Abstract

The present study was conducted to investigate the effects of Nigella sativa and Lepidium sativum on the pharmacokinetics of cyclosporine in rabbits. Two groups of animals were treated separately with Nigella sativa (200 mg/kg p.o.) or Lepidium sativum (150 mg/kg p.o.) for eight consecutive days. On the 8th day, cyclosporine (30 mg/kg p.o.) was administered to each group one hour after herbal treatment. Blood samples were withdrawn at different time intervals (0.0, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 12, and 24 hrs) from marginal ear vein. Cyclosporine was analyzed using UPLC/MS method. The coadministration of Nigella sativa significantly decreased the C max and AUC0−∞ of cyclosporine; the change was observed by 35.5% and 55.9%, respectively (P ≤ 0.05). Lepidium sativum did not produce any significant change in C max of cyclosporine, although its absorption was significantly delayed compared with control group. A remarkable change was observed in T max and AUC0−t of Lepidium sativum treated group. Our findings suggest that concurrent consumption of Nigella sativa and Lepidium sativum could alter the pharmacokinetics of cyclosporine at various levels.

Highlights

  • Based on the belief that natural medicines are much safer than synthetic medicines, the use of complementary and alternative medical therapies has become a common trend in developing countries [1]

  • The in vivo investigations were carried out to determine the effect of Nigella sativa and Lepidium sativum on Cyclosporine A (CsA) pharmacokinetics

  • The observations showed that mean maximum blood concentration and area under curve of CsA was significantly decreased when coadministered with Nigella sativa

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Summary

Introduction

Based on the belief that natural medicines are much safer than synthetic medicines, the use of complementary and alternative medical therapies has become a common trend in developing countries [1]. The literature based on in vitro and in vivo investigations suggests that concomitant administration of natural products and prescription drugs may modulate drug pharmacokinetics, which may lead to toxic or subtherapeutic incidences. Herbal remedies may contain multiple active constituents such as alkaloids, flavonoids, glycosides, anthraquinones, saponins, and others, which have the potential to interact with therapeutic drugs. Consumption of herbs that are capable of modulating CYP or drug transporters may cause clinically relevant herb-drug interactions by altering the bioavailability and pharmacokinetics of drugs [10]

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