Capsorb™ is also known as sodium caprate, as sodium decanoate, and as C10. Sodium decanoate is a salt of decanoic acid. Decanoic acid is a naturally-occurring mediumchain fatty acid used in the manufacture of decanoate esters, which are used in perfumes, as flavourings, and in pharmaceuticals.

Capsorb™ is an absorption promoter Capsorb™ increases the oral bioavailability of poorly permeable compounds, by increasing absorption across the gut wall. [Note: Pharmaceuticals are divided into the Biopharmaceutics Classification System (BCS), a system to differentiate the drugs on the basis of their solubility and permeability. Sodium decanoate may be used to promote the oral absorption of Class III compounds – those with high solubility but low permeability.]

Capsorb™ dilates tight junctions Many bioavailability enhancers work by increasing cellular permeability, allowing greater transcellular movement (through the epithelial cells) by diffusion or active transport. Capsorb™ dilates tight junctions (TJs) in the intestinal epithelium, increasing their permeability, facilitating paracellular transport (between the cells).

C10’s TJ dilatating effects are believed to be short-lived, being reversed as soon as 40 mins after exposure – long enough to enhance absorption of those compounds co-administered. Clinical trials of enteric-coated matrices combining C10 with a variety of poorly-absorbed pharmaceuticals have consistently demonstrated improved bioavailability of the active ingredient.

Capsorb™ is Generally Recognized As Safe (GRAS) Although there were concerns that the TJ-widening effect of Capsorb™ may permit or promote the coabsorption of bacterial pathogens, several studies have shown this not to be the case. Capsorb™, as sodium caprate, is already approved as a food additive, and is generally recognized as safe when used use as a binder, emulsifier, and anticaking agent. [See: 21CFR172.863]

References and further reading: Cox AB, Rawlinson L-A, Baird AW, Bzik V, Brayden DJ. In vitro interactions between the oral absorption promoter, sodium caprate (C(10)) and S. typhimurium in rat intestinal ileal mucosae. Pharm Res. 2008 Jan;25(1):114–22. Leonard TW, Lynch J, McKenna MJ, Brayden DJ. Promoting absorption of drugs in humans using mediumchain fatty acid-based solid dosage forms: GIPET™. Expert Opin Drug Deliv. 2006 Sep 1;3(5):685–92. Kurasawa M, Kuroda S, Kida N, Murata M, Oba A, Yamamoto T, et al. Regulation of tight junction permeability by sodium caprate in human keratinocytes and reconstructed epidermis. BiochemBiophys Res Commun. 2009 Apr 3;381(2):171–5. Maher S, Leonard TW, Jacobsen J, Brayden DJ. Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic. Adv Drug Deliv Rev. 2009 Dec 17;61(15):1427–49.

Although little-known in the USA, arecoline is the fourth most common self-administered psychoactive substance in the world — only behind after alcohol, caffeine, and nicotine.  No surprise, then, that it’s a potent stimulant that operates via multiple mechanisms of action:

-Arecoline is a non-selective agonist of muscarinic acetylcholine receptors.  The M1 receptor subtype, in particular, underlies Arecoline’s CNS stimulant and nootropic effects.  It is highly expressed in the central nervous system, regulates dopamine and adrenaline secretion in the brain, and is important to the processes of learning and memory.

-Arecoline is a weaker agonist at nicotinic acetylcholine receptors.  This also contributes to its stimulant effect, and may additionally impart anti-inflammatory activity.

-Arecoline has lipolytic effects and inhibits the growth of adipocytes.  Although the molecular mechanisms behind this are not well understood, it has been shown that arecoline inhibits GLUT4, an enzyme which shuttles glucose into fat cells.  Regardless of the mechanism, what is certain is that in addition to arecoline’s effects as a stimulant, it has a separate, and noteworthy, fat-burning effect.

Arecoline HBr is non-toxic at reasonable dosage levels — in most respects it is significantly less dangerous than caffeine.  With chronic oral use in a mouse model, no adverse effects were seen at doses lower than 100mg/kg/day — close to caffeine’s LD50.

Arecoline is a potent stimulant alkaloid, and is ideal for use in fat burner and pre-workout products.  Put the world’s third most popular stimulant to work for you.