bioperine

Bioperine

$8.99

Due to its ability to increase the absorption of nutrients comprising nutritional supplement formulations as shown in Figures 1-4, BioPerine has been termed a natural Thermonutrient® and bioavailability enhancer (Majeed, M. et al; 1999).

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The Patented extract from black pepper fruit significantly improves the gastrointestinal absorption and systemic utilization of nutrients that are supplemented. In a series of clinical studies performed on various nutrients, BioPerine’s bioavailability benefits were evaluated and findings were published in peer-reviewed journals.  BioPerine’s bioavailability enhancement effect has been well studied with several nutrients such as curcumin, resveratrol coenzyme Q10, vitamins such as B6, vitamin C and beta carotenes.   Optimizing nutrient delivery can go a long way in enhancing the dosage efficiency and health benefits obtained from your supplements.

In a recently published University of Wisconsin study, BioPerine enhances the bioavailability degree of exposure of Resveratrol the chief polyphenol of red wine by 229%.  Bioperine is a self-affirmed GRAS ingredient, clinically proven and patented extract from black pepper fruits used for over 15 years.  Studies that show BioPerine’s bio-enhancement activity on variety of ingredients such as Curcumin, CoQ10, vitamins and minerals.

With just 5mg of BioPerine, it is possible to change the way the body looks at supplements.  When using supplements, you might think that by merely increasing the milligrams of an ingredient, the supplement becomes more potent and available for use by the body.  In fact, research indicates that this approach can actually negate the benefit and absorption of other nutrients.  Instead by adding 5 mg of Bio Perine, Natures Own Thermonutrient, a patented extract from the black pepper fruit.  Based on clinical data, having Bioperine in the right place at the right time in the digestive tract, with a supplemented nutrient, improves absorption.  Give yourself the optimum nutrition and supplementation by boosting absorption with BioPerine.

It may be interesting to note that high absorption may not always lead to high bioavailability. Similarly, low bioavailability may not necessarily result from poor absorption. Resveratrol is a stilbene polyphenol which has a good absorption profile; oral absorption of resveratrol in human has been found to be around 75% of the ingested amount, however due to extensive metabolism in the intestine and the liver, hardly 1% of the ingested amount is bioavailable as resveratrol. The rest is converted to metabolites such as resveratrol glucuronides.

bioperine

A recent study (Johnson et al. 2011) explored the effect of piperine co-administration with resveratrol on serum levels resveratrol and resveratrol-3-O-β-D-glucuronide in C57BL mice. Mice were administered resveratrol (100 mg/kg; oral gavage) or resveratrol (100 mg/kg; oral gavage) piperine (10 mg/kg; oral gavage), and the serum levels of resveratrol and resveratrol-3-O-β-D-glucuronide were analyzed. The authors found that the degree of exposure (i.e. AUC) to resveratrol was enhanced to 229% and the maximum serum concentration (Cmax) was increased by 1544% with the addition of piperine, the Cmax of resveratrol-β-D-glucuronide was increased by 184%, and Tmax was increased from 0.25h to 0.5 h. The authors therefore concluded that the results of this study demonstrated that that piperine significantly improves the in vivo bioavailability of resveratrol. The mechanism proposed was through inhibition of glucuronidation of resveratrol by piperine

Other new research suggests the beneficial role of Bioperine® in enhancing the bioavailability of biologically significant phytonutrients such as resveratrol, which have garnered scientific validation in benefits in healthy aging and longevity . However, although laboratory studies offered great promise in potential therapeutic and preventative applications, the poor bioavailability of resveratrol in formulation has precluded its applicability as in controlled clinical settings. Pharmacokinetic studies in animals and humans have identified that the major metabolites of trans-resveratrol are derived by glucuronidation or sulfation, and the metabolism of resveratrol has been shown to be very rapid with the majority of biotransformation occurring within the first hour following oral administration. Furthermore, resveratrol metabolites have very short half-life and are subjected to rapid urinary elimination. There is therefore a need for efficacious co-administered substances that will sufficiently enhance the absorption of resveratrol in vivo.

A pioneering study evaluated the potential of a standardized piperine-enhanced curcuminoid preparation to alter the disposition of drugs metabolized by a number of the most important drug metabolizing enzymes in healthy human subjects. The results clearly demonstrate that there is no clinically significant effect of this particular preparation on the pharmacokinetic disposition flurbiprofen, acetaminophen, or midazolam as compared with placebo. These findings suggest that short-term (2 day) treatment with a curcuminoid/piperine combination is unlikely to substantially alter the disposition of medications primarily dependent on CYP3A or CYP2C9, or on the UGTs or SULTs responsible for metabolizing acetaminophen (Volak et al. (2013)). The authors further expressed the need for assessing drug interaction potential of nanoparticles of curcuminoids and other preparations that have been reported to be alternative methods to enhance bioavailability of curcuminoids. Though the genotoxicity of piperine has been investigated by several researches previously, owing to lack of data on the dose levels covering the range from “Not Toxic” to as “high as possible”, information on the genotoxicity of this traditional herb was considered incomplete until recently, in an animal study published in 2014, it was shown that piperine did not cause micronucleus induction in vivo up to the MTD (Maximum tolerated Dose) levels, thus providing strong evidence that Piperine is not genotoxic (A Theil et al. 2014).

