Twelve young (24-41 years) and 11 elderly (62-77 years) volunteer subjects received a single 1.0-gram dose of antipyrine on three occasions: intravenously, orally in the fasting state and orally following a standard breakfast. Plasma antipyrine concentrations were determined for 24 h after each dose. Compared to young males, elderly men had significantly prolonged elimination half-life (17 vs. 11 h, p less than 0.025) and reduced clearance (32 vs. 54 ml/min, p less than 0.06). However, elderly and young women did not differ in half-life (12 vs. 11 h) or clearance (37 vs. 44 ml/min). After oral dosage in the fasting state, young and elderly groups (regardless of gender) did not differ in peak plasma antipyrine concentration (Cmax) or time of peak concentration (Tmax). Absolute bioavailability was not significantly less than 100% and was not related to age. Postprandial oral dosage of antipyrine caused reduced Cmax and prolonged Tmax in all groups, but absolute bioavailability was not significantly less than 100%. Again, there were no age-related differences. Although aging may lead to reduced clearance of antipyrine among men, there is no evidence that old age is associated with impairment of the rate or extent of antipyrine absorption from the gastrointestinal tract.
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http://dx.doi.org/10.1159/000138369 | 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
February 2025
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 PDFAnn Pharm Fr
November 2024
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L. Mehta Road, Vile Parle (W), 400056 Mumbai, Maharashtra, India. Electronic address:
Objectives: Edaravone (EDR) is an effective neuroprotective agent in various neurological diseases; however, its use is restricted due to poor oral absorption. Bile salts are known for improving solubility and inhibiting drug crystallization in supersaturated conditions of the gastrointestinal tract (GIT). In our previous work, we prepared coamorphous dispersion (COAM) of EDR with sodium taurocholate (NaTC) using spray drying.
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