Tegaserod, a serotonin agonist, has been shown to have prokinetic effects in horses, but pharmacokinetic information is not currently available. The pharmacokinetics and in vitro effects of tegaserod were evaluated. Tegaserod increased the contractile activity of smooth muscle preparations of the equine pelvic flexure. Pertinent pharmacokinetic parameters for a single IV and oral dose were determined. Therapeutic plasma concentrations of tegaserod were achieved by a single oral dose at 0.27 mg/kg. These findings indicate that further clinical studies are warranted to investigate potential benefits in cases of functional gastrointestinal motility disorders in horses.
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Sci Rep
January 2025
School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, P.R. China.
Hawthorn leave flavonoids (HLF) are widely used as an herb or dietary supplements for cardio-cerebrovascular diseases. However, its gastrointestinal absorption behavior and mechanism have not been disclosed. In this study, gastrointestinal absorption and its regulation of 4''-O-glucosylvitexin (GLV), 2''-O-rhamnosylvitexin (RHV), vitexin (VIT), rutin (RUT) and hyperoside (HP) in HLF were investigated using in vitro, in situ and in vivo models.
View Article and Find Full Text PDFEur J Med Chem
December 2024
School of Pharmacy and Food Engineering, Wuyi University, 529020, Jiangmen, China; Department of Chemistry, University of Liverpool, L69 7ZD, Liverpool, UK. Electronic address:
Aryl quinolone derivatives can target the cytochrome bc complex of Plasmodium falciparum, exhibiting excellent in vitro and in vivo antimalarial activity. However, their clinical development has been hindered due to their poor aqueous solubility profiles. In this study, a series of bioisosteres containing saturated heterocycles fused to a 4-pyridone ring were designed to replace the inherently poorly soluble quinolone core in antimalarial quinolones with the aim to reduce π-π stacking interactions in the crystal packing solid state, and a synthetic route was developed to prepare these alternative core derivatives.
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January 2025
Department of Parasitology and Mycology, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran.
Medical and surgical treatments for cystic echinococcosis (CE) are challenged by various complications. This study evaluates in vitro protoscolicidal activity of piperine-loaded mesoporous silica nanoparticles (PIP-MSNs) against protoscoleces of Echinococcus granulosus. MSNs were prepared by adding tetraethyl orthosilicate to cetyltrimethylammonium bromide and NaOH, and then loaded with PIP.
View Article and Find Full Text PDFInt J Pharm
December 2024
Guangdong Provincial Key Laboratory for Research and Evaluation of Pharmaceutical Preparations, College of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, PR China. Electronic address:
Pharmacol Res
December 2024
State Key Laboratory of Traditional Chinese Medicine Syndrome, Guangdong Key Laboratory for Translational Cancer Research of Chinese Medicine, International Institute for Translational Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510006, China; Chinese Medicine Guangdong Laboratory, Guangdong Hengqin, China. Electronic address:
Wogonin is a flavonoid with efficacy in ulcerative colitis (UC), while the mechanism of its action remains to be fully elucidated. Previous research has indicated that the activation of the triple recycling pathway significantly enhances the bioavailability of flavonoids. The efflux transporters, BCRP and MRP2 are critical regulatory molecules within the enterohepatic triple recycling pathways.
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