Piperine is commercially available. If desired, it may be extracted from black pepper using dichloromethane. Aqueous hydrotopes can also be used in the extraction to result in high yield and selectivity. The amount of piperine varies from 1-2% in long pepper, to 5-9% in the white and the black peppers of commerce.
Further, it may be prepared by treating the solvent-free residue from an alcoholic extract of black pepper, with a solution of potassium hydroxide to remove resin (said to contain chavicine, an isomer of piperine) and solution of the washed, insoluble residue in warm alcohol, from which the alkaloid crystallises on cooling.
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Piperine is the standardized extract made from the fruit of Piper Nigrum (black pepper) or Piper longum L (long pepper) and is manufactured for use as a nutritional ingredient for both human and animal health.
Piperine is involved to increase the absorption of other nutrients in the body and has other novel applications as well - such as helping to fight colon cancer and having an anti-depressant effect while enhancing the cognitive functions of the brain.
Piperine(CAS NO:94-62-2) was discovered in 1819 by Hans Christian Ørsted, who isolated it from the fruits of Piper nigrum, the source plant of both the black and white pepper grains. Piper longum and Piper officinarum, two species called "long pepper" also were found to contain it by Flückiger and Hanbury.West African pepper also contains it.
Piperine(CAS NO:94-62-2) has been found to inhibit human CYP3A4 and P-glycoprotein, enzymes important for the metabolism and transport of xenobiotics and metabolites.In animal studies, piperine also inhibited other enzymes important in drug metabolism.
By inhibiting drug metabolism, piperine may increase the bioavailability of various compounds and alter the effectiveness of some medications. Notably, piperine may enhance bioavailability of curcumin by 2000% in humans.The exact mechanism of piperine's bioavailability enhancing abilities is unknown.Chemopreventive efficacy of curcumin and piperine has been shown during 7,12-dimethylbenz[a]anthracene-induced hamster buccal pouch carcinogenesis.
The pungency of capsaicin and piperine is caused by activation of the heat and acidity sensing TRPV ion channel TRPV1 on nociceptors .
Recently the journal Molecular Nutrition Food Research published evidence that piperine can enhance the pharmacokinetic parameters of resveratrol via inhibiting its glucuronidation, thereby slowing its elimination.
In February 2008, researchers discovered that piperine can stimulate pigmentation in the skin, together with the exposure to UVB light. Piperine has shown 'anti-depression like activity, and cognitive enhancing effects in rats. Piperine has shown anti-inflammatory and anti-arthritic effects in human interleukin-1beta-stimulated fibroblast-like synoviocytes and in rat arthritis models.
Various studies have proven the effectiveness of BioPerine and some showed that absorption levels were increased up to 60%. In one study it was shown that it also has value in helping to maintain a healthy colon and to help protect against colon cancer, while another study showed that it possessed anti-depression like activity and cognitive enhancing properties, while yet another study showed it may contain antibacterial properties as well as anti-allergy properties.
It is interesting to note that Ayurvedic medicine the ancient Indian medical system has been preoccupied for more than 6,000 years with the proper functioning of the digestive tract and especially the digestion and absorption of nutrients. Nearly 60% of all traditional Ayurveda medicine contains some special blend of ingredients, which include black pepper in the blend.
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Ranolazine is an anti-anginal medication. It works by improving blood flow to help the heart work more efficiently. It is used to treat chronic angina (chest pain). But it is not for use during an acute (emergency) attack of angina. It may also be used for purposes not listed in this medication guide.
Ranolazine(CAS NO:94-62-2), sold under the trade name Ranexa by Gilead Sciences (who acquired the developer, CV Therapeutics in 2009), is an antianginal medication. In India, it is sold under the name "Ranozex". On January 31, 2006, ranolazine was approved for use in the United States by the Food and Drug Administration (FDA) for the treatment of chronic angina pectoris.
In this article , let us learn about how Ranolazine(CAS NO:94-62-2) was approved to use in Europe and United States.
In Europe
On 24 April 2008, the European Medicines Agency's Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion, recommending to grant a marketing authorisation for the medicinal product Latixa, 375-mg, 500-mg and 750-mg, prolonged-release tablets intended for treatment of patients with stable angina pectoris. The applicant for this medicinal product is CV Therapeutics Europe Limited.
The approved indication is: “Latixa is indicated as add-on therapy for the symptomatic treatment of patients with stable angina pectoris who are inadequately controlled or intolerant to first-line antianginal therapies (such as beta blockers and/or calcium antagonists).”
In United States
The Food and Drug Administration has approved a new, first-line indication for ranolazine(CAS NO:94-62-2) for the treatment of chronic angina. The new labeling also provides information showing ranolazine reduced arrhythmias, including ventricular arrhythmias, new onset atrial fibrillation and a potentially dangerous slow heartbeat known as bradycardia in patients with coronary artery disease. In addition, the new labeling states Ranexa reduces hemoglobin A1c (HbA1c) in patients with diabetes.
According to the revised labeling, ranolazine is indicated for the treatment of chronic angina and may be used alone or in combination with traditional therapies for chronic angina, such as beta blockers, calcium channel blockers and nitrates, and common cardioprotective treatments for cardiovascular disease, such as antiplatelet therapy, lipid-lowering therapy, ACE inhibitors and angiotensin receptor blockers.
Ranolazine may now be used as part of a medical therapy regimen for chronic angina patients, regardless of whether or not they receive a stent or other medical intervention. Ranolazine does not reduce heart rate or blood pressure and, unlike long-acting nitrates, ranolazine can be prescribed for patients taking oral erectile dysfunction treatments.
These new labeling changes were supported by a supplemental new drug application submitted in September 2007 that included data from the 6,560-patient MERLIN TIMI 36 trial, which showed no adverse trend in death or arrhythmia in a high-risk acute coronary syndromes patient population.
The revised labeling includes new language noting a significantly lower incidence of arrhythmias (ventricular tachycardia, bradycardia, supraventricular tachycardia and new atrial fibrillation) in patients treated with Ranexa versus placebo. This difference in arrhythmias did not lead to a reduction in mortality, a reduction in arrhythmia hospitalization or a reduction in arrhythmia symptoms.
The revised labeling also includes new language noting ranolazine produces small reductions in HbA1c. Though Ranolazine should not be considered a treatment for diabetes, it may be a particularly useful medication for the reduction of chronic angina in this patient population, which is difficult to treat because some antianginal medications, such as beta blockers, increase HbA1c.
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