In Vitro Dissolution Evidence for Delivering Multiple Vitamin-Mineral Ingredients past the Stomach by Novel Capsule Delivery System (P24-009-19). (13th June 2019) - Bucci, Luke
Abstract: Objectives: The ability of a novel beadlet-in-oil, gastric-resistant, vegetarian capsule containing a multiple vitamin-mineral (MVM) composition to deliver capsule contents past the stomach was tested by standard in vitro tablet disintegration procedures using magnesium as the marker of capsule contents dissolution. Methods: A novel capsule design using a gastric-resistant vegetarian hypromellose/gellan gum capsule (DRcaps®, Capsugel®) was tested for disintegration in a standard tablet disintegration apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. The MVM ingredients were encapsulated into size 0 Vcaps® (hypromellose with no gastric acid resistance) and DRcaps®. Individual capsules were placed into chambers containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.0) for an additional 300 minutes. Aliquots were tested for magnesium concentration at ten time points by atomic absorption spectrometry. Results: Magnesium was contained inside coated beadlets along with ferrous bisglycinate, methylcobalamin, 5-methyltetrahydrofolate, calcium fructoborate and cellulose. Vcaps® released 50% of the magnesium between 30–45 minutes and all by 60 minutes in the acid phase. DRcaps® released 25% of the magnesium at 45 minutes, and 43% at 120 minutes, followed by slow, steady release of the remaining magnesium by 420 minutes. Conclusions: These dissolution profiles reproduce the known, rapid disintegration profile of Vcaps® when wetted. DRcaps® released the majority of their contents after the pH was changed to intestinal conditions, and then the beadlets released the water-soluble ingredients (magnesium) in a linear manner over a two hour period. Since normal stomach emptying of DRcaps® without a meal is less than 20–30 minutes (previously shown), DRcap® MVMs bypass the stomach almost completely to release ingredients in the small intestine. Thus, a novel, beadlet-in-oil, gastric-resistant capsule delivered its contents past the stomach. These properties have the ability to improve tolerability and thus, compliance with users. Funding Sources: Capsugel®, Greenwood, SC, conducted this study for Ritual. Supporting Tables, Images and/or Graphs: