Summary
An attempt was made to create a delayed release preparation of cytosine arabinoside (araC) which could be administered subcutaneously, and would produce plasma levels similar to steady state infusion concentrations. A thixotropic suspension of araC in arachis oil and aluminium distearate was formulated. This preparation was similar to that previously used with bleomycin oil suspension and procaine penicillin. Two hundred mg/ml of araC in arachis oil containing varying amounts of aluminium distearate were administered firstly to New Zealand White rabbits and then to patients with acute myelogenous leukaemia. This preparation was well tolerated by both rabbits and patients but did not delay the release of araC from the subcutaneous tissues.
Similar content being viewed by others
References
Skipper HE, Schabel FM, Wilcox WS: Experimental evaluation of potential anticancer agents XXI: scheduling of arabinosylcytosine to take advantage of its S-phase specificity against leukaemia cells. Cancer Chemother Rep 51:125–141, 1967
Bodey GP, Freireich EJ, Monto RW, Hewlett JS: Cytosine arabinoside (NSC-63878) therapy for acute leukaemia in adults. Cancer Chemother Rep (Pt I) 53(1):59–66, 1969
Southwest Oncology Group: Cytarabine for acute leukaemia in adults effect of schedule on therapeutic response. Arch Int Med 133:251–259, 1974
Slevin ML, Piall EM, Aherne GW, Johnston A, Sweatman MC, Lister TA: The pharmacokinetics of subcutaneouscytosine arabinoside in patients with acute myelogenousleukaemia. Brit J of Clin Pharmacol 12:507–510, 1981
Weinstein HJ, Griffin T, Cohen H, Propper RD, Sallan S: Pharmacology of cytosine arabinoside (a-c). Proc Am Assoc Cancer Res 19:157, 1978
Slevin ML, Piall EM, Aherne GW, Johnston A, Lister TA:Subcutaneous infusion of cytosine arabinoside, a practical alternative to intravenous infusion. Cancer Chemother Pharmacol 10:112–114, 1983
Ho DWH, Neil GL: Pharmacology of 5′-esters of 1-B-D-arabinofuranosylcytosine. Cancer Res 37:1640–1643, 1977
Ho DWH, Rodriguez V, Loo TL, Bodey GP, Feireich EJ: Clinical pharmacology of 2,2′-0-cyclocytidine. Clin Pharmacol Ther 17:66–72, 1975
Hoshi A, Kanzawa F, Kuretani K, Saneyoshi M, Arai Y: 2,2′-0-cyclocytidine, an antitumour cytidine analogue resistant to cytidine deaminase. Gann 62:145–146, 1971
Lokich JJ, Chawla PL, Jaffe N, Frei E: Phase I evaluation of cyclocytidine. Cancer Chemother Rep 59:389–393, 1975
Finklestein JZ, Higgins G, Krivit W, Hammond D: Evaluation of cyclocytidine in children with advanced acuteleukaemia and solid tumours. Cancer Treap Rep 63:1331–1333, 1979
Ikeda S: Local therapy with bleomycin oil suspension in dermatology. Med Treat 9:59–76, 1976
Kimura K, Niitani H, Sakai Y, Chikada C, Shimoyama M, Sakano T, Ibuka T, Minato K, Takenaka T, Sasaki S, Inoue T: Antitumour agents, their cytocidal acting mode and the way of their administration. Jap J Clin Med 33:1862–1872, 1975
Buchi VJ, Gunderson FO: Untersuchengen Über Einige Penicillin-Depotpraparate. Pharmaceutica Acta Helvetiae 23:290–301, 1948
Piall EM, Aherne GW, Marks VM: A radioimmuno assay for cytosine arabinoside. Brit J Cancer 40:548–545, 1979
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Slevin, M.L., Piall, E.M., Johnston, A. et al. The pharmacokinetics of subcutaneous bolus cytosine arabinoside in an arachis oil plus aluminium distearate suspension. Invest New Drugs 2, 271–276 (1984). https://doi.org/10.1007/BF00175376
Issue Date:
DOI: https://doi.org/10.1007/BF00175376