Bioavailability using cold labels: studies on a novel antidiarrhoeal agent SC-27166
The use of simultaneous administration of a compound to an animal or man by two routes where one route is distinguished by a stable-isotope-labelled derivative has been described in a study of the absolute availability of procainamide in man (Strong et al., 1975; Dutcher et al., 1975). Generally the method has a number of advantages, not least being the necessity to take only one set of blood samples. Also, in the usual crossover study the assumption is made that the kinetics of drug absorption, distribution, metabolism and elimination remain unchanged between doses. However, problems associated with the technique of simultaneous administration could arise if a high circulating plasma concentration of the compound interferes with the absorption of an orally administered dose or if extensive biliary excretion of free drug should take place, thereby making a high percentage of the intravenously administered drug available for intestinal re-absorption.
KeywordsSimultaneous Administration Electron Impact Mass Spectrum Deuterated Analogue Electron Impact Spectrum Trapezoidal Area
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- Dajani, E. Z., Bianchi, R. G., Adelstein, G. W. and Yen, C. H. (1975). Studies on the biological properties of SC-27166, a novel antidiarrhoeal agent. Presented at The Philadelphia G.I. Research Forum, PhiladelphiaGoogle Scholar
- Dutcher, J. S., Strong, J. M., Lee, W.-K. and Atkinson, A. J. (1975). Proceedings of the Second International Conference on Stable Isotopes, Oak Brook, Illinois, USA, National Technical Information Service Document CONF-751027, p. 186Google Scholar
- Metzler, C. M. (1969). NONLIN, Technical Report No. 7292/69/7293/005, The Upjohn Co., KalamazooGoogle Scholar
- Strong, J. M., Dutcher, J. S., Lee, W.-K. and Atkinson, A. J. (1975). Clin. Pharmacol. Ther., 18, 613Google Scholar