To enhance solubility a drug inclusion complex with cyclodextrin was developed using a spray-drying process. The powder complex characterized using DSC, XRPD, FT-IR, and (1)H NMR techniques confirmed interaction of cyclodextrin
with the CA indicating formation BLZ945 of a true complex wherein the drug is encapsulated in the cyclodextrin cavity. The saturation solubility and dissolution kinetics of drug complex evaluated in a discriminating medium showed significantly higher solubility and faster dissolution as compared to a physical mixture or powder blend comprising of drug and cyclodextrin. Pharmacokinetic (PK) studies in Wistar rats indicated a significant increase in the rate and extent of absorption for the drug complex as compared to a nanoparticulate dispersion that was used as the positive control. selleck chemicals llc Pharmacological activity following peroral administration of drug
complex in athymic nude mice with implanted tumors revealed that the tumor inhibition activity was equivalent to commercially available intravenous (IV) formulation with comparable safety profile. These studies demonstrated for the first instance feasibility of developing a safe and efficacious peroral formulation for a sparingly soluble camptothecin analog that may provide another viable, patient compliant, and cost effective option for the treatment of solid tumors.”
“A copolymer (2,4-DHBPOF) GDC-0973 concentration synthesized by the condensation of 2,4-dihydroxybenzophenone and oxamide with formaldehyde in the presence of acid catalyst with varying the molar proportions of the reacting monomer. Composition of the copolymer has been determined by elemental analysis. The copolymer has been characterized by UV-visible, FTIR, and H-1 NMR spectroscopy. The morphology of synthesized copolymer was studied by scanning electron microscopy (SEM). The activation energy
(E-a) and thermal stability calculated by using Sharp-Wentworth, Freeman-Carroll, and Freidman’s method. Thermogravimetric analysis (TGA) data were analyzed to estimate the characteristic thermal parameters. Freeman-Carroll and Sharp Wentworth methods have been used to calculate activation energy and thermal stability. The activation energy (E-a) calculated by using the Sharp-Wentworth has been found to be in good agreement with that calculated by Freeman-Carroll method. Thermodynamic parameters such as free energy change (Delta F), entropy change (Delta S), apparent entropy change (S*), and frequency factor (Z) have also been evaluated based on the data of Freeman-Carroll method. (C) 2011 Wiley Periodicals, Inc. J Appl Polym Sci 122: 2181-2188, 2011″
“Poorly water-soluble drugs such as cefpodoxime proxetil (400 mu g/ml) offer a challenging problem in drug formulation as poor solubility is generally associated with poor dissolution characteristics and thus poor oral bioavailability.