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The Journal of Orthomolecular Medicine Vol. 16, 1st Quarter 2001

ABSTRACT

Are There Merits in Sustained-Release Preparations?

E. CHERASKIN, M.D., D.M.D.


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There is no question that the most common way most people take their vitamins is indeed the worst way, namely, throwing down one's vitamins first thing in the morning (often with hostility). This is the basis for the oft-heard comment that " taking vitamins will only give you expensive urine." It is for that and many other reasons that there have been attempts through the years to put medicaments in general, and for our purposes here vitamin C in particular, into timed- or sustained-release form.

There are a number of these types of formulations available today. The general effort has been to develop delayed, sustained- release principles with the assumption that longer intestinal transit would result in continued increased absorption. Our particular studies dealt with the "Spansule" concept which consisted of a core of sugar and starch to which a vitamin was applied. This then was surrounded by semi-permeable coatings that were tailor made blends of selected waxes and fats whose precise composition was dictated by the physicochemical characteristics of the particular substance to be delivered. Moisture permeated the shell by osmosis and the core became swollen, eventually rupturing the crust. The phenomenon of sustained- or timed-release was based on the rate of moisture permeation into hundreds of pellets with layers of various thicknesses. The thinner envelopes were found to be more permeable and ruptured first, while the thicker coatings which were progressively less porous, were delayed in their time of rupture.


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