摘要
建立了反相HPLC测定血浆中阿糖腺苷的方法。研究和比较了阿糖腺苷溶液型注射剂和毫微囊型注射剂在家兔体内的药代动力学。毫微囊使阿糖腺苷在体液中维持较高的浓度和较长的时间。
A method to determine the concentration of Ara-a in plasma by reversed phase high performance liquid chromatography is established. The method offers the advantage of rapid andimple preparation of plasma samples and sampling volumes as small as 0. 5 ml. There is no need to ex-tract Ara-A (adenine arabinoside) or to remove or modify sugar inoities to obtain samples of adequateseparation. In pharmacokinetic studies, when amounts of clinical material are small and large numbersof assay are required, the present method is very useful. The calibration curve is linear for a widerange of concentration. The recovery is 87.5%. After a single dose of Ara-A-NC adenine arabinoside nanocapsules or Ara-A injection via intra-venous administration in rabbits, the Ara-A concentration in plasma was determined by this method.The pharmaceutical parameters of Ara-A-NC and Ara-A injections were obtained by using PKBP-N1program in NEC computer. The data obtained fitted an open two-compartment model well with twocorrelation coefficients more than 0. 99. In mice given Ara-A injection a shorter elimination half-time (20. 32 min), MRT (9. 647 min) and a smaller AUC (233. 4 μg·min·ml^(-1)) were obtained comparedwith the group given Ara-A-NC injection. For the latter, the figures were 67. 82 min, 156. 7 minand 309.9 μg·min·ml^(-1), respectively. It can be concluded that NC can alter the pharmacokinetic beh-avior of Ara-A in mice significantly and keep the drug at a higher level and for a longer time.
出处
《药学学报》
CAS
CSCD
北大核心
1992年第12期923-927,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金~~
关键词
阿糖腺苷
毫微囊
药代动力学
9--β--D--Arabinofuranosyl adenine
Nanocapsules
Pharmacokinetics
HPLC