Acute, subacute and chronic toxicity studies of piperine in laboratory animals indicate that piperine used even in a broad range of doses does not cause abnormalities in the general growth pattern, body to organ weight ratio, clinical symptomatology, or blood chemistry. The dose of piperine considered to be bioenhancing for absorption of nutrients is calculated as 0.04 to 0.08 mg piperine/kg body weight. That dose is 4,000 times less than the LD50 dose (dose toxic to 50% animals tested) of piperine established in mice and rats. Incidentally, the dose of piperine, which increased the bioavailability of the actives studied, was several times lower than the estimated amount of piperine consumed daily in the diet by an average individual in the USA (Majeed, M. et al.; 1999). Research into the bioavailability effects of piperine show that such bioenhancing effect lasts only for a short duration and there is a progressive time dependent reversion of such effect to baseline levels which negate any adverse reaction or interaction with any nutrient or drug ingested with sufficient time lag. This rapid reversion of the bioavailability effects could be one underlying reasons for lack of reports on piperine or pepper associated drug interactions as commented by

A thermonutrient such as BioPerine would potentially improve the process of nutrient absorption by enhancing thermogenesis. The leading theory of food-induced thermogenesis relates to the autonomous nervous system. The autonomous nervous system is represented by two main receptors in the gastrointestinal tract, the alpha and beta adrenergic receptors. Most of the food or thermonutrient-induced thermogenesis is facilitated by beta receptors, which include a compound known as cyclic adenosine 3’, 5’ monophosphate (cAMP). The role of cAMP as a “second messenger” to the hormonal and enzymatic actions in the body is well recognized. When thermogenesis occurs, the demand for fresh nutrients to sustain the metabolic processes rapidly increases. Other mechanisms by which piperine stimulates nutrient absorption have also been discussed in literature. These include increased micelle formation, stimulation of active transport of amino acids (gamma-glutamyl transpeptidase), and epithelial cell wall modification due to the affinity of piperine towards fats and fatty substances. Piperine has recently been investigated for its anti-adipogenic activity. Using 3T3-L1 cells which are used in biological research on adipose tissue, scientists were able to show piperine attenuates fat cell differentiation by down regulating the PPARϒ activity as well as suppressing the PPARϒ expression, leading to potential benefits in weight management in obese subjects (UH Park et al, 2012). As there are number of piper containing Ayurvedic preparation used for liver disorders such as Trikatu in traditional medicinal system, piperine, and the active substance has been evaluated for its effect on hepatic health. In the animal model using piperine showed liver protective benefits against the hepatoxicity created by t-butyl hydoperoxide and carbon tetrachloride (IB Kaul and A Kapil, 1992). Nutrient delivery can play major role in its efficacy and usually can be key to a successful product. Optimizing the nutrient delivery can go a long way in enhancing the dosage efficiency and health benefits obtained from the formulation. BioPerine® can be safe, clinically proven, scientifically validated, Bioenhancer with a long history of usage for your formulation. In view of these findings it is proposed that piperine ingested in relatively small amounts would act as a thermonutrient. Localized thermogenic action on the epithelial cells would in turn increase the rate of absorption of supplemented nutrient(s). These thermogenic properties may explain how a small amount of BioPerine (5 mg) can afford such a profound effect on serum nutrient levels (as shown in our studies on water soluble, fat soluble and botanical ingredients). It is possible that when piperine is ingested, it has a localized thermogenic effect on epithelial cells which increase the uptake of nutrients. One of the other important mechanism by which Piperine enhances the bioavailability is by inhibiting the biotransformation of the nutrients via the major phase II metabolic pathway- glucuronidation. This transformation is catalyzed by UDP glucuronosyltransferases which transfers the glucuronic acid component of UDP-glucuronic acid to nutrient or xenobiotics. Piperine reduces the glucuronidation process by inhibiting the UDP glucuronyl transferase activity as well as lowering the levels of endogenous glucuronic acid. (Singh et al 1986, Reen et al 1993). By inhibiting the glucuronidation process, BioPerine is able to reduce the biotransformation of nutrients like Curcumin into metabolites such as Curcumin glucuronides. Studies in recent past have shown that the curcumin metabolites such as Curcumin monoglucoronides do not have anti-inflammatory activity nor do they have toxicity towards the cancer cells, hence do not possess the anti cancerous activity as Piperine has been found in independent studies well. (Motomu Shoji et al 2014, A Pal et al 2014). to stimulate the release of catecholamines, thermogenic hormones whose action is made possible by the presence of cAMP. However, the nature of the thermogenic response mediated by catecholamines is relatively short-lived. Therefore, the window of opportunity for piperine-induced thermogenesis and enhanced nutrient absorption is small.

