Supplement excipients

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Excipients derived from various sources

Plant based

Microcrystalline cellulose

  • A wood pulp fibre that is indigestible to humans (6)
  • Some studies have shown benefits for improving bowel evacuation in men and women (7)

Carbohydrates

Starch

  • Starch, a carbohydrate polymer (8), is a polysaccharide that is converted to glucose, used as a bulking agent
  • Starches absorb water rapidly allowing tablets to disintegrate appropriately (9)
  • May be sourced from tapioca, rice, corn or wheat
  • Corn may be GMO or non-GMO sourced, caution for those with allergy
  • Rice (oryza sativa) is low allergen (8), a unique filler, binder (11)
  • Tapioca (Manihot esculanta) is gluten free, an alternative to corn and wheat (12)

Maltodextrin

  • Maltodextrins (MDs) are a class of carbohydrates extracted from a range of botanical sources
  • Maltodextrin exists in either a digestible or a digestion-resistant form (14)
  • They are industrially produced by enzymatic or acid hydrolysis of the starch, followed by purification and spray drying (13)
  • Glucose from digested maltodextrins is rapidly absorbed in the small intestine which raises questions about potential effects on metabolism and health (13)

Further research on the benefits and side effects of maltodextrin is needed

Fruit extracts

Thaumatococcus danielli fruit

  • A plant native to Africa
  • Protein sweetener for palatability, evoking a sweet taste with low calorie value
  • Unlike sucrose, does not trigger a demand for insulin in diabetic individuals (15)

Stevia rebaudiana

  • Zero calorie sweetener with a low carbon footprint  extracted from a South American plant  (16)

Dehydrated coconut water (drupe)

  • Dehydrated coconut water (organic/non-organic)
  • Naturally occurring, rich in potassium, contains sodium, chloride, and carbohydrate
  • Hydrating beverage of choice in certain parts of the world (17)

Pectin

  • A soluble fibre found in berries, apples, and other fruit, can act as a sweetener or as a filler
  • Pectin as a dietary fibre has been demonstrated to have different immune effects depending on its chemical composition (18)
  • Pectin has many potential health benefits, including (18):
    • Binds and inhibits toll-like receptor 2 (TLR2) and specifically inhibits the proinflammatory TLR2–TLR1 pathway
    • Widely consumed dietary fibre having immunomodulatory effects
    • Dietary effects of pectin have been shown to be effective against endotoxin-induced inflammation, allergic airway inflammation, colitis, pancreatitis and in supporting colonic anastomosis healing in various animal models

Herbal extracts

  • Vanilla: Sweetener, derived from vanilla bean pods
  • Cinnamomum cassia (Cinnamon) powder: Sweetener, organic/non-organic
  • Orange oil: Pressed oil from orange peel is used as a flavour masker
  • Peppermint oil: Flavouring agent to mask the unpleasant smell of B vitamins or to improve compliance

Lecithin

  • A mixture of phospholipids and oil
  • Phospholipids are a component of the cell membrane in all plants and animals, but lecithin is most often derived from sunflower kernels, rapeseed (canola), milk, soy, and egg yolks (19)
  • May help transport fat-soluble drugs and nutrients across fat insoluble cell membranes. Curcumin for example, has shown enhanced absorption when delivered with lecithin (18)
  • Conversion into phytosomes (complex of a natural active ingredient and a phospholipid) improves efficacy without compromising safety (20)
  • Soy allergies are triggered by soy proteins. An allergic response to soy depends on its protein content. Soy lecithin contains very little soy protein, and lecithin from some sources contains no detectable protein at all (20)

Chlorophyll

A natural green dye made from chlorella algae. Used as a colouring agent and a deodorant (21)

Citric acid

  • Flavour enhancer, preservative
  • May be sourced from citrus, non-GMO corn or synthetically produced
  • In rare cases, mould residues from the manufacturing process may trigger allergies in rare cases. Is generally deemed safe. More research is needed
  • An organic compound found in many fruits. It was first identified in apple juice and named after the Latin word for apple, mālum (22)

Malic acid

  • Sour flavour enhancer, highly water soluble
  • Antimicrobial effect due to a lowering of the pH (23)
  • According to a study with 24 patients, a supplement containing malic acid (200mg) and magnesium (50 mg) may improve pain and tenderness associated with fibromyalgia, but only when taken for at least 6 months (24)
  • It is unclear what a safe and effective dose of malic acid is in most cases due to a lack of research

