Characteristics of drug substances in oily solutions. Drug release rate, partitioning and solubility

In Vitro Assessment of Lidocaine Release from Aqueous and Oil Solutions and from Preformed and in Situ Formed Aqueous and Oil Suspensions. Parenteral Depots for Intra-Articular Administration

“…This cosolvent therefore may be of potential interest in the design of in situ suspension forming drug delivery systems (Larsen et al 2003). The solubility of lidocaine in sesame oil was found to be of the same order of magnitude as that previously obtained in Viscoleo (1.05 M) and castor oil (1.74 M) (Larsen et al 2002). The solubility of lidocaine in sesame oil increased almost three-fold by addition of 20% (v/v) NMP.…”

IUPAC-NIST Solubility Data Series. 102. Solubility of Nonsteroidal Anti-inflammatory Drugs (NSAIDs) in Neat Organic Solvents and Organic Solvent Mixtures

“…The drug is administered as a racemic mixture; however, the (S)-enantiomer exhibits by far the higher anti-inflammatory activity, which is reported to be 30 times larger than the activity of the racemic mixture. 90 There are several published studies 60,65,83,84,91,92 involving the solubility of flurbiprofen in organic solvents. Most notably, Perlovich et al 84 measured the mole-fraction solubility of flurbiprofen dissolved in 22 different organic solvents, including four saturated hydrocarbons (pentane, hexane, heptane and octane), two aromatic hydrocarbons (benzene and methylbenzene), one alkyl alkanoate (ethyl ethanoate), one cyclic ether (1,4-dioxane), eight primary alcohols (methanol, ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, 1-heptanol, and 1-octanol), one alkanone (propanone), and one miscellaneous organic solvent (ethanenitrile) at 298 K and atmospheric pressure.…”

“…Most notably, Perlovich et al 84 measured the mole-fraction solubility of flurbiprofen dissolved in 22 different organic solvents, including four saturated hydrocarbons (pentane, hexane, heptane and octane), two aromatic hydrocarbons (benzene and methylbenzene), one alkyl alkanoate (ethyl ethanoate), one cyclic ether (1,4-dioxane), eight primary alcohols (methanol, ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-hexanol, 1-heptanol, and 1-octanol), one alkanone (propanone), and one miscellaneous organic solvent (ethanenitrile) at 298 K and atmospheric pressure. Larsen et al 92 determined the solubility of flurbiprofen in castor oil at 310 K, while Rytting et al 65 measured the solubility in polyethylene glycol 400 (PEG 400) at ambient room temperature.…”

“…Lejal et al 162 found that naproxen protected Madin-Darby canine cells against HqN1 and H3N2 viral strains, and that naproxen decreased the viral titers in mice lungs after intranasal viral infection. There have been several studies 64,65,92,111,117,[163][164][165][166][167][168][169][170] involving the solubility of naproxen in organic solvents. Perlovich et al 163 measured naproxen solubilities in hexane, benzene, methanol, ethanol, 1-propanol, 1-butanol, 1-pentanol, 1-heptanol, and 1-octanol at 298 K based on spectroscopic methods.…”

Lipid nanoparticles for the delivery of poorly water-soluble drugs

“…[8,9] Mixtures with comparatively polar lipid components, like medium chain triglycerides or diacetylated monoglycerides, are thus used in some commercial emulsion formulations ( Table 1). The use of nonglyceride oils may also be considered in order to overcome solubility limits as, for example, described for vitamin E derivatives (tocols) for the preparation of paclitaxel-containing emulsions.…”