Cook C E, Brine D R, Jeffcoat A R, Hill J M, Wall M E, Perez-Reyes M, Di Guiseppi S R
Clin Pharmacol Ther. 1982 May;31(5):625-34. doi: 10.1038/clpt.1982.87.
[3H]-Phencyclidine (PCP) hydrochloride was given in intravenous (0.1 or 1 mg) or oral (1 mg) doses to male subjects. After 1 mg IV, drug and metabolites were recovered in urine (72.8 +/- 4.0% of dose), feces (4.7 +/- 0.9%), and perspiration. Fecal excretion was low (3.4 +/- 0.4%) after oral dosing and oral bioavailability was estimated at 72%. PCP comprised 16% of urinary radioactivity with 31% consisting of enzymatically hydrolyzable conjugates of hydroxylated metabolites. Both cis and trans isomers of 4-phenyl-4-(1-piperidinyl)cyclohexanol were found. Maximum average plasma PCP concentrations of 2.7 to 2.9 ng/ml were observed after oral and intravenous 1-mg doses. Blood/plasma ratios were approximately 1.0 and plasma binding was about 65%. Parent drug was found in saliva. Apparent terminal phase half-lifes averaged 21 +/- 3 hr (harmonic mean 17 hr, range 7 to 46 hr). The volume of distribution averaged 6.2 +/- 0.3 l/kg. Renal clearances were variable, but the average was 9% of the total clearance. Thus, PCP is cleared principally by metabolism.
给男性受试者静脉注射（0.1或1毫克）或口服（1毫克）盐酸[3H]-苯环己哌啶（PCP）。静脉注射1毫克后，药物及其代谢产物在尿液（占剂量的72.8±4.0%）、粪便（4.7±0.9%）和汗液中被回收。口服给药后粪便排泄量较低（3.4±0.4%），口服生物利用度估计为72%。PCP占尿液放射性的16%，其中31%为由羟基化代谢产物的酶促水解共轭物组成。发现了4-苯基-4-（1-哌啶基）环己醇的顺式和反式异构体。口服和静脉注射1毫克剂量后，观察到平均血浆PCP最高浓度为2.7至2.9纳克/毫升。血/浆比约为1.0，血浆结合率约为65%。在唾液中发现了母体药物。表观终末相半衰期平均为21±3小时（调和均值17小时，范围7至46小时）。分布容积平均为6.2±0.3升/千克。肾脏清除率各不相同，但平均值为总清除率的9%。因此，PCP主要通过代谢清除。
