Because of the need for resource-sparing assays of the solubility of new drug candidates, we sought to develop and validate a rapid method for determining the solubility of nonvolatile pharmaceutical solids in water. Vapor-phase osmometry was used to determine the concentration of drugs in saturated solutions prepared by a rapid ultrasound-mediated dissolution protocol. The osmolality of saturated solutions as measured by the vapor-phase osmometer is an excellent predictor of the solubility of pharmaceutical solids in water. Each osmolality measurement requires less than 10 µl of saturated solution and takes less than 2 min to complete. For small-molecule drugs with solubilities greater than 10 g/kg, osmometry may prove to be a rapid and accurate method for determining the water solubilities of drugs.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1177/108705719900400606 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Molecular motion of a nickel-bis(dithiolato) complex in solution.
J Phys Chem B
November 2007
Department of Chemistry, Saint Louis University, 3501 Laclede Avenue, St. Louis, Missouri 63103, USA.
The molecular motion of the planar bis(maleonitriledithiolato)nickel anion, Ni(mnt)(2)(-), has been studied as a function of temperature using electron spin resonance (ESR) in several polar solvents; they are ethyl alcohol, eugenol, dimethyl phthalate, tri-n-butyl phosphate, tris(2-ethyl-hexyl)phosphate, diglyme, and a dimethylformamide-chloroform mixed solvent. Calculated spectra in agreement with the experimental X-band spectra are obtained using axially symmetric reorientation when the long in-plane axis is the unique (parallel) axis of the rotational diffusion tensor with D parallel/D perpendicular = 3.0-4.
View Article and Find Full Text PDFRapid Solubility Determination Using Vapor-Phase Osmometry.
J Biomol Screen
January 1999
Department of Pharmaceutics, State University of New York at Buffalo, Buffalo, NY.
Because of the need for resource-sparing assays of the solubility of new drug candidates, we sought to develop and validate a rapid method for determining the solubility of nonvolatile pharmaceutical solids in water. Vapor-phase osmometry was used to determine the concentration of drugs in saturated solutions prepared by a rapid ultrasound-mediated dissolution protocol. The osmolality of saturated solutions as measured by the vapor-phase osmometer is an excellent predictor of the solubility of pharmaceutical solids in water.
View Article and Find Full Text PDFStandard nonionic emulsifiers are heterogeneous by nature. Their reported molecular weight is unreliable, especially when several lots of the product are used in a study. The number-average molecular weights of two nonionic emulsifiers, poloxamer 188 and polyoxyethylene (23) lauryl ether were determined by vapor-phase osmometry.
View Article and Find Full Text PDFThe C40 isopranol-containing glycerol ether residues which characterize the complex lipids of the extreme thermoacidophile Thermoplasma acidophilum were isolated and purified from the glycolipid and phospholipid fractions. The glycerol ether, as well as the acetate and methoxy derivatives were characterized by thin-layer, gel-permeation and gas-liquid chromatography, infrared, nuclear magnetic resonance and mass spectrometry and by vapor phase osmometry. The glycerol ethers are proposed to be unique fully saturated diglycerol tetraethers, primarily C86H172O6, Mr 1300, which contain two sn-2,3-glycerol residues bridged through ether linkages by two C40 isopranoid branched diols.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!