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Article

The Effect of Capsule-in-Capsule Combinations on In Vivo Disintegration in Human Volunteers: A Combined Imaging and Salivary Tracer Study

1
Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, 17489 Greifswald, Germany
2
Department of Diagnostic Radiology and Neuroradiology, University Hospital Greifswald, 17475 Greifswald, Germany
3
Department of Clinical Pharmacology, University Hospital Greifswald, 17487 Greifswald, Germany
4
Lonza Capsules & Health Ingredients, Morristown, NJ 07960, USA
5
Lonza Capsules & Health Ingredients, 68000 Colmar, France
*
Author to whom correspondence should be addressed.
Academic Editor: Thierry Vandamme
Pharmaceutics 2021, 13(12), 2002; https://doi.org/10.3390/pharmaceutics13122002
Received: 11 October 2021 / Revised: 12 November 2021 / Accepted: 23 November 2021 / Published: 25 November 2021
Controlling the time point and site of the release of active ingredients within the gastrointestinal tract after administration of oral delivery systems is still a challenge. In this study, the effect of the combination of small capsules (size 3) and large capsules (size 00) on the disintegration site and time was investigated using magnetic resonance imaging (MRI) in combination with a salivary tracer technique. As capsule shells, Vcaps® HPMC capsules, Vcaps® Plus HPMC capsules, gelatin and DRcaps® designed release capsules were used. The three HPMC-based capsules (Vcaps®, Vcaps® Plus and DRcaps® capsules) were tested as single capsules; furthermore, seven DUOCAP® capsule-in-capsule combinations were tested in a 10-way crossover open-label study in six healthy volunteers. The capsules contained iron oxide and hibiscus tea powder as tracers for visualization in MRI, and two different caffeine species (natural caffeine and 13C3) to follow caffeine release and absorption as measured by salivary levels. Results showed that the timing and location of disintegration in the gastrointestinal tract can be measured and differed when using different combinations of capsule shells. Increased variability among the six subjects was observed in most of the capsule combinations. The lowest variability in gastrointestinal localization of disintegration was observed for the DUOCAP® capsule-in-capsule configuration using a DRcaps® designed release capsule within a DRcaps® designed release outer capsule. In this combination, the inner DRcaps® designed release capsule always opened reliably after reaching the ileum. Thus, this combination enables targeted delivery to the distal small intestine. Among the single capsules tested, Vcaps® Plus HPMC capsules showed the fastest and most consistent disintegration. View Full-Text
Keywords: MRI; salivary tracer; DUOCAP®; capsule-in-capsule; HPMC; in vivo disintegration; site-specific drug delivery MRI; salivary tracer; DUOCAP®; capsule-in-capsule; HPMC; in vivo disintegration; site-specific drug delivery
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MDPI and ACS Style

Rump, A.; Weiss, F.N.; Schulz, L.; Kromrey, M.-L.; Scheuch, E.; Tzvetkov, M.V.; White, T.; Durkee, S.; Judge, K.W.; Jannin, V.; Bellamine, A.; Weitschies, W.; Grimm, M. The Effect of Capsule-in-Capsule Combinations on In Vivo Disintegration in Human Volunteers: A Combined Imaging and Salivary Tracer Study. Pharmaceutics 2021, 13, 2002. https://doi.org/10.3390/pharmaceutics13122002

AMA Style

Rump A, Weiss FN, Schulz L, Kromrey M-L, Scheuch E, Tzvetkov MV, White T, Durkee S, Judge KW, Jannin V, Bellamine A, Weitschies W, Grimm M. The Effect of Capsule-in-Capsule Combinations on In Vivo Disintegration in Human Volunteers: A Combined Imaging and Salivary Tracer Study. Pharmaceutics. 2021; 13(12):2002. https://doi.org/10.3390/pharmaceutics13122002

Chicago/Turabian Style

Rump, Adrian, Franziska N. Weiss, Louisa Schulz, Marie-Luise Kromrey, Eberhard Scheuch, Mladen V. Tzvetkov, Tyler White, Shane Durkee, Kevin W. Judge, Vincent Jannin, Aouatef Bellamine, Werner Weitschies, and Michael Grimm. 2021. "The Effect of Capsule-in-Capsule Combinations on In Vivo Disintegration in Human Volunteers: A Combined Imaging and Salivary Tracer Study" Pharmaceutics 13, no. 12: 2002. https://doi.org/10.3390/pharmaceutics13122002

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