Balap Aishwarya, Lohidasan Sathiyanarayanan, Sinnathambi Arulmozhi, Mahadik Kakasaheb
Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University (BVDU), Pune 411038, India.
Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University (BVDU), Pune 411038, India.
J Ethnopharmacol. 2017 Jan 4;195:214-221. doi: 10.1016/j.jep.2016.11.022. Epub 2016 Nov 12.
Andrographis paniculata Nees (Acanthacae) have broad range of pharmacological effects such as hepatoprotective, antifertility, antimalarial, antidiabetic, suppression of various cancer cells and anti-inflammatory properties and is widely used medicinal plant in the traditional Unani and Ayurvedic medicinal systems. Andrographolide (AN) is one of the active constituent of the A. paniculata Nees extract (APE). They have been found in many traditional herbal formulations in India and proven to be effective as anti-inflammatory drug.
To evaluate the pharmacokinetic and pharmacodynamic (anti arthritic) herb-drug interactions of A. paniculata Nees extract (APE) and pure andrographolide (AN) with naproxen (NP) after oral co-administration in wistar rats.
After oral co-administration of APE (200mg/Kg) and AN (60mg/kg) with NP (7.5mg/kg) in rats, drug concentrations in plasma were determined using HPLC method. The main pharmacokinetic parameters of C, t, t, MRT, Vd, CL, and AUC were calculated by non-compartment model. Change in paw volume, mechanical nociceptive threshold, mechanical hyperalgesia, histopathology and hematological parameters were evaluated to study antiarthritic activity.
Co-administration of NP with APE and pure AN decreased systemic exposure level of NP in vivo. The C, t AUC of NP was decreased. In pharmacodynamic study, NP (10mg/kg) alone and NP+AN (10+60mg/kg) groups exhibited significant synergistic anti-arthritic activity as compared to groups NP+APE, APE and AN alone.
The results obtained from this study suggested that NP, APE and pure AN existed pharmacokinetic herb-drug interactions in rat which is correlated with anti-arthritic study. The knowledge regarding possible herb-drug interaction of NP might be helpful for physicians as well as patients using AP. So further studies should be done to understand the effect of other herbal ingredients of APE on NP as well as to predict the herb-drug interaction in humans.
穿心莲（爵床科）具有广泛的药理作用，如保肝、抗生育、抗疟疾、抗糖尿病、抑制多种癌细胞以及抗炎特性，是传统尤那尼和阿育吠陀医学体系中广泛使用的药用植物。穿心莲内酯（AN）是穿心莲提取物（APE）的活性成分之一。它们在印度的许多传统草药配方中都有发现，并被证明是有效的抗炎药物。
评估在Wistar大鼠口服联合给药后，穿心莲提取物（APE）、纯穿心莲内酯（AN）与萘普生（NP）之间的药代动力学和药效学（抗关节炎）药物相互作用。
在大鼠中口服联合给予APE（200mg/Kg）、AN（60mg/kg）与NP（7.5mg/kg）后，采用高效液相色谱法测定血浆中的药物浓度。通过非房室模型计算C、t、t、MRT、Vd、CL和AUC的主要药代动力学参数。评估爪体积、机械性痛觉阈值、机械性痛觉过敏、组织病理学和血液学参数的变化，以研究抗关节炎活性。
NP与APE和纯AN联合给药降低了NP在体内的全身暴露水平。NP的C、t、AUC降低。在药效学研究中，与NP+APE、APE和单独的AN组相比，单独的NP（10mg/kg）组和NP+AN（10+60mg/kg）组表现出显著的协同抗关节炎活性。
本研究获得的结果表明，NP、APE和纯AN在大鼠中存在药代动力学药物相互作用，这与抗关节炎研究相关。关于NP可能的药物相互作用的知识可能对使用穿心莲的医生和患者都有帮助。因此，应进一步开展研究，以了解APE的其他草药成分对NP的影响，以及预测人体中的药物相互作用。
