In Vitroin Vivo Correlation of the Effect of Supersaturation on the Intestinal Absorption of BCS Class 2 Drugs

H Higashino, T Hasegawa, M Yamamoto… - Molecular …, 2014 - ACS Publications
The aim of this study was to establish an in vitro method for evaluating the effect of
supersaturation on oral absorption of poorly water-soluble drugs in vivo. Albendazole …

In vitro and in vivo assessment of the potential of supersaturation to enhance the absorption of poorly soluble basic drugs

J Li, Y Bukhtiyarov, N Spivey, C Force… - Journal of …, 2020 - Springer
Purpose Delaying precipitation of weakly basic drugs in supersaturated state following their
transition from the acidic gastric environment to the near-neutral proximal small intestinal …

In vitro assessment of supersaturation/precipitation and biological membrane permeation of poorly water-soluble drugs: a case study with albendazole and …

M Kataoka, S Takeyama, K Minami, H Higashino… - Journal of …, 2019 - Elsevier
This study aimed to elucidate the relationship between supersaturation and precipitation
and the effect of a supersaturated state on drug membrane permeation. Stock solutions of …

Quantitative analysis of the effect of supersaturation on in vivo drug absorption

R Takano, N Takata, R Saito, K Furumoto… - Molecular …, 2010 - ACS Publications
The purpose of this study is to clarify the effects of intestinal drug supersaturation on
solubility-limited nonlinear absorption. Oral absorption of a novel farnesyltransferase …

In Vitro, in Silico, and in Vivo Assessments of Intestinal Precipitation and Its Impact on Bioavailability of a BCS Class 2 Basic Compound

D Kou, C Zhang, H Yiu, T Ng, JW Lubach… - Molecular …, 2018 - ACS Publications
In this study, a multipronged approach of in vitro experiments, in silico simulations, and in
vivo studies was developed to evaluate the dissolution, supersaturation, precipitation, and …

Supersaturation–nucleation behavior of poorly soluble drugs and its impact on the oral absorption of drugs in thermodynamically high-energy forms

S Ozaki, T Minamisono, T Yamashita, T Kato… - Journal of …, 2012 - Elsevier
In order to better understand the oral absorption behavior of poorly water-soluble drugs,
their supersaturation–nucleation behavior was characterized in fasted state simulated …

Gastrointestinal behavior of itraconazole in humans–Part 1: Supersaturation from a solid dispersion and a cyclodextrin-based solution

J Brouwers, S Geboers, R Mols, J Tack… - International journal of …, 2017 - Elsevier
This study evaluated the fasted state gastrointestinal behavior of the lipophilic drug
itraconazole, orally administered to healthy volunteers as either a solid dispersion …

In vivo evaluation of supersaturation/precipitation/re-dissolution behavior of cinnarizine, a lipophilic weak base, in the gastrointestinal tract: the key process of oral …

Y Tanaka, A Kawakami, A Nanimatsu, M Horio… - European Journal of …, 2017 - Elsevier
The aim of this study is to evaluate how supersaturation, precipitation, and re-dissolution
processes influence the intestinal absorption of cinnarizine (CNZ), a lipophilic weak base, by …

Evaluating the predictability of the in vitro transfer model and in vivo rat studies as a surrogate to investigate the supersaturation and precipitation behaviour of different …

A Ruff, R Holm, ES Kostewicz - European Journal of Pharmaceutical …, 2017 - Elsevier
The present study investigated the ability of the in vitro transfer model and an in vivo
pharmacokinetic study in rats to investigate the supersaturation and precipitation behaviour …

The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system …

Y Tsume, K Matsui, AL Searls, S Takeuchi… - European Journal of …, 2017 - Elsevier
The development of formulations and the assessment of oral drug absorption for
Biopharmaceutical Classification System (BCS) class IIb drugs is often a difficult issue due to …