Animal

Gelatin

  • Animal protein from cow or pig
  • Gelling agent used to assist coating the outside of capsules making them easier to swallow
  • World Health Organisation (WHO) has ruled that gelatin has been transformed to such an extent from its original source, it is permissible for those with religious dietary restrictions (25)

Lactose

  • A disaccharide sugar present in milk and used as a binder and a diluent (26)
  • May cause gastro-intestinal upset in individuals sensitive to milk products or those lactose intolerant
  • The amount required to cause GIT upset is often very low

Mineral

Calcium phosphate

  • Binder and filler with flowability and compressibility (27)
  • Assists in formulation flow and resists the uptake of moisture, thus reducing the risk of poor stability
  • Inorganic substances of mineral origin are generally recognized as safe

Colloidal anhydrous silica

  • Synthetically made from sodium silicate
  • Adsorbent, disintegrant or glidant, to allow powder to flow freely when tablets are processed (28)

Sodium bicarbonate (baking soda)

  • Naturally occurring inorganic mineral, a buffer used to stabilize pH (29)
  • To be listed only as excipients
  • Sodium bicarbonate contains 27% sodium (1 mg sodium bicarbonate = 0.27 mg sodium)

 Synthetic

Nature identical flavours – vanilla, peppermint

  • Obtained by synthesis or isolated through chemical processes, which are chemically and organoleptically (taste, sight, smell, touch) identical to flavouring substances naturally present in products intended for human consumption
  • Used for flavour consistency, do not contain amines
  • Chemically identical to a substance naturally present in material of vegetable or animal origin
  • They cannot contain any artificial flavouring substances

Betaine hydrochloride (HCl)

  • Promotes optimal gastric lumen acidity. Large amounts of betaine HCl may cause stomach irritation (30)
  • Individuals with a history of peptic ulcers, gastritis, or gastrointestinal symptoms should consult their physician before taking betaine HCl

Glycine

  • Nonessential amino acid, sweetener, derived from natural or synthetic sources
  • Used as an emollient, emulsifying agent and solubilizing agent to improve gastric absorption of the supplement
  • Larger doses of glycine promotes both inhibitory and excitatory functions within the CNS (31)

Glycerine (glycerol)

  • A sugar alcohol often found in herbal extract tinctures
  • Sweetener and preservative with antimicrobial properties, useful alternative to ethanol
  • Prevents tannins, which can bind to plant proteins and impede proper digestion, from forming in plant extracts
  • Low glycaemic index

Enteric coated capsules

  • A barrier that controls the location of oral medication in the digestive system where it is absorbed
  • The word “enteric” indicates small intestine; therefore enteric coatings prevent release of medication before it reaches the small intestine
  • Materials used for enteric coatings include the following polymers: Cellulose acetate phthalate CAP, Poly(vinyl acetate phthalate) PVAP, fatty acids, waxes, shellac, plastics and plant fibres (32)

Genetically Modified Organism (GMO)

  • Common example: GMO corn and soy
  • Unpredictable side effects, not much is known regarding long-term effects on humans (33)

Titanium dioxide (TiO2)

  • Whitening agent, pro-oxidant
  • Considered an inert and safe material and has been used in many applications for decades
  • Although TiO2 is permitted as an additive (E171) in food and pharmaceutical products there is no reliable data on its absorption, distribution, excretion and toxicity on oral exposure (34)

Artificial colourants / synthetic dyes

  • Tartrazine, a yellow colouring agent used in some supplements and pharmaceuticals is the most common food colouring additive
  • It has been shown to cause adverse reactions in certain individuals
  • It is well known to cause asthma and urticaria in sensitive individuals and has been shown to cause behavioural changes such as irritability, restlessness, and sleep disturbance in children (35)

Artificial sweeteners

  • Synthetic sugar substitutes defined by the criterion that the flavouring substance is not chemically identical to a substance naturally present in materials of vegetable or animal origin
  • Examples include aspartame, saccharin or high fructose corn syrup and sucralose
  • Aspartame is a synthetic dipeptide formed by the reaction of L-aspartic acid with L-phenylalanine methyl ester (36). Safety studies are primarily based on animal models. The data is controversial and further research is required. Recent animal studies and the limited human studies show aspartame and its metabolites consumed within the recommended “safe” levels may induce oxidative stress and  damage cell membrane integrity (37)
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References
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