PHARMACOKINETICS OF PRIMAQUINE IN MAN .1. STUDIES OF THE ABSOLUTE BIOAVAILABILITY AND EFFECTS OF DOSE SIZE
PHARMACOKINETICS OF PRIMAQUINE IN MAN .1. STUDIES OF THE ABSOLUTE BIOAVAILABILITY AND EFFECTS OF DOSE SIZE
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DOI：
10.1111/j.1365-2125.1985.tb02709.x
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发表时间：
1985-01-01
影响因子：
3.4
通讯作者：
BRECKENRIDGE, AM
中科院分区：
文献类型：
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作者：
MIHALY, GW;WARD, SA;BRECKENRIDGE, AM
5名健康志愿者分别单次口服伯氨喹15、30和45 mg，研究了伯氨喹的药代动力学。每个受试者都接受了静脉注射。示踪剂量[14C]-伯氨喹(7.5u.Ci)，同时口服45毫克。吸收或伯喹基本完全，平均绝对生物利用度为0.96.+-。0.08。伯氨喹和羧酸代谢物的消除半衰期、口服清除量和表观分布体积均不受剂量大小或给药途径的影响。伯喹的曲线下面积与剂量大小呈线性关系(r=0.99，P<0.01)。0.01)及其羧酸代谢产物(r=0.99，P.ltoreq.0.01)。伯喹和伯喹的羧酸代谢物的全血/血浆平均浓度比分别为0.81和0.84。伯喹是一种低清除化合物(CL=24.2.+-)。7.41/h)，广泛分布于体内组织(V[分布体积]=242.9.+-)。69.51)，并且不受广泛的首过代谢的影响。
The pharmacokinetics of primaquine [an antimalarial drug] were examined in 5 healthy volunteers who received single oral doses of 15, 30 and 45 mg of the drug, on separate occasions. Each subject received an i.v. tracer dose of [14C]-primaquine (7.5 .mu.Ci), simultaneously with the 45 mg oral dose. Absorption or primaquine was virtually complete with a mean absolute bioavailability of 0.96 .+-. 0.08. Elimination half-life, oral clearance and apparent volume of distribution for both primaquine and the carboxylic acid metabolite were unaffected by either dose size, or route of administration. The relationships between area under the curve and dose size were linear for both primaquine (r = 0.99, P .ltoreq. 0.01) and its carboxylic acid metabolite (r = 0.99, P .ltoreq. 0.01). The mean whole blood to plasma concentration ratio were determined for primaquine (0.81), and for the carboxylic acid metabolite of primaquine (0.84). Primaquine is a low clearance compound (CL = 24.2 .+-. 7.4 1/h), is extensively distributed into body tissues (V [volume of distribution] = 242.9 .+-. 69.51) and is not subject to extensive first pass metabolism.