Nutrient delivery can play major role in its efficacy and usually can be key to a successful product. Optimizing the nutrient delivery can go a long way in enhancing the dosage efficiency and health benefits obtained from the formulation. BioPerine® can be safe, clinically proven, scientifically validated, Bioenhancer with a long history of usage for your formulation.

References 1. PL Toutain & AB Melou. Bioavailability and its assessment. J. Vet. Pharmacol. Therap. 27, 455-466. 2004. 2. Basu, T.K.: The influence of drugs with particular reference to aspirin on bioavailability of Vitamin C; in Counsel, Hornig, Vitamin C, pp.273-281 (Applied Science Publishers, Barking 1981). 3. Walle T. Bioavailability of Resveratrol. Ann N Y Acad Sci 1215, 9-15.2011. 4. Majeed M, et al. BioPerine® Nature’s Own Thermonutrient® and Natural Bioavailability Enhancer. Nutriscience Publishers Inc. Piscataway, NJ, 1999. 5. Badmaev, V, Majeed, M. et al. Piperine, An Alkaloid Derived from Black Pepper, Increases Serum Response of Beta-Carotene During 14 Days of Oral Beta-Carotene Supplementation. Nutrition Research, 19(3) 381-388, 1999. 6. Badmaev, V, Majeed, M. et al. Piperine derived from black pepper increases the plasma levels of coenzyme q10 following oral supplementation, The Journal of Nutritional Biochemistry. 11 (2), 109-113, 2000. 7. Shoba G, et al. Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers. Planta Med; 64(4):353-6. 1998. 8. Johnson, JJ et al. Enhancing the bioavailability of resveratrol by combining it with piperine. Mol. Nutr. Food Res. 2011 Aug;55(8):1169-76. 9. A Mohammadi et al. Effects of supplementation with curcuminoids on Dyslipidemia in obese patients: A randomized Crossover trial. Phytotherapy Research. 27(3), 374-379. 2013. 10. A Sehgal et al. Piperine as an adjuvant increases the efficacy of curcumin in mitigating benzo(a)pyrene toxicity. Human and Experimental Toxicology. 31(5), 473-482. 11. Gulseren et al. Effect of interfacial composition on uptake of curcumin-piperine mixtures in oil in water emulsions by Caco-2 cells. Food & Function. DOI 10.1039/c3fo60554j 2014. 12. Majeed, M and Prakash, L. THP: An All Natural Delivery System Adjuvant. In Delivery System Handbook for Personal Care and Cosmetic Products: Technology, Applications and Formulations. Meyer R. Rosen (editor), William and Andrew Publishing, 2005. 13. Han Y, Tan TMC, Lim LY. In vitro and in vivo evaluation of the effects of piperine on P-gp function and expression. Toxicology and Applied Pharmacology. 230(3): 283-289. 2008 14. Volak, LP et al. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers. Br J Clin Pharmacol. 2013 Feb;75(2):450-62. 15. Theil et al. Black pepper constituent piperine: Genotoxicity studies in vitro and in vivo. Food and Chemical Toxicology. 66, 350-357. 2014. 16. Singh J, Dubey RK and Atal CK. Piperine-mediated inhibition of glucuronidation activity in isolated epithelial cells of the guinea – pig small intestine: evidence that piperine lowers the endogenous UDP-glucuronic acid content. 17. RK Reen et al. Impairment of UDP-glucose dehydrogenase and glucuronidation activities in liver and small intestine of rat and guinea pig in vitro by piperine. Biochem Pharmacol. 46(2), 229-38. 1993. 18. A Pal et al. Curcumin glucuronides: assessing the proliferative activity against human cell lines. Bioorganic & Medicinal Chemistry.22, 435-439. 2014. 19. M Shoji et al. Comparison of the effects of Curcumin and curcumin glucuronides in human hepatocellular carcinoma HepG2 cells. Food Chemistry. 151, 126-132. 2013. 20. Ui-Hyun Park et al. Piperine, a component of black pepper, inhibits adipogenesis by antagonizing PPARϒ activity in 3T3-L1cells. Journal of agriculture and Food Chemistry. 60, 3853-3860. 2012. 21. IB Koul and A Kapil. Evaluation of the liver protective potential of p

 

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