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Solid Self-Microemulsifying Drug Delivery System for Improved Oral Bioavailability of Relugolix: Preparation and Evaluation.
Int J Nanomedicine
January 2025
School of Pharmacy, Jiangxi Medical College, Nanchang University, Nanchang, 330006, People's Republic of China.
Purpose: To improve the oral absorption of relugolix (RLGL), which has low oral bioavailability due to its low solubility and being a substrate of P-glycoprotein (P-gp). A solid self-microemulsifying drug delivery system of relugolix (RLGL-S-SMEDDS) was prepared and evaluated in vitro and in vivo.
Methods: The composition of the solid self-microemulsifying drug delivery system (S-SMEDDS) was selected by solubility study and pseudo-ternary phase diagram, and further optimized by Design-Expert optimization design.
Potential and challenges in application of physiologically based pharmacokinetic modeling in predicting diarrheal disease impact on oral drug pharmacokinetics.
Drug Metab Dispos
January 2025
Department of Pharmaceutics, University of Washington, Seattle, Washington. Electronic address:
Physiologically based pharmacokinetic (PBPK) modeling is a physiologically relevant approach that integrates drug-specific and system parameters to generate pharmacokinetic predictions for target populations. It has gained immense popularity for drug-drug interaction, organ impairment, and special population studies over the past 2 decades. However, an application of PBPK modeling with great potential remains rather overlooked-prediction of diarrheal disease impact on oral drug pharmacokinetics.
View Article and Find Full Text PDFHuman enteroid monolayers: A novel, functionally stable model for investigating oral drug disposition.
Drug Metab Dispos
January 2025
Department of Pharmaceutics, School of Pharmacy, University of Washington, Seattle, Washington. Electronic address:
To further the development of an in vitro model that faithfully recapitulates drug disposition of orally administered drugs, we investigated the utility of human enteroid monolayers to simultaneously assess intestinal drug absorption and first-pass metabolism processes. We cultured human enteroid monolayers from 3 donors, derived via biopsies containing duodenal stem cells that were propagated and then differentiated atop permeable Transwell inserts, and confirmed transformation into a largely enterocyte population via RNA sequencing analysis and immunocytochemistry (ICC) assays. Proper cell morphology was assessed and confirmed via bright field microscopy and ICC imaging of tight junction proteins and other apically and basolaterally localized proteins.
View Article and Find Full Text PDFIntegrative RNA, miRNA, and 16S rRNA sequencing reveals immune-related regulation network for glycinin-induced enteritis in hybrid yellow catfish, ♀ × ♂.
Front Immunol
January 2025
College of Fisheries, Key Lab of Freshwater Animal Breeding, Ministry of Agriculture, Huazhong Agricultural University, Wuhan, Hubei, China.
Glycinin-induced foodborne enteritis is a significant obstacle that hinders the healthy development of the aquatic industry. Glycinin causes growth retardation and intestinal damage in hybrid yellow catfish ( ♀ × ♂), but its immune mechanisms are largely unknown. In the current study, five experimental diets containing 0% (CK), 1.
View Article and Find Full Text PDFCocoa Seeds as a Phytobezoar Causing Intestinal Obstruction in a Ghanaian Child: A Case Report.
Cureus
December 2024
Emergency Medicine Department, Komfo Anokye Teaching Hospital, Kumasi, GHA.
Phytobezoars are indigestible organic matter that forms organized masses in the gastrointestinal tract. Seeds reported causing bezoars include sunflower seeds, watermelon seeds, and wild banana seeds. Cocoa seeds causing bezoar have not been reported.
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