Is the full potential of the biopharmaceutics classification system reached?

Biomimetic PVPA in vitro model for estimation of the intestinal drug permeability using fasted and fed state simulated intestinal fluids

“…An important point for a better prediction of a drug's performance in vivo is thus to use the biorelevant media to mimic the in vivo condition in the permeability test set up (Bergstrom et al, 2014). The PVPAbiomimetic model was selected as an in vitro model to better predict the GI absorption in the presence of FaSSIF and FeSSIF.…”

“…It is known that drugs from different classes might be affected differently in the presence of biorelevant fluids and also the presence of certain components in the GI fluid such as lecithin and bile salt (sodium taurocholate) might have a large impact on the solubility and permeability of poorly soluble compounds (Bergstrom et al, 2014;Dahan and Miller, 2012). Among the biorelevant media, FaSSIF and FeSSIF, first introduced in 1998 by Dressman and co-workers and later modified to better predict in vivo behavior of drugs, are the most utilized fluids originally applied as dissolution medium and later employed as medium in the permeability screening (Galia et al, 1998;Jantratid et al, 2008).…”

“…The PVPAbiomimetic established to be an intestinal mimicking barrier, has proven to be tremendously more robust towards the presence of tensides and co-solvents compared to the original PVPA (PVPAo), granting the model an enhanced ability to estimate the permeability of poorly soluble compounds. This is of great importance since many drug candidates today are suffering from poor water solubility (BCS class II or IV drugs) (Bergstrom et al, 2014).…”

Pharmaceutical Equivalence and Similarity Studies of Metoclopramide Tablets

“…For these products (typically solid oral dosage forms containing APIs with suitable properties), the similarity in in vitro dissolution profiles and excipient comparisons and riskbenefit analysis can be used to document equivalence of a multisource product with a comparator product and waive in vivo bioequivalence testing (4). This BCSbased biowaiver scheme has important advantages such as economic impact, time-saving, and avoidance of unnecessary testing in humans (3,6).…”

“…In this framework, the BCS serves as a tool to identify compounds eligible for biowaiver, which implies that in vivo proof of bioequivalence may be replaced by in vitro dissolution studies comparing test and reference product (5,6). The dissolution test, at first exclusively a quality control test, is now emerging as a surrogate equivalence test for certain categories of orally administered pharmaceutical products.…”