Slevin M L, Piall E M, Johnston A, Levison D A, Aherne G W, Tree S B, Lister T A
Invest New Drugs. 1984;2(3):271-6. doi: 10.1007/BF00175376.
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.
曾尝试制备一种可皮下给药的阿糖胞苷(araC)缓释制剂,使其产生的血浆浓度类似于稳态输注浓度。配制了阿糖胞苷在花生油和二硬脂酸铝中的触变混悬液。该制剂类似于先前用于博来霉素油混悬液和普鲁卡因青霉素的制剂。首先将含有不同量二硬脂酸铝的花生油中200mg/ml的阿糖胞苷给予新西兰白兔,然后给予急性髓性白血病患者。该制剂在兔和患者中均耐受性良好,但并未延缓阿糖胞苷从皮下组织的释放。