TY - JOUR
TI - Unraveling the behavior of oral drug products inside the human gastrointestinal tract using the aspiration technique: History, methodology and applications
AU - Augustijns, P.
AU - Vertzoni, M.
AU - Reppas, C.
AU - Langguth, P.
AU - Lennernäs, H.
AU - Abrahamsson, B.
AU - Hasler, W.L.
AU - Baker, J.R.
AU - Vanuytsel, T.
AU - Tack, J.
AU - Corsetti, M.
AU - Bermejo, M.
AU - Paixão, P.
AU - Amidon, G.L.
AU - Hens, B.
JO - EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
PY - 2020
VL - 155
TODO - null
SP - null
PB - Elsevier B.V.
SN - 0928-0987
TODO - 10.1016/j.ejps.2020.105517
TODO - abiraterone acetate;  amprenavir;  atazanavir;  diclofenac potassium;  fenofibrate;  fosamprenavir;  ibuprofen;  indinavir;  itraconazole;  mesalazine;  paracetamol;  paromomycin;  posaconazole;  ritonavir;  simvastatin;  tenofovir disoproxil;  theophylline, aspiration;  computer model;  drug absorption;  drug formulation;  drug release;  drug solubility;  gastrointestinal tract;  history;  human;  in vitro study;  lower gastrointestinal tract;  methodology;  nuclear magnetic resonance imaging;  plasma concentration-time curve;  precipitation;  priority journal;  product development;  Review;  stomach motility;  upper gastrointestinal tract
TODO - Fluid sampling from the gastrointestinal (GI) tract has been applied as a valuable tool to gain more insight into the fluids present in the human GI tract and to explore the dynamic interplay of drug release, dissolution, precipitation and absorption after drug product administration to healthy subjects. In the last twenty years, collaborative initiatives have led to a plethora of clinical aspiration studies that aimed to unravel the luminal drug behavior of an orally administered drug product. The obtained drug concentration-time profiles from different segments in the GI tract were a valuable source of information to optimize and/or validate predictive in vitro and in silico tools, frequently applied in the non-clinical stage of drug product development. Sampling techniques are presently not only being considered as a stand-alone technique but are also used in combination with other in vivo techniques (e.g., gastric motility recording, magnetic resonance imaging (MRI)). By doing so, various physiological variables can be mapped simultaneously and evaluated for their impact on luminal drug and formulation behavior. This comprehensive review aims to describe the history, challenges and opportunities of the aspiration technique with a specific focus on how this technique can unravel the luminal behavior of drug products inside the human GI tract by providing a summary of studies performed over the last 20 years. A section ‘Best practices’ on how to perform the studies and how to treat the aspirated samples is described. In the conclusion, we focus on future perspectives concerning this technique. © 2020 The Author(s)
ER -