Search results for "solubility"
showing 10 items of 681 documents
Automated simultaneous triple dissolution profiles of two drugs, sulphamethoxazole-trimethoprim and hydrochlorothiazide-captopril in solid oral dosag…
2003
This article deals with the simultaneous determination of three dissolution profiles with the aid of the new and emerging continuous-flow methodology known as multicommutation. This methodology is based on a flow network of a set of solenoid valves controlled by the computer and acting as independent multicommutators to allow the easy and automated control of flowing solutions. The obtained three dissolution profiles from one dosage form are the whole formulation profile or "global profile" recommended by pharmacopoeias, and, at same time, are recorded two "individual" profiles from two drugs present in the formulation. This is the second attempt to obtain simultaneously three dissolution p…
Validation of Dissolution Testing with Biorelevant Media: An OrBiTo Study.
2017
Dissolution testing with biorelevant media has become widespread in the pharmaceutical industry as a means of better understanding how drugs and formulations behave in the gastrointestinal tract. Until now, however, there have been few attempts to gauge the reproducibility of results obtained with these methods. The aim of this study was to determine the interlaboratory reproducibility of biorelevant dissolution testing, using the paddle apparatus (USP 2). Thirteen industrial and three academic laboratories participated in this study. All laboratories were provided with standard protocols for running the tests: dissolution in FaSSGF to simulate release in the stomach, dissolution in a singl…
Harnessing medically relevant metals onto water-soluble subphthalocyanines: towards bimodal imaging and theranostics
2014
International audience; Subphthalocyanine (SubPc), a putative fluorophore for optical imaging (OI), was conjugated to chelating ligands (DOTA, DTPA) affording water-soluble conjugates complexed with (non-radioactive) metals relevant to the following medical imaging techniques/therapies: MRI (Gd), PET (Cu, Ga), SPECT (In, Ga, Lu), RIT (Cu, Lu, Y), and NCT (Gd). Magneto-optical properties of ditopic gadolinium species (and optical properties of other metal containing species) were examined (brightness (ε × Φ F) and relaxivity R 1) and fluorescence confocal/biphoton microscopy studies were conducted. † Electronic supplementary information (ESI) available: Experimental characterization, NMR and…
αα- and αβ-Zinc-meso-A2B2-tetraarylporphyrins with large optical responses to triethylamine
2012
Synthesis and separation of αα- and αβ-meso-A(2)B(2)-zinc(II) tetraarylporphyrin atropisomers with A = mesityl and B = ortho-phenylethynyl-phenyl are reported. Both isomers exhibit large optical responses upon axial NEt(3) coordination which are visible to the human eye and could therefore be beneficial for the design of smart amine sensing materials. The larger spectral changes as compared to Zn(TPP) are attributed to pronounced distortions of the porphyrin π-system due to steric interactions of the coordinating amine with the porphyrin periphery. This effect as well as the coordination site of NEt(3) at the αα-isomer have been studied by NMR experiments and were rationalized by DFT calcul…
About the relevance of anion-π interactions in water.
2021
Anion-π interactions are emerging as exotic features with potential applications in chemistry. In the last years, their relevance in living systems has been outlined, and so far there is no concluding significant evidence recognized about the participation of anion-π interactions in water because anion-π sensors contain large aromatic hydrophobic surfaces with limited solubility. By transforming a neutral heterocycle (for example quinoline) into its corresponding salt (quinolinium), we have been able to overcome these solubility issues, and new cationic water-soluble fluorophores have been prepared. Herein, we used N-alkylated heterocycles as π-acidic surfaces to shed light on the nature of…
Tetraurea calix[4]arenes with sulfur functions: synthesis, dimerization to capsules, and self-assembly on gold.
2007
Various calix[4]arene derivatives, fixed in the cone conformation by decylether groups and functionalized at their wide rim by urea residues, were synthesized. In two compounds (4f,g) sulfur functions were attached to the urea groups via different spacers in order to allow binding to metal surfaces. While they exist as single molecules in polar solvents, tetraurea calix[4]arenes of this type (4) combine to form dimeric capsules in aprotic, apolar solvents. A solvent molecule is usually included in such a capsule, if no guest with a higher affinity is present. In the presence of an equimolar amount of the tetratosylurea 5, the exclusive formation of heterodimers, consisting of one molecule o…
The significance of serum soluble IL-2 receptor as a marker for active visceral leishmaniasis in Sicilian patients
1992
SUMMARY Sera from nine Sicilian patients with confirmed visceral leishmaniasis (Leishmania donovani infantum; VL), at the moment of the diagnosis, during the course of the disease and after clinical recovery, were analysed for the concentration of soluble IL-2 receptor (sIL-2R). The results show that sIL-2R is a marker of disease activity, since it is in high concentration at the beginning of infection and returns to the normal range following successful chemotherapy. At the same time of serum analysis for sIL-2R, peripheral blood mononuclear cells (PBMC) of VL patients were stimulated with phytohaemagglutinin (PHA) or antigen and supernatant tested for IL-2 and interferon-gamma (IFN-γ) pro…
Physico-chemical state influences in vitro release profile of curcumin from pectin beads
2014
International audience; Curcumin is a polyphenolic compound with diverse effects interesting to develop health benefit products but its formulation in functional foods or in food supplement is hampered by its poor water solubility and susceptibility to alkaline conditions, light, oxidation and heat. Encapsulation of curcumin could be a mean to overcome these difficulties. In this paper, curcumin was encapsulated by ionotropic gelation method in low methoxyl pectin beads associated with different surfactants: Solutol®, Transcutol® and sodium caseinate. After encapsulation, physico-chemical properties of encapsulated curcumin such as its solubility, physical state, tautomeric forms and encaps…
Fortification of milk with calcium: effect on calcium bioavailability and interactions with iron and zinc.
2006
Calcium solubility, dialysability, and transport and uptake (retention + transport) by Caco-2 cells as indicators of calcium bioavailability have been estimated in the in vitro gastrointestinal digests of milk and calcium fortified milk. A significant linear correlation (p < 0.05) was obtained between calcium uptake and the amount of soluble calcium added to the cells, and also between percentage calcium uptake and the calcium measured in the analyzed samples. The solubility, dialysis, transport, and uptake values are higher (p < 0.05) for calcium fortified milks than for nonfortified milks; that is, calcium fortification increases not only calcium content but also its bioavailability. An i…
Influence of cryogenic grinding on properties of a self-emulsifying formulation
2003
Abstract Recently, self-emulsifying drug delivery systems (SEDDS) have been developed as a method to deliver lipophilic drugs. Gelucire® 44/14 is an excipient, from the lauroyl macrogolglycerides family, producing a fine oil-in-water emulsion when introduced into an aqueous phase under gentle agitation as SEDDS, improving thereby solubility of poorly water-soluble drugs and their bioavailability. The aims of this study were to process Gelucire® 44/14 into a powder by cryogenic grinding to produce solid oral dosage forms and to investigate influence of this process on different properties of a formulation made of Gelucire® 44/14 and ketoprofen (90/10). Cryogenic grinding produced Gelucire® 4…