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Tritiated Water (tritiated + water)
Selected AbstractsSynthesis of [3H]doxorubicin by isotope exchange with tritiated water,JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 5-6 2007Valerii P. Shevchenko [source] Preparation of tritium-labelled BIIL 260 of high specific radioactivityJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 3 2003V.P. Shevchenko Abstract Various approaches to the synthesis of tritium-labelled BIIL 260 with high specific radioactivity were investigated. Attempts to incorporate tritium directly into BIIL 260 were made by solid-phase isotope exchange with tritium gas and by isotope exchange with tritiated water which yielded a final product with specific activities ranging from 2 to 7 Ci/mmol. However, the solid-phase and liquid-phase dehalogenations of an appropriate synthon fragment of BIIL 260 followed by its subsequent conversion to the final product via chemical synthesis yielded the desired tritium-labelled BIIL 260 with specific activities of 25 or 71 Ci/mmol, depending upon the precursors and methods used in the dehalogenation step. Copyright © 2002 John Wiley & Sons, Ltd. [source] Synthesis of tritium labelled zaleplonJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 11 2002V.P. Shevchenko Abstract The reaction conditions for the incorporation of tritium into zaleplon have been investigated. The methods studied were the catalytic isotope exchange reaction with tritium gas and catalytic isotope exchange reaction with tritiated water. The results showed that the latter method was the method of choice giving a compound with a higher specific activity and a better yield. Copyright © 2002 John Wiley & Sons, Ltd. [source] Investigation of nail permeation enhancement by chemical modification using water as a probeJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 2 2002Gouri G. Malhotra Abstract Our objective was to screen molecules that could interact with keratin in the human nail and thereby improve the topical penetration of actives into and through the nail plate. We used specialized Franz-type diffusion cells for our permeation experiments and water as a marker molecule. Aqueous/hydroalcoholic gels containing the enhancers were spiked with tritiated water and compared with a control (without enhancer). We computed the normalized water flux (defined as a product of flux and nail thickness) for each gel. We defined an enhancement factor for water as the ratio of the normalized water flux from a gel containing enhancer to that of the control. Our results indicate that the chemical structure of the modifier is most important in determining its ability to enhance penetration. The best enhancement effect was obtained using N-(2-mercaptopropionyl) glycine, a mercaptan derivative of an amino acid, in combination with urea. The concentration of each chemical modifier was linearly related to normalized water flux and mercaptan levels were more important that urea levels in penetration enhancement. Barrier integrity of nails was compromised after treatment with effective chemical modifiers. Thus, we have developed a suitable technique to screen nail penetration enhancers using water as a probe. © 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:312,323, 2002 [source] |