Supersaturation and Precipitation Applicated in Drug Delivery Systems: Development Strategies and Evaluation Approaches

Y Gan, JPA Baak, T Chen, H Ye, W Liao, H Lv, C Wen… - Molecules, 2023 - mdpi.com
Supersaturation is a promising strategy to improve gastrointestinal absorption of poorly
water-soluble drugs. Supersaturation is a metastable state and therefore dissolved drugs …

Revisiting supersaturation of a biopharmaceutical classification system IIB drug: Evaluation via a multi-cup dissolution approach and molecular dynamic simulation

Y Gan, Y Xu, X Zhang, H Hu, W Xiao, Z Yu, T Sun… - Molecules, 2023 - mdpi.com
As a subclass of the biopharmaceutical classification system (BCS) class II, basic drugs
(BCS IIB) exhibit pH-dependent solubility and tend to generate supersaturation in the …

Formulation predictive dissolution (fPD) testing to advance oral drug product development: An introduction to the US FDA funded '21st Century BA/BE'project

B Hens, PD Sinko, N Job, M Dean, J Al-Gousous… - International journal of …, 2018 - Elsevier
Over the past decade, formulation predictive dissolution (fPD) testing has gained increasing
attention. Another mindset is pushed forward where scientists in our field are more confident …

[HTML][HTML] A mechanistic physiologically-based biopharmaceutics modeling (PBBM) approach to assess the in vivo performance of an orally administered drug product …

M Bermejo, B Hens, J Dickens, D Mudie, P Paixão… - Pharmaceutics, 2020 - mdpi.com
The application of in silico modeling to predict the in vivo outcome of an oral drug product is
gaining a lot of interest. Fully relying on these models as a surrogate tool requires …

Posaconazole cocrystal with superior solubility and dissolution behavior

G Kuminek, KL Cavanagh, MFM da Piedade… - Crystal Growth & …, 2019 - ACS Publications
This work reports the first cocrystal of the basic drug posaconazole (PSZ). PSZ is poorly
water-soluble and has low and erratic bioavailability based on its large positive food effect …

Development of posaconazole nanosuspension for bioavailability enhancement: Formulation optimization, in vitro characterization, and pharmacokinetic study

T Kolipaka, S Sen, SS Mane, GD Bajad… - Journal of Drug Delivery …, 2023 - Elsevier
Abstract Posaconazole (PSZ), an anti-fungal drug, has broad-spectrum activity. But its action
is limited due to the poor solubility of posaconazole. The objective of the present study was …

Dose adjustment of venetoclax when co-administered with posaconazole: clinical drug–drug interaction predictions using a PBPK approach

S Bhatnagar, D Mukherjee, AH Salem, D Miles… - Cancer Chemotherapy …, 2021 - Springer
Purpose Venetoclax, a targeted anticancer agent approved for the treatment of chronic
lymphocytic leukemia and acute myeloid leukemia, is a substrate of cytochrome P450 (CYP) …

Hot melt extrusion technology for improved dissolution, solubility and “spring-parachute” processes of amorphous self-micellizing solid dispersions containing BCS II …

NQ Shi, SR Wang, Y Zhang, JS Huo, LN Wang… - European Journal of …, 2019 - Elsevier
Many strategies have been employed to improve oral drug delivery. One such approach
involves the use of supersaturable delivery systems such as amorphous self-micellizing …

[HTML][HTML] Biopredictive capability assessment of two dissolution/permeation assays, µFLUX™ and PermeaLoop™, using supersaturating formulations of Posaconazole

FL Holzem, A Weck, JP Schaffland, C Stillhart… - European Journal of …, 2022 - Elsevier
The majority of new drug entities exhibits poor water solubility and therefore enabling
formulations are often needed to ensure sufficient in vivo bioavailability upon oral …

PBPK modeling coupled with biorelevant dissolution to forecast the oral performance of amorphous solid dispersion formulations

A Kambayashi, T Kiyota, M Fujiwara… - European Journal of …, 2019 - Elsevier
The aim of this research was to develop an in silico modeling and simulation approach to
predict the oral performance of a poorly soluble drug candidate, T2CP, formulated as an …