Predicting impact of food and feeding time on oral absorption of drugs with a novel rat continuous intestinal absorption model was written by Radice, Casey;Korzekwa, Ken;Nagar, Swati. And the article was included in Drug Metabolism & Disposition in 2022.Application of 10238-21-8 This article mentions the following:
Intricacies in intestinal physiol., drug properties, and food effects should be incorporated into models to predict complex oral drug absorption. A previously published human continuous intestinal absorption model based on the convection-diffusion equation was modified specifically for the male Sprague-Dawley rat in this report. Species-specific physiol. conditions along intestinal length – exptl. velocity and pH under fasted and fed conditions, were measured and incorporated into the intestinal absorption model. Concentration-time (C-t) profiles were measured upon a single i.v. and peroral (PO) dose for three drugs: amlodipine (AML), digoxin (DIG), and glyburide (GLY). Absorption profiles were predicted and compared with exptl. collected data under three feeding conditions: 12-h fasted rats were provided food at two specific times after oral drug dose (1 h and 2 h for AML and GLY; 0.5 h and 1 h for DIG), or they were provided food for the entire study. I.v. vs. PO C-t profiles suggested absorption even at later times and informed design of appropriate math. input functions based on exptl. feeding times. With this model, AML, DIG, and GLY oral C-t profiles for all feeding groups were generally well predicted, with exposure overlap coefficients in the range of 0.80-0.97. Efflux transport for DIG and uptake and efflux transport for GLY were included, modeling uptake transporter inhibition in the presence of food. Results indicate that the continuous intestinal rat model incorporates complex physiol. processes and feeding times relative to drug dose into a simple framework to provide accurate prediction of oral absorption. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8Application of 10238-21-8).
5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Application of 10238-21-8
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics