Evaluation of Pharmacokinetic Profile of Cirpusins®, Extract of Cyperus rotundus in Presence of Bioavailability Enhancer, BioPerine®

Abstract

Obesity, a condition accompanying abnormal or excessive accumulation of fat in the body has become a major public health concern globally. Various herbs hailed from traditional systems of medicine like Ayurveda have gained importance in recent years to combat obesity. One such herb Cyperus rotundus (nutgrass), is known for its beneficial effects in obesity, in Ayurveda. Cirpusins® a patented extract from the dried rhizomes of Cyperus rotundus (standardized for minimum of 6% total identified stilbenes - Piceatannol, Scirpusin A & Scirpusin B) and BioPerine®, a bioavailability enhancer, obtained from the dried fruits of Piper nigrum (standardized to minimum 95% piperine). In this study, we examined the pharmacokinetic profile and bioavailability of Cirpusins® in Sprague-Dawley rats at two different doses (45 and 90 mg/kg) in the presence and absence of BioPerine® respectively. The results signifies that addition of BioPerine® (0.45 mg/kg) with Cirpusins® (45 mg/kg) enhances the bioavailability by reducing the effective dose of Cirpusins® (90 mg/kg) to half.

Enhancement in Bioavailability of CurCousin<sup>®</sup>, A Minor Metabolite from <i>Curcuma longa</i> by Addition of BioPerine<sup>®</sup> <br/>—A Pharmacokinetic Study

“…Bioenhancers are compounds that help to enhance the bioavailability of the active substance through increased absorption by enhancing the efficacy as well as reducing the dosage required to achieve the therapeutic effect. In this study, BioPerine ® , a natural bioenhancer has been used, which has been proven to significantly improve the bioavailability when co-administered with various compounds such as curcumin, resveratrol, ginseng, β-carotene [14], coenzyme Q10 [15], minerals (elemental iron, selenium), and vitamins (vitamin B6, vitamin C) [13]. The bioavailability enhancement mechanism of piperine could be elucidated through the-modulation of P-glycoprotein-mediated drug/ nutrient efflux, interaction with metabolic enzymes involved in biotransformation of drugs/nutrients, enhanced intestinal absorption, and its thermogenic action [13].…”

“…In this study, BioPerine ® , a natural bioenhancer has been used, which has been proven to significantly improve the bioavailability when co-administered with various compounds such as curcumin, resveratrol, ginseng, β-carotene [14], coenzyme Q10 [15], minerals (elemental iron, selenium), and vitamins (vitamin B6, vitamin C) [13]. The bioavailability enhancement mechanism of piperine could be elucidated through the-modulation of P-glycoprotein-mediated drug/ nutrient efflux, interaction with metabolic enzymes involved in biotransformation of drugs/nutrients, enhanced intestinal absorption, and its thermogenic action [13]. CurCousin ® is a nutritional ingredient containing 99% pure Calebin A, a curcumin analog with potent pharmacological benefits has been clinically proven to have positive impact in managing healthy weight, lipid levels and metabolic health [9] [10].…”

“…Multiple studies have been reported to confirm that BioPerine ® significantly improves bioavailability when co-administered with various compounds through their increased absorption. Compounds such as curcumin, resveratrol, ginseng, β-carotene, coenzyme Q10, minerals (elemental iron, selenium), and vitamins (vitamin B6, vitamin C) were shown to enhance the bioavailability through increased absorption when administered with BioPerine ® [13]. Thus, reducing the concentration of the dose will help to reduce the side effects and pricing of therapies that benefit more people due to their low cost.…”