Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats,Journal of Natural Products

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Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats
Journal of Natural Products ( IF 3.3 ) Pub Date : 2021-02-23 , DOI: 10.1021/acs.jnatprod.0c01163
Shyam H Kamble _{1,

2} , Erin C Berthold ₁ , Tamara I King ₁ , Siva Rama Raju Kanumuri _{1,

2} , Raluca Popa ₁ , Julius R Herting ₁ , Francisco León ₃ , Abhisheak Sharma _{1,

2} , Lance R McMahon ₄ , Bonnie A Avery _{1,

2} , Christopher R McCurdy _{1,

2,

3}

Affiliation

Kratom, Mitragyna speciosa Korth., is being widely consumed in the United States for pain management and the reduction of opioid withdrawal symptoms. The central nervous system (CNS) active alkaloids of kratom, including mitragynine, 7-hydroxymitragynine, and numerous additional compounds, are believed to derive their effects through opioid receptor activity. There is no literature describing the systemic exposure of many of these alkaloids after the consumption of kratom. Therefore, we have developed and validated a bioanalytical method for the simultaneous quantitation of 11 kratom alkaloids (mitragynine, 7-hydroxymitragynine, corynantheidine, speciogynine, speciociliatine, paynantheine, corynoxine, corynoxine-B, mitraphylline, ajmalicine, and isospeciofoline) in rat plasma. The validated method was used to analyze oral pharmacokinetic study samples of lyophilized kratom tea (LKT) and a marketed product, OPMS liquid shot, in rats. Among the 11 alkaloids, only mitragynine, 7-hydroxymitragynine, speciociliatine, and corynantheidine showed systemic exposure 8 h postdose, and the dose-normalized systemic exposure of these four alkaloids was higher (1.6–2.4-fold) following the administration of the commercial OPMS liquid. Paynantheine and speciogynine levels were quantifiable up to 1 h postdose, whereas none of the other alkaloids were detected. In summary, the method was successfully applied to quantify the exposure of individual kratom alkaloids after an oral dose of traditional or commercial products. This information will contribute to understanding the role of each alkaloid in the overall pharmacology of kratom and elucidating the pharmacokinetic differences between traditional and commercial kratom products.

中文翻译：

大鼠口服传统或商业 Kratom 产品后 11 种 Kratom 生物碱的药代动力学

Kratom, Mitragyna speciosaKorth.，在美国被广泛用于疼痛管理和减少阿片类药物戒断症状。kratom 的中枢神经系统 (CNS) 活性生物碱，包括 mitragynine、7-hydroxymitragynine 和许多其他化合物，被认为是通过阿片受体活性获得它们的作用。没有文献描述食用 kratom 后许多这些生物碱的全身暴露。因此，我们开发并验证了一种生物分析方法，用于同时定量 11 种 kratom 生物碱（mitragynine、7-hydroxymitragynine、corynantheidine、speciogynine、speciociliatine、paynantheine、corynoxine、corynoxine-B、mitraphylline、ajmalicine 和 isospeciofolia。经验证的方法用于分析冻干卡托姆茶 (LKT) 和市售产品 OPMS 液体注射剂在大鼠中的口服药代动力学研究样品。在这 11 种生物碱中，只有 mitragynine、7-hydroxymitragynine、speciciliatine 和 corynantheidine 在给药后 8 小时显示全身暴露，并且这四种生物碱的剂量标准化全身暴露在商业 OPMS 给药后更高（1.6-2.4 倍）液体。Paynantheine 和 speciogynine 水平在给药后 1 小时内可量化，而没有检测到其他生物碱。总之，该方法已成功应用于量化口服传统或商业产品后单个 kratom 生物碱的暴露量。

更新日期：2021-04-23

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