Summary
Bioavailability of capsule and tablet formulations of tolamolol were compared by measuring plasma concentration of tolamolol and reduction in maximum exercise heart rate over a period of twelve hours in eight healthy subjects in a two-way cross-over study. Tolamol was absorbed more rapidly from capsules than from tablets; this did not result in any significant difference in the reduction in maximum exercise heart rate between the two formulations. There was no significant difference between area under curve of reduction in exercise tachycardia and area under curve of plasma concentration of tolamolol for the two formulations. Reduction in maximum exercise heart rate was related to logarithm of plasma concentration of tolamolol between two and twelve hours after both formulations.
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Adam, K.R., Baird, J.R.C., Burges, R.A., Linnell, J.: The β-blocking potency and cardioselectivity of tolamolol and its isomers in rodents. Europ. J. Pharmacol.25, 170–175 (1974)
Augstein, J., Cox, D.A., Ham, A.L., Leeming, P.R., Snarey, M.: β-Adrenoreceptor blocking agents. 1. Cardioselective 1 — aryloxy — 3 — (aryloxyalkylamino) propan — 2 ols. J. Med. Chem.16, 1245–1251 (1973)
Briant, R.H., Dollery, C.T., Fenyvesi, T., George, C.F.: Assessment of selective beta-adrenoreceptor blockade in man. Brit. J. Pharmacol.49, 106–114 (1973)
Coltart, D.J., Shand, D.G.: Plasma propranolol levels in the quantitative assessment of beta-adrenergic blockade in man. Brit. med. J.1970 III, 731–735
Faulkner, J.K., Stopher, D.A., Walden, R., Singleton, W., Taylor, S.H.: Pharmacokinetic and pharmacological studies with tolamolol in man. Brit. J. clin. Pharmacol.2, 423–428 (1975)
Medical Research Council Annual Report, 1962–63. Statement on responsibility in investigations on human subjects. Brit. med. J.1964 II, 178–180
Ormrod, R.: Medical ethics. Brit. med. J.1968 II, 7–10
Singleton, W., Faulkner, J.K., Taylor, S.H.: The circulatory effects of tolamolol in man. In preparation.
Singleton, W., Davidson, C., Thadani, U., Taylor, S.H.: Tolamolol in hypertension. Brit. Heart J. (In press).
Stopher, D.A.: Thin layer chromatography-fluorimetric estimation of tolamolol in human plasma. J. Pharm. Pharmacol.27, 133–134 (1975)
Thadani, U., Singleton, W., Taylor, S.H.: Tolamolol in angina pectoris. Brit. Heart J. (In press).
Thadani, U., Davidson, C., Singleton, W., Taylor, S.H.: Comparative activity of beta-adrenoceptor antagonists in man. Brit. J. clin. Pharmacol. (in press)
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Faulkner, J.K., Stopher, D.A., Walden, R. et al. Bioavailability of tolamolol. Eur J Clin Pharmacol 9, 315–317 (1976). https://doi.org/10.1007/BF00561666
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DOI: https://doi.org/10.1007/BF00561666