Piperine - Is a purified extract from the fruit of Black and Long Peppers (Piper nigrum and Piper longum), a generally recognized as safe (GRAS) lipophilic (‘fat soluble”) alkaloid that is responsible for pepper’s pungency (“spiciness”).
(Studies listed in the Scientific Studies)
Increased Nutrient Absorption up to 300%
It is a part of Ayurveda, the traditional medicine of India, dating back well over two thousand years ago, and one of its most widely used herbs in two-thirds
of all Ayurvedic prescriptions. Together with the pungent alkaloids found in other spices like garlic, ginger, licorice and turmeric, it increases the bioavailabilty of coadministered substances such as vitamins, minerals, dietary supplements and pharmaceutics.
Piperine acts as “bioenhancer” of various substances. Current published studies have shown that it significantly increases the absorption and
bioavailabilty of vitamins (B1, B2, B3, B6, B9, B12, C), minerals (iodine, calcium, iron, zinc, copper, selenium, magnesium, potassium, manganese), amino acids (lysine, isoleucine, leucine, threonine, valine, tryptophan, phenylalanine, methionine), herbal compounds (curcumin, ginsenosides, quercetin, coenzyme Q10, resveratrol, epigallocatechin gallate from green tea, pycnogenol), and drugs (such as ibuprofen, diclofenac, rifampicin, ampicillin, tetracycline, pyrazinamide, fexofenadine). For example, it has been shown to increase curcumin
levels by 2000%.
Drugs, supplements and nutrients taken by mouth (as opposed to intravenous, sublingual, intranasal, transdermal, buccal) are affected by “first pass metabolism.” Essentially, they are degraded by digestion in the stomach and intestines by acids and enzymes; significantly altered in the liver; and, excreted. This affects their bioavailabilty – the amount of the substance that actually ends up in circulation – in the blood.
For example, cannabidiol (CBD) is 34-46% bioavailable intranasally; 40% when vaporized; but, approximately 6-9% when taken orally: so, for every 100mg ingested, only 9mg is available for use. Orally, aspirin is 68%, Zolpidem (i.e. Ambien®) 67%, diphenhydramine (e.g. Benadryl®) 40-60%, ACE inhibitors (e.g. Benazepril/Lotensin®) 37% and statins (i.e. Simvastatin/Zocor®) only 5% capable of being used by the body.
The bioavailabilty of a substance is based on four different processes: (1) conversion: enzymes in the gut breakdown the substance into something much less active; (2) absorption: shuttling the substance to the intestines where they can be transferred to the blood thru the intestinal lining; (3) exclusion: removing substances from the cells that cannot be used; and, (4) solubility: adding to the substance to make it unable to enter the cells. Piperine has the ability to
affect all of these processes.
Piperine inhibits the enzymes in the gut and intestines that breakdown/metabolize and convert drugs and nutritive substances. It stimulates the activity of amino-acid transporters in the intestinal lining. It inhibits p-glycoprotein, the ‘pump’ protein that removes substances from cells and it decreases the intestinal production of glucuronic acid, thereby permitting more of the substances to enter the body in active form. Consequently, some of these substances are able to reach, enter, and remain within their target cells for longer periods of time than would otherwise be the case. Therefore, Piperine can sometimes turn a marginally effective therapeutic substance into a highly effective one simply by increasing its bioavailability and intracellular residency.
Ingredient: PIPERINE - Works Cited:
(1) Panahi Y, Ghanei M, Hajhashemi A et al: Effects of Curcuminoids-Piperine
Combination on Systemic Oxidative Stress, Clinical Symptoms and Quality of
Life in Subjects with Chronic Pulmonary Complications Due to Sulfur
Mustard: A Randomized Controlled Trial. J Diet Suppl. 2014 Aug 29. [Epub
ahead of print] http://www.ncbi.nlm.nih.gov/pubmed/25171552
(2) Panahi Y, Badeli R, Karami GR et al: Investigation of the Efficacy of
Adjunctive Therapy with Bioavailability-Boosted Curcuminoids in Major
Depressive Disorder. Phytother Res. 2014 Aug 4. doi: 10.1002/ptr.5211. [Epub
ahead of print] http://www.ncbi.nlm.nih.gov/pubmed/25091591
(3) Rahimnia AR, Panahi Y, Alishiri G et al: Impact of Supplementation with
Curcuminoids on Systemic Inflammation in Patients with Knee Osteoarthritis:
Findings from a Randomized Double-Blind Placebo- Controlled Trial. Drug
Res (Stuttg). 2014 Jul 22. [Epub ahead of print]
(4) Ajazuddin, Alexander A, Qureshi A et al: Role of herbal bioactives as a
potential bioavailability enhancer for Active Pharmaceutical Ingredients.
Fitoterapia. 2014 Sep;97C:1-14.
(5) Wightman EL, Reay JL, Haskell CF et al: Effects of resveratrol alone or in
combination with piperine on cerebral blood flow parameters and cognitive
performance in human subjects: a randomised, double-blind, placebocontrolled,
cross-over investigation. Br J Nutr. 2014 Jul;112(2):203-13.
(6) Feng X, Liu Y, Wang X et al: Effects of piperine on the intestinal
permeability and pharmacokinetics of linarin in rats. Molecules. 2014 Apr
(7) Kesarwani K1, Gupta R, Mukerjee A: Bioavailability enhancers of herbal
origin: an overview. Asian Pac J Trop Biomed. 2013 Apr; 3(4):253-66.
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