Review: Pharmacokinetics of illicit drugs in oral fluid

This article reviews studies that have measured drug concentrations in oral fluid following controlled dosing regimens. A total of 23 studies have been identified over the last 15 years. These show that the amphetamines including designer amphetamines, cocaine, cannabis and cocaine are quickly found in oral fluid following dosing and usually have similar time-courses to that in plasma. Following common doses peak oral fluid concentrations exceed 0.1 μg/mL and often even 1 μg/mL. The drug concentration will depend on whether a dilution step occurs with buffer as part of the sampling procedure. The uses of collectors that stimulate oral fluid usually reduce the drug concentration compared to a non-stimulated manner. This reduction will not disadvantage the recipient since it will potentially reduce the detectablity of drug in oral fluid compared to non-stimulated collections. Only one recent study has been reported for a benzodiazepine. This showed nanogram per milliliter concentrations for flunitrazepam. More studies are required for benzodiazepines and indeed for other drugs, particularly in multiple drug situations and where disease may affect the pharmacokinetics of drugs.     

2'-氯地西泮及其代谢物的药代动力学特征的LC/MS研究

目的利用液质联用法研究2’-氯地西泮及其代谢物在大鼠体内的药代动力学规律。方法SD大鼠经灌胃给药2’-氯地西泮2.625mg/kg,给药后采集不同时间的血样。蛋白沉淀法处理血浆样品后,进样分析。结果2’-氯地西泮及其代谢物在给药后1h均达到最高血药浓度。2’-氯地西泮在大鼠体内的半衰期约为93h,在给药后144h均能检测到。3种代谢产物地洛西泮、氯甲西泮、劳拉西泮在大鼠血浆的检出时限分别24h、144h、48h。结论2’-氯地西泮在大鼠体内吸收较快,半衰期较长,原体药物和代谢物在大鼠体内的检测窗口均较长。该研究可为临床救治2’-氯地西泮中毒患者以及相关案件的侦破提供一定的实验依据。     

高效液相色谱法测定桔梗多糖对桔梗皂苷D在大鼠体内药物代谢动力学参数的影响

目的 考察桔梗多糖(Platycodon grandiflorum polysaccharides,PGP)对桔梗皂苷D(platycod-in D,PD)在大鼠体内药物代谢动力学参数的影响,为桔梗的临床应用提供实验依据.方法 将24只SD大鼠随机分为PD组,PD+PGP低、中、高剂量组(PD-PGP-L、PD-PGP-M、PD-PGP-H组),灌胃给药后在各时间点眼眦取血,采用高效液相色谱法测定给药后PD的血药浓度变化,由DAS 2.1软件拟合药物代谢动力学参数.结果 与PD组比较,各PD-PGP实验组均显著缩短PD的达峰时间(P<0.05),并显著提高峰浓度(P<0.05)以及药时曲线下面积(P<0.05).结论 PGP能够显著改变PD口服后的药物代谢动力学参数.