Low Allicin Release from Garlic Supplements: a Major Problem Due to the Sensitivities of Alliinase Activity

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Abstract
Most garlic supplements are standardized on allicin potential and are enteric-coated to prevent gastric acid inactivation of the allicin-producing enzyme, alliinase. To determine whether these products release the claimed amount of allicin under simulated gastrointestinal conditions, USP dissolution method 724A for drug release was applied to all 24 known brands of enteric-coated tablets. It was found that nearly all brands employed effective coatings and that they met their claims for allicin potential when crushed and suspended in water. However, all brands except one gave low dissolution allicin release, with 83% of the brands releasing less than 15% of their potential. The low allicin release was found to be due to both impaired alliinase activity, mostly caused by tablet excipients, and to slow tablet disintegration, which also impairs alliinase activity. Only when tablets had high alliinase activity and disintegrated rapidly did they show high allicin release. The ability of USP 724A to estimate allicin release in vivo was validated by monitoring breath levels of the allicin metabolite, allyl methyl sulfide. In conclusion, garlic powder supplements should no longer be standardized on allicin potential, but rather on dissolution allicin release. Keywords: Garlic; allium sativum; allicin; alliinase; serum cholesterol; dissolution; enteric-coated