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目的：观察中国健康志愿者对乙氧苯柳胺软膏的临床耐受性和单次给药的药代动力学过程．方法：２２名健康志愿者，分别单次外用乙氧苯柳胺软膏（２．５％，５％，１０％，１５％）各０．２５ｇ，进行人体耐受性试验；８名健康试验者，分别涂乙氧苯柳胺软膏４ｇ（１５％）４ｃｍ × ４ｃｍ，采用高效液相电化学检测器，检测血药浓度，进行药代动力学研究．结果：人体耐受性试验结果表明，四组志愿者均无明显的皮肤反应，也无异常的自觉症状；乙氧苯柳胺的血药浓度时间曲线符合一级吸收的一房室模型，其主要药代动力学参数为： ｔ１／２ｋａ ０.６６ ± ０．１９ｈ， ｔ１／２ｋｅ４．９４±１．０９ｈ，ｔｐｅａｋ２．１４±０．２７ｈ，Ｃｍａｘ２１．１±３．３μｇ·Ｌ－１，ＡＵＣ２１６±３１μｇ·Ｌ－１·ｈ－１。结论：人体对乙氧苯柳胺软膏具有良好的耐受性。
OBJECTIVE: To observe the clinical tolerability and the pharmacokinetics of phenoxybenzamide ointment in Chinese healthy volunteers. Methods: Twenty-two healthy volunteers were given a single oral topical 0.25% (0.5%, 5%, 10%, 15%) of phenylephrine ointment respectively for human tolerance test. Eight healthy volunteers , Respectively, 4 g of phenylephrine ointment (15%) 4cm × 4cm, using high performance liquid electrochemical detector, the detection of plasma concentration for pharmacokinetic studies. Results: The results of human tolerance test showed that there was no obvious skin reaction and no abnormal symptoms in the four groups of volunteers. The time curve of the concentration of the phenylephideamide conformed to the one-compartment model of first-order absorption. The main pharmacokinetic parameters were: t1 / 2ka 0.66 ± 0.19h, t1 / 2ke4.94 ± 1.09h, tpeak2.14 ± 0.27h, Cmax21.1 ± 3.3μg · L-1, AUC216 ± 31 μg · L-1 · h-1. Conclusion: The body has good tolerance to phenylamine dipyridamole ointment.