1. An altered functional state of liver due to experimental cholestasis could result in a change in the biotransformation of drugs. The aim of this study was to evaluate an influence of obstructive cholestasis on the pharmacokinetics of phenazone (antipyrine). 2. The investigation was carried out on male rabbits, randomly allocated into two groups: shamoperated and animals with biliary ducts ligation. Phenazone was administered intragastrically as a probe of drug metabolism. 3. Measurements, i.e. laboratory and pharmacodynamic tests, as well as pharmacokinetic assays, were performed before the operation as well as 10-12 days after the bile duct ligation. At the end of the study livers were examined macro- and microscopically and biochemical analysis of the liver microsomes was performed. 4. The measured pharmacokinetic parameters suggested an impaired biotransformation of phenazone in animals with obstructive cholestasis, leading to a slower drug elimination.
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http://dx.doi.org/10.1111/j.1476-5381.1996.tb15146.x | DOI Listing |
Micromachines (Basel)
November 2024
Department of Metabolic Health Research, Netherlands Organisation for Applied Scientific Research (TNO), 2333 BE Leiden, The Netherlands.
Background: To accurately measure permeability of compounds in the intestine, there is a need for preclinical in vitro models that accurately represent the specificity, integrity and complexity of the human small intestinal barrier. Intestine-on-chip systems hold considerable promise as testing platforms, but several characteristics still require optimization and further development.
Methods: An established intestine-on-chip model for tissue explants was adopted for intestinal cell monolayer culture.
Eur J Pharm Biopharm
December 2024
Laboratory of Pharmaceutical Technology, Kobe Pharmaceutical University, 4-19-1 Motoyamakitamachi, Higashinada-ku, Kobe, Hyogo 658-8558, Japan.
Despite the potential benefits of nasal drug delivery, there is a need for a systematic evaluation of the efficacy of powder formulations adhering to the nasal mucosa. This study aims to establish a systematic evaluation method for nasal drug absorption from powder formulations. We selected three model compounds-antipyrine, griseofulvin, and acyclovir-and analyzed their pharmacokinetics following nasal administration of powder formulations under physiological conditions.
View Article and Find Full Text PDFEpilepsy Behav
January 2025
Albert Einstein College of Medicine, Saul R. Korey Department of Neurology, Laboratory of Developmental Epilepsy, Albert Bronx, NY, USA; Isabelle Rapin Division of Child Neurology, Albert Einstein College of Medicine, Bronx, NY, USA; Dominick P Purpura Department of Neuroscience, Albert Einstein College of Medicine, Bronx, NY, USA. Electronic address:
Objective: To test whether anti-inflammatory and antioxidant drugs that inhibit the nuclear factor kappa light chain enhancer of activated B cells (NF-kB), celastrol and edaravone, suppress spasms and improve developmental outcomes in the multiple-hit rat model of refractory infantile spasms (IS) due to structural lesions.
Methods: Postnatal day 3 (PN3) Sprague-Dawley rats were treated according to the multiple-hit IS model protocol. Using a randomized, blinded, vehicle-controlled, dose- and time-response study design, we tested the effects of single celastrol [1, 2, or 4 mg/kg intraperitoneally (i.
J Pharm Sci
November 2024
Faculty of Pharmaceutical Sciences, Setsunan University, 45-1 Nagaotoge-cho, Hirakata, Osaka 573-0101, Japan. Electronic address:
This study aims to clarify the process of oral drug absorption from jelly formulations. Agar and pectin-based jellies containing drugs with different membrane permeability (high: antipyrine [ANT], medium: metoprolol [MET], low: atenolol [ATE]) were prepared and tested for in vitro drug release and in vivo drug absorption in rats. All drugs showed similar release profiles in vitro from both jelly formulations, except for the faster release from pectin jelly at neutral pH.
View Article and Find Full Text PDFChem Biodivers
November 2024
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru, 560107, Karnataka, India.
Pyrazole and its derivatives remain popular heterocycles in drug research, design, and development. Several drugs include the pyrazole scaffold, such as ramifenazone, ibipinabant, antipyrine, and axitinib, etc. They have been extensively studied by the scientific community and are said to have a wide range of biological activity, especially anticancer agents targeting EGFR.
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