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Metabolic Study of Tetra-PEG-Based Hydrogel after Pelvic Implantation in Rats.
Molecules
September 2022
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
In vivo metabolism of polyethylene glycol (PEG) hydrogels has rarely been studied. In this study, we prepared a chemically crosslinked hydrogel formulation using 14C-labeled tetra-armed poly (ethylene glycol) succinimidyl succinate (Tetra-PEG-SS) and 3H-labeled crosslinking agent for implantation into the pelvis of Sprague-Dawley (SD) rats. This radioactive labeling technique was used to investigate the radioactivity excretion rates in of feces and urine, the blood exposure time curve, and the radioactivity recovery rate in each tissue over time.
View Article and Find Full Text PDFQualitative and quantitative prediction of human in vivo metabolic pathways in a human hepatocyte-murine stromal cell co-culture model.
Xenobiotica
December 2018
a Eli Lilly and Company, Lilly Corporate Centre, Indianapolis , IN , USA.
1. This study assessed the value of a static in vitro human hepatocyte-murine stromal cell co-culture model to qualitatively and quantitatively predict human in vivo metabolic clearance pathways using C-labeled test compounds and compared these results to an in vitro suspended human hepatocyte model and the in vivo human C ADME studies. 2.
View Article and Find Full Text PDFApplication of HPLC mixed-mode chromatography in determining radiochemical purity of [(14) C] labeled metformin hydrochloride.
J Labelled Comp Radiopharm
April 2015
Analytical and Process Chemistry, Merck Research Laboratories, Rahway, NJ, 07065, USA.
Metformin is currently prescribed worldwide to treat type 2 diabetes, and therefore, radiolabeled [(14) C] metformin is often prepared for clinical comparisons of new drug candidates. Prior to using the radiolabeled metformin, the purity needs to be determined to ensure the quality of the material. While typical reversed-phase LC methods are often the first choice for purity analysis, they are not suitable for this determination because the compound is poorly retained under these conditions.
View Article and Find Full Text PDFThe synthesis of 14C-labeled N-succinimidyl-3-maleimidopropionate, a linker molecule for PEGylated biologics.
J Labelled Comp Radiopharm
October 2014
Department of Chemical Synthesis, Radiochemistry Group, Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research and Development, P.O. Box 4000, Princeton, NJ, 08543, USA.
Carbon-14 labeled linker molecule, N-succinimidyl-3-maleimidopropionate was prepared for disposition studies of PEGylated biologics. Our new route started with 100 mCi of carbon-14 labeled Potassium cyanide (KCN) to prepare 55 mCi of [1-(14)C]N-succinimidyl-3-maleimidopropionate, 6 in five steps. This represents a multiple of 5.
View Article and Find Full Text PDFSyntheses of [14C]-labeled 2-(3-chlorophenyloxy)-3-[3-(3-hydroxy) pyridin-4-yl propoxy]pyridine, a phosphodiesterase 4 inhibitor and its metabolites.
J Labelled Comp Radiopharm
June 2014
Drug Research Division, Dainippon Sumitomo Pharma Co., Ltd., 33-94 Enoki-cho, Suita, Osaka, 564-0053, Japan.
We describe here the synthesis of [(14)C]-2-(3-chlorophenyloxy)-3-[3-(3-hydroxy)pyridin-4-yl propoxy]pyridine (1), a phosphodiesterase 4 inhibitor. [(14)C]-Labeled 1 was prepared in three steps from [(14)C]-2-bromopyridin-3-ol in an overall yield of 32%. Preparation of [(14)C]-labeled 2 and 3, two metabolites of 1, is also described.
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