Olawoye O S, Adeagbo B A, Bolaji O O
Department of Pharmaceutical Chemistry, Obafemi Awolowo University, Ile-Ife, Nigeria.
J Clin Pharm Ther. 2018 Oct;43(5):626-632. doi: 10.1111/jcpt.12725. Epub 2018 Jun 19.
Moringa oleifera (MO) Lam (Moringaceae) is commonly used as food supplement and as medicine in most African countries where malaria is also endemic. Therefore, co-administration of MO with antimalarials is a possibility. This study investigated the effects of MO leaves powder on the pharmacokinetics of amodiaquine (AQ) in human subjects.
Twenty healthy volunteers were recruited for the 3-period study. In the first period, a single dose of AQ tablet (10 mg/kg) was administered orally after an overnight fast. After a 7-day washout period, AQ was co-administered with MO. For the third period, each subject took 3 g MO once daily for 7 days and on the 8th day, MO was co-administered with AQ. The plasma concentrations of amodiaquine and desethylamodiaquine (DEAQ) were simultaneously determined using a validated HPLC method.
The results showed a significant decrease (P = .037) in the Cmax of AQ after concurrent administration (CA) with MO, whereas after pretreatment (PT), there was a 32% decrease in the C of AQ. For the metabolite, DEAQ, C increased significantly (P = .006) by 79.36%, and Cmax in PT was significantly higher than (P = .001) that of the CA arm of the study. AUC of DEAQ increased significantly by 40.4% (P = .006) and by 188% (P = .001) after CA and PT, respectively.
The study established pharmacokinetic interaction between AQ and MO when given together or following a long period of ingestion of MO. This may have clinical implications for malaria therapy.
辣木(MO)(辣木科)在大多数疟疾流行的非洲国家通常用作食品补充剂和药物。因此,辣木与抗疟药联合使用是有可能的。本研究调查了辣木叶粉对人体阿的平(AQ)药代动力学的影响。
招募20名健康志愿者进行为期3个阶段的研究。在第一阶段,禁食过夜后口服单剂量的阿的平片剂(10mg/kg)。经过7天的洗脱期后,阿的平与辣木联合给药。在第三阶段,每位受试者每天服用3g辣木,持续7天,在第8天,辣木与阿的平联合给药。使用经过验证的高效液相色谱法同时测定血浆中阿的平和去乙基阿的平(DEAQ)的浓度。
结果显示,与辣木同时给药(CA)后,阿的平的Cmax显著降低(P = 0.037),而预处理(PT)后,阿的平的C降低了32%。对于代谢物DEAQ,C显著增加(P = 0.006),增加了79.36%,PT组的Cmax显著高于(P = 0.001)研究的CA组。CA和PT后,DEAQ的AUC分别显著增加40.4%(P = 0.006)和188%(P = 0.001)。
该研究确定了阿的平和辣木同时给药或长期摄入辣木后存在药代动力学相互作用。这可能对疟疾治疗具有临床意义。