Nakamura Kazuyo, Kokubun Hideya, Komatsu Toshiaki, Matoba Motohiro, Hoka Sumio, Yago Kazuo
Department of Pharmacy, Shizuoka General Hospital.
Gan To Kagaku Ryoho. 2007 Sep;34(9):1449-53.
Oxycodone is a useful analgesic for cancer patients in pain. However, its pharmacokinetics have not been sufficiently examined and there is a lack of information, with very few reports on pharmacokinetics concerning the absorption process in particular. With this in mind, we studied the pharmacokinetics of controlled-release oxycodone (Oxy contin). We measured its serum concentration in patients with cancer pain, and calculated parameters derived using the nonlinear least-squared method program (MULTI). In the result, pharmacokinetic parameters calculated at CL/F were: 45.6+/-22.0 L/hr (Mean+/-SD), Vd/F: 473.0+/-19 6.7 L, t(1/2): 7.2+/- 6.2 hr, kel: 0.103+/-0.034, kal: 1.082+/-0.604, Lag time: 0.9 9+/-0.40 hr. In addition, the serum oxycodone concentration hardly rose until 1 hour after and just before medication, whereupon a rapid increase was evident after 1 hour. The pharmacokinetics of controlled-release oxycodone in patients with cancer pain were clarified in this study. Especially during the absorption process, the lag time was calculated specifically at about 1 hour, making it approximately equal to MS contin.
羟考酮是一种对疼痛的癌症患者有效的镇痛药。然而，其药代动力学尚未得到充分研究，且缺乏相关信息，特别是关于吸收过程的药代动力学报道极少。考虑到这一点，我们研究了控释羟考酮（奥施康定）的药代动力学。我们测量了癌症疼痛患者的血清浓度，并使用非线性最小二乘法程序（MULTI）计算得出相关参数。结果显示，按CL/F计算的药代动力学参数为：45.6±22.0升/小时（平均值±标准差），Vd/F：473.0±196.7升，t(1/2)：7.2±6.2小时，kel：0.103±0.034，kal：1.082±0.604，滞后时间：0.99±0.40小时。此外，在用药后1小时及用药前血清羟考酮浓度几乎没有升高，而在1小时后明显快速上升。本研究阐明了癌症疼痛患者中控释羟考酮的药代动力学。特别是在吸收过程中，滞后时间经具体计算约为1小时，使其与美施康定大致相当。
