Trends in the Precipitation and Crystallization Behavior of Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs Assessed Using Synchrotron Radiation

The inhibiting role of hydroxypropylmethylcellulose acetate succinate on piperine crystallization to enhance its dissolution from its amorphous solid dispersion and permeability

“…The factors affecting the inhibition ability of polymer include drug-polymer interaction, steric hindrance of polymer, hydrophobicity and solution viscosity, etc. [31][32][33] HPMCAS has a better inhibition role than L100-55, which may be ascribed to steric hindrance of HPMCAS. HF is the most effective in the inhibition of crystallization of Pip, which may be attributed to the strong hydrophobic interactions between Pip and HF (HF is the most hydrophobic when compared to MF and HF due to its low carboxyl content).…”

Biopharmaceutic Profiling of Salts to Improve Absorption of Poorly Soluble Basic Drugs

“…There are some reports available regarding formulation strategies that can be applied to inhibit in vivo precipitation. [29][30][31][32][33] The cannabinoid receptor 1 antagonists AZD1175 and AZD2207 are highly lipophilic weak bases with low pH-dependent solubility and high intestinal permeability in the Caco-2 model ( Fig. 1 and Table 1).…”

Using Environment-Sensitive Fluorescent Probes to Characterize Liquid-Liquid Phase Separation in Supersaturated Solutions of Poorly Water Soluble Compounds

“…Recently, the concentration where LLPS is first observed to occur in aqueous solutions of high log P drugs has been linked to the solubility of a water-saturated supercooled liquid phase of the drug i.e., the Bamorphous solubility^. When LLPS occurs, a one phase supersaturated aqueous solution separates into two phases, one of which is initially a dispersed, nano-sized drug-rich phase, while the other is a continuous aqueous rich phase (14)(15)(16)(17). The solution remains supersaturated until crystallization occurs, even though a visible precipitate is present.…”

“…Model compounds (see Fig. 2) selected for this work belong to the dihydropyridine class and have been well characterized by our group in terms of their crystallization tendency and LLPS behavior (15,16,(26)(27)(28). LLPS onset concentrations as detected by fluorescence measurements were compared to those obtained using a UV extinction method, in addition to the theoretically estimated Bamorphous solubilityv alues.…”