ADME in Nutraceuticals: How Absorption, Distribution, Metabolism, and Excretion Define Supplement Effectiveness

Uncover the pharmacokinetic science of nutraceuticals – from gastrointestinal absorption to metabolic bioavailability and systemic nutrient fate.

ADME in Nutraceuticals – The Pharmacokinetic Science Behind Bioavailability

In the nutraceutical industry, “absorption” is often discussed, but true efficacy is governed by ADME – Absorption, Distribution, Metabolism, and Excretion.

While drugs undergo rigorous pharmacokinetic profiling, supplements often lack such quantitative scrutiny. SKD Pharmaceuticals approaches supplement design as pharmacologically active nutrition, where molecular behaviour in vivo dictates biological impact.

Absorption – Crossing the Biological Threshold

Most nutrients are absorbed through enterocyte-mediated mechanisms in the small intestine.

Liposoluble compounds (e.g. vitamins A, D, E, K) depend on micellar solubilisation via bile acids; hydrosoluble vitamins use sodium-dependent co-transporters.

However, bioavailability is frequently impaired by poor dissolution kinetics, first-pass metabolism, or competitive absorption (e.g., zinc–iron antagonism).

Pharmaceutical encapsulation technologies – liposomal, cyclodextrin inclusion, or phospholipid complexation – now enhance nutrient diffusion and retention.

Distribution – Beyond the Plasma Pool

After absorption, nutrients distribute into distinct compartments – plasma, interstitial fluid, intracellular stores.

Lipophilic compounds bind extensively to albumin or lipoproteins, while hydrophilic micronutrients remain plasma-restricted.

The volume of distribution (Vd) determines whether a compound achieves tissue-specific targeting. For instance, curcumin, with its poor aqueous solubility and high protein binding, demonstrates a paradoxically high Vd but low plasma retention – explaining its low systemic efficacy unless nanocarrier-enhanced.

H2: Metabolism – The Double-Edged Sword of Biotransformation

Phase I metabolism (oxidation/reduction via CYP450 enzymes) and Phase II conjugation (glucuronidation, sulfation) alter both activity and half-life.

Polyphenols such as resveratrol undergo extensive first-pass glucuronidation, leaving <1% as free aglycone in circulation.

Advances in nutrigenomics now explore enzyme polymorphisms (CYP2D6, UGT1A1) that determine individual variation in nutrient metabolism — the foundation of precision supplementation.

H2: Excretion – The Forgotten Pharmacokinetic Phase

Nutrients are excreted renally (hydrosoluble) or via bile/faeces (lipophilic). Renal clearance depends on glomerular filtration and tubular reabsorption, often influenced by pH and transporter expression (e.g., OAT, OCT).

Magnesium, for example, demonstrates biphasic kinetics, where intracellular stores buffer serum concentrations, complicating correlation between intake and measurable plasma levels.

The SKD Approach to Nutrient Pharmacokinetics

SKD Pharmaceuticals integrates ADME profiling into every supplement design phase — employing in silico modelling, dissolution testing, and bioequivalence simulation to predict bioavailability.

Our R&D philosophy views supplements as biophysically active formulations, not passive nutrition.

Through formulation engineering (liposomal encapsulation, micronisation, controlled release matrices), SKD maximises biological access and retention – ensuring measurable efficacy rather than theoretical benefit.

In the future, AI-driven nutrikinetic mapping and wearable biosensor feedback loops will redefine supplement science from population averages to personalised pharmaconutrition – an innovation frontier SKD actively pursues.