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Pharmacokinetics of chlorambucil in man after administration of the free drug and its prednisolone ester (prednimustine, Leo 1031)

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Summary

The pharmacokinetics of chlorambucil has been investigated in a cross over study after oral administration of the free drug (10 mg) and its prednisolone ester (prednimustine, 100 mg). The bioavailability of chlorambucil was about five times lower when given as prednimustine as compared to administration of the free drug. The peak plasma concentration was about twice as high and it was obtained more rapidly when the free drug was given. No intact prednimustine could be detected in plasma.

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References

  1. Könyves I, Fex H, Högberg B (1973) Novel corticosteroid esters with alkylating properties. Antineoplastic Chemotherapy, Daikos GK (ed) Proc. 8th Int. Congress of Chemotherapy, 791–795

  2. Pedersen-Bjergaard J, Mørk Hansen M, Geisler CH, Nissen NI (1980) Clinical trial of Prednimustine, Leo-1031 (NSC-134087), in patients with non-Hodgkin lymphomata and chronic lymphocytic leukaemia previously treated with steroids and alkylating agents. Acta Med Scand 207: 215–220

    Google Scholar 

  3. Johnsson JE, Tropé C, Mattsson W, Grundsell H, Aspegren K, Könyves I (1979) Phase II study of Leo 1031 (Prednimustine) in advanced ovarian carcinoma. Cancer Treat Rep 63: 421–424

    Google Scholar 

  4. Mouridsen HT, Kristensen D, Halskov Nielsen J, Dombernowsky P (1980) Phase II trial of prednimustine, L-1031, (NSC-134087) in advanced breast cancer. Cancer 46: 253–255

    Google Scholar 

  5. Kirdani RY, Murphy GP, Sandberg AA (1978) Some metabolic aspects of a nitrogen mustard of prednisolone. Oncology 35: 47–53

    Google Scholar 

  6. Plym Forshell G, Mattsson W (1981) Plasma concentrations of parent drug and metabolites after oral administration of prednimustine to patients with malignant disease. Internal Research Report, AB Leo, UP J Leo 1031 Nr 2797

  7. Könyves I, Nordenskjöld B, Plym Forshell G, de Schryver A, Westerberg-Larsson H (1975) Preliminary clinical and absorption studies with prednimustine in patients with mammary carcinoma. Eur J Cancer 11: 841–844

    Google Scholar 

  8. Ehrsson H, Eksborg S, Wallin I, Mårde Y, Joansson B (1980) Determination of chlorambucil in plasma by GLC with selected-ion monitoring. J Pharm Sci 69: 710–712

    Google Scholar 

  9. Jakhammer T, Olsson A, Svensson L (1977) Mass fragmentographic determination of prednimustine and chlorambucil in plasma. Acta Pharm Suec 14: 485–496

    Google Scholar 

  10. Ehrsson H, Nilsson SO, Ehrnebo M, Wallin I, Wennersten G (1979) Effect of food on kinetics of 8-methoxsalen. Clin Pharmacol Ther 25 [2]: 167–171

    Google Scholar 

  11. Metzler CM (1969) NONLIN — a computer program for parameter estimation in nonlinear situations. The Upjohn Co., Technical Report No 7292/69/7292/005

  12. Lund B, Kampmann JP, Lindahl F, Mølholm Hansen J (1976) Pivampicillin and ampicillin in bile, portal and peripheral blood. Clin Pharmacol Ther 19: 587–591

    Google Scholar 

  13. Pütter J (1979) Extramicrosomal drug metabolism. Eur J Drug Metab Pharmacokin et 4: 1–7

    Google Scholar 

  14. Gunnarsson PO, Svensson L, Wennberg B (1980) Metabolism of prednimustine by plasma enzymes. Internal Research Report, AB Leo UPJ Leo 1031 Nr 2583

  15. Wilkinson R. Gunnarsson PO, Plym Forshell G, Renshaw J, Harrap KR (1978) The hydrolysis of prednimustine by enzymes from normal and tumour tissues. Characterization and treatment of human tumours. Maltoni C (ed). Excerpta Medica International Congress Series 420: 260–273

    Google Scholar 

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Ehrsson, H., Wallin, I., Nilsson, S.O. et al. Pharmacokinetics of chlorambucil in man after administration of the free drug and its prednisolone ester (prednimustine, Leo 1031). Eur J Clin Pharmacol 24, 251–253 (1983). https://doi.org/10.1007/BF00613827

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  • DOI: https://doi.org/10.1007/BF00613827

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