The pharmacokinetics of a new verapamil retard tablet formulation have been investigated in a randomized cross-over bioequivalence study on 12 healthy subjects. The drug was given orally at a single new or standard retard tablet dose of 240mg and at a single intravenous dose of 5mg. Plasma verapamil concentrations were determined by HPLC. New retard tablets produced peak plasma verapamil concentrations of 81.34+/-5.69microg/l, time to peak plasma concentrations of 4.91+/-0.89h and an AUC (0-24h) of 1291+/-103.4h x microg/l, with a terminal phase half-life of 55.1+/-14.9h. After intravenous administration verapamil exhibited biphasic elimination kinetics with a terminal plasma half-life of 2.36+/-0.42h and systemic clearance of 34.32+/-5.81 l/h. Bioavailability of the new peroral retard formulation ranged from 19.49+/-4.41% to 67.69+/-11.70%. Absorption rates and amounts were evaluated by means of the spline-convolutional method. Input rates for the new verapamil retard formulation ranged from 0.77+/-0.20mg/h to 5.57+/-1.58mg/h. The cumulative amount of verapamil input was 39.17+/-9.71% for the new retard tablets. All pharmacokinetic parameters for the new verapamil retard tablet formulation, were in reasonable agreement with the data obtained on already registered verapamil retard formulations, indicating their bioequivalence.
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http://dx.doi.org/10.1007/BF03191124 | DOI Listing |
Int J Pharm
May 2023
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China; Research Institute of Pharmaceutical Particle Technology, Zhejiang University of Technology, Hangzhou 310014, China. Electronic address:
Despite remarkable progress in the last decade in transdermal microneedle drug delivery systems, great difficulties in precisely manufacturing microneedles with sophisticated microstructures still strongly retard their practical applications. Herein we propose morphology-customized microneedles (spiral, conical, cylindroid, ring-like, arrow-like and tree-like) fabricated by stereolithography (SLA) based 3D-printing technique, and in-depth investigate the correlation between the customized morphologies and the received qualities of the corresponding microneedles such as the mechanical properties and skin penetration behavior, drug loading capacity and the drug release profiles. Results indicated that 3D-printed morphology-customized microneedles not only enhanced the mechanical strength but also improved both drug loading capacity and drug release behavior, which resulted from their highly controllable and 3D-printable morphologies (surface area and volume).
View Article and Find Full Text PDFInt J Nanomedicine
March 2021
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, 75270, Pakistan.
Purpose: This study systematically investigated the potential of four model drugs (verapamil HCl, flurbiprofen, atenolol, and furosemide), each belonging to a different class of Biopharmaceutics Classification Systems (BCS) to be developed into oral modified release dosage forms after loading with halloysite nanotubes (HNTs).
Methods: The drugs were studied for their loading (mass gain %) by varying solvent system, method, pH, and ratios of loading into the nanotubes using D-optimal split-plot design with the help of Design Expert software. Drug-loaded halloysites were characterized by XRD, DTA, FTIR, SEM, and HPLC-UV-based assay procedures.
Endocrinol Diabetes Metab Case Rep
August 2020
Section on Endocrinology and Genetics, The Eunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, Maryland, USA.
Summary: A 29-year-old primigravida woman with a known history of primary aldosteronism due to a right aldosteronoma presented with uncontrolled hypertension at 5 weeks of estimated gestation of a spontaneous pregnancy. Her hypertension was inadequately controlled with pharmacotherapy which lead to the consideration of surgical management for her primary aldosteronism. She underwent curative right unilateral adrenalectomy at 19 weeks of estimated gestational age.
View Article and Find Full Text PDFBMJ Case Rep
October 2019
Department of Neurology, SS Annunziata Hospital, Chieti, Italy.
Hemiplegic migraine (HM) is a rare subtype of migraine with aura in which attacks include transient motor weakness or hemiparesis that can last several days. HM is linked to mutations in three different genes, CACNA1A, ATP1A2 and SCN1A, which encode for ion transporters. The clinical spectrum includes atypical symptoms such as impaired consciousness, epileptic seizures, permanent cerebellar ataxia or mental retardation.
View Article and Find Full Text PDFClin Toxicol (Phila)
April 2019
c The Swedish Poisons Information Centre, Stockholm , Sweden.
Objective: Extended release (ER) tablets/capsules in massive ingestion overdoses are prone to form pharmacobezoars potentially increasing the risk of late-appearing toxic effects and prolonged symptoms. Oral activated charcoal is often sufficient to prevent drug absorption, but in a recent massive ingestion of highly toxic substances, prior orogastric lavage might be considered. The disintegration characteristics of ER preparations in overdose situations is valuable to understand if the time line and course of the intoxication might be prolonged, but information on these characteristics are unavailable.
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