PHARMACOKINETICS OF LIDOCAINE AND BUPIVACAINE AND STABLE ISOTOPE LABELED ANALOGS - A STUDY IN HEALTHY-VOLUNTEERS
PHARMACOKINETICS OF LIDOCAINE AND BUPIVACAINE AND STABLE ISOTOPE LABELED ANALOGS - A STUDY IN HEALTHY-VOLUNTEERS
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DOI：
10.1002/bod.2510090109
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发表时间：
1988-01-01
影响因子：
2.1
通讯作者：
BREIMER, DD
中科院分区：
文献类型：
--
作者：
BURM, AGL;DEBOER, AG;BREIMER, DD
研究了利多卡因和布比卡因及三氘甲基标记利多卡因和布比卡因在健康志愿者体内的药代动力学。氘标记和未标记形式的药物进行研究，同时注入10分钟。血浆浓度测定使用毛细管气相色谱法和质谱法相结合。血浆浓度-时间数据拟合双指数函数。平均分布和消除半衰期为8.4 ±。5.9 min和96 . ±.利多卡因组为9.2 ± 0.5min。7.0 min和98 . ±.氘标记利多卡因27分钟，15.3 ±。9.9 min和111 . ±.布比卡因组32 min，对照组15.2 ±. 10.9 min和109 . ±.氘标记的布比伐他汀分别为32 min。中央室的平均容积和平均稳态分布容积为：利多卡因37 ± 0.05。151和97 .+-. 201，氘标记利多卡因39。161和98 .+-. 181，布比卡因27。111和66 .+-. 231和氘标记的布比卡因28。121和65 .+-. 221、分别各自的平均血浆清除率为0.88 ± 0.99。0.181 min-1，0.87 ±。0.181 min-1，0.61 ±。0.151 min-1和0.62 ±-. 0.171 min-1。研究结果表明，氘代甲基的取代不会改变利多卡因和布比卡因在健康硫酸盐中的药代动力学。
The pharmacokinetics of lidocaine and bupivacaine and tri-deuteromethyl-labelled lidocaine and bupivacaine were investigated in healthy volunteers. The deuterium-labelled and the unlabelled form of the drug to be investigated were simultaneously infused in 10 min. Plasma concentrations were determined using a combination of capillary gas chromatography and mass fragmentography. Bi-exponential functions were fitted to the plasma concentration-time data. The mean distribution and elimination half-lives were 8.4 .+-. 5.9 min and 96 .+-. min for lidocaine, 9.2 .+-. 7.0 min and 98 .+-. 27 min for deuterium-labelled lidocaine, 15.3 .+-. 9.9 min and 111 .+-. 32 min forbupivacaine, and 15.2 .+-. 10.9 min and 109 .+-. 32 min for deuterium-labelled bupivarcaine, respectively. The mean volumes of the central compartment and mean steady state volumes of distribution were: lidocaine 37 .+-. 151 and 97 .+-. 201, deuterium-labelled lidocaine 39 .+-. 161 and 98 .+-. 181, bupivacaine 27 .+-. 111 and 66 .+-. 231 and deuterium-labelled bupivacaine 28 .+-. 121, and 65 .+-. 221, respectively. The respective mean plasma clearances were 0.88 .+-. 0.181 min-1, 0.87 .+-. 0.181 min-1, 0.61 .+-. 0.151 min-1, and 0.62 .+-. 0.171 min-1. The results of the study indicate that substitution of a deuterated methyl group does not alter the pharmacokinetics of lidocaine and bupivacaine in healthy sujects.