GI tract, act to incorporate lipophilic compounds into mixed micelles consisting of bile salts and phospholipids (Augustijns et al, 2014). This effect generally results in enhanced solubility of poorly soluble drugs.…”

“…Modern drug discovery programs are often based on combinatorial chemistry and high-throughput screening, and a majority of the new drug candidates are suffering from poor water solubility (Augustijns et al, 2014). It is recognized that up to 90 % of the new chemical entities are classified as Class II and IV in the Biopharmaceutics Classification System (BCS) (Sjogren et al, 2013).…”