In Vivo Evaluation of a Gastro-Resistant HPMC-Based "Next Generation Enteric" Capsule
Invivo: Many orally dosed APIs are bioavailable only when formulated as an enteric dosage form to protect them from the harsh environment of the stomach. However, an enteric formulation is often accompanied with a higher development effort in the first place and the potential degradation of fragile APIs during the coating process. Ready-to-use enteric hard capsules would be an easily available alternative to test and develop APIs in enteric formulations, while decreasing the time and cost of process development. In this regard, Lonza Capsugel® Next Generation Enteric capsules offer a promising approach as functional capsules. The in vivo performance of these capsules was observed with two independent techniques (MRI and caffeine in saliva) in eight human volunteers. No disintegration or content release in the stomach was observed, even after highly variable individual gastric residence times (range 7.5 to 82.5 min), indicating the reliable enteric properties of these capsules. Seven capsules disintegrated in the distal part of the small intestine; one capsule showed an uncommonly fast intestinal transit (15 min) and disintegrated in the colon. The results for this latter capsule by MRI and caffeine appearance differed dramatically, whereas for all other capsules disintegrating in the small intestine, the results were very comparable, which highlights the necessity for reliable and complementary measurement methods. No correlation could be found between the gastric residence time and disintegration after gastric emptying, which confirms the robust enteric formulation of those capsules
Flexible-Dosage Development Strategies for Today's Clinical Landscape
January 8th 2025This executive summary focuses on dose-flexible manufacturing strategies and their role in drug development. Dose flexibility is increasingly important for early clinical studies, particularly in areas such as pediatric medicines and oncology. However, flexible dosing strategies are often neglected or not prioritized early in development. This presentation will focus on technical strategies that can help anticipate appropriate timing for implementation and how to do so cost effectively while adhering to required timelines.
Diving Deep into Carrier-Based Formulation and Process Optimization
December 23rd 2024Carrier-based formulations for dry powder inhalers are carefully designed to transport extremely small particles into the lungs. Jet milling can be used to micronize these particles, with both high and low shear mixing processes used to formulate mixtures capable of carrying the fine API particles into the deep lung. This paper looks at the requirements for pulmonary delivery via carrier-based inhaled powder formulations, and how jet milling can be used to manufacture effective and stable materials for these formulations
Molecular Properties of PROTACs and the Relationship to Formulation Design
December 20th 2024Analyzation of a diverse set of PROTAC (Proteolysis Targeting Chimeras – a class of TPDs) structures and their calculated properties, identifying key structure-property trends that contribute to low oral bioavailability.
Clinical Supply Planning in Europe - Balancing Cost, Flexibility and Time
December 19th 2024The packaging and distribution of clinical supplies is a fundamental piece to the overall success of a clinical trial, and advance preparation can help establish a more efficient supply chain. Selecting the best geographical location for those activities, however, depends on the clinical trial protocol, business decisions, and even the investigational medicinal product (IMP) being studied.
