Gastrointestinal fluid is a complex milieu and it is recognised that gut drug solubility is different to that observed in simple aqueous buffers. Simulated gastrointestinal media have been developed covering fasted and fed states to facilitate in vitro prediction of gut solubility and product dissolution. However, the combination of bile salts, phospholipids, fatty acids and proteins in an aque...

Reductive alkylation of three graphite starting materials G(flake), G(powder), and G(spherical) reveals pronounced differences in the obtained covalently functionalized graphene with respect to the degree of functionalization, exfoliation efficiency and product homogeneity, as demonstrated by statistical Raman microscopy (SRM), TGA/MS, IR-spectroscopy and solubility behavior.

Hydrotrifluoromethylation, vinylic trifluoromethylation, and iodotrifluoromethylation of simple alkenes have been achieved by using Togni reagent in the absence of any transition metal catalyst. These reactions were readily controllable by selection of appropriate salts and solvents. The addition of K2CO3 afforded the hydrotrifluoromethylation product, with DMF acting not only as a solvent, but...

Purpose: The aim of this research was to formulate and develop an orally disintegrating tablet (ODT) that incorporated a MEL/β-CD complex, using a quality by design (QbD) approach to enhance solubility and drug release. Methods: Multiple regression linear analysis was conducted to develop the kneading process and ODT formulation. Mixing time and amount of solvent were used as independent variab...

Literature data pertaining to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate-release (IR) solid oral dosage forms containing efavirenz as the only active pharmaceutical ingredient (API) are reviewed. Because of lack of conclusive data about efavirenz's permeability and its failure to comply with the "high solubility" criteria according to the Biop...

The specific aim of this study was to prepare sustained release matrix tablets containing indapamide as a low dose and low water solubility model drug. The matrix formers were composed of blends of hydroxypropyl methylcellulose as a swellable polymer and methyl cellulose as an erodible polymer. The matrix tablets were prepared by the direct compression technique and they have shown robust and a...

To develop methodology to predict the potential druggability of middle molecules, we examined structure, solubility, and permeability relationships a diverse library (HKDL ver.1) consisting 510 molecules (359 natural product derivatives, 76 non-natural products, 46 29 derivatives). The included peptides, depsipeptides, macrolides, lignans, 476 compounds had molecular weight in range 500–2000 Da...