The pharmacokinetics of vinpocetine (Cavinton) and of its main metabolite apovincaminic acid (AVA), has been studied in 5 healthy male volunteers after the administration of 3 x 5 and 3 x 10 daily doses of vinpocetine for seven days. The pharmacokinetic curves of both vinpocetine and AVA have been determined prior to the chronic administration and on the last day of the treatment, whereas between the 2nd and 6th days, concentration was measured once daily. On the basis of these pharmacokinetic studies it can be concluded that both vinpocetine and AVA show linear pharmacokinetics at the doses used and that there is no accumulation or autoinduction.
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http://dx.doi.org/10.1007/BF03190120 | DOI Listing |
J Drug Target
November 2024
Basic Science Research Center (Off-Campus), KLE College of Pharmacy, Bengaluru, Karnataka, India.
Alzheimer's disease (AD), which is marked by gradual neuronal decline and subsequent loss of cognitive functions and memory, poses significant treatment challenges. The present study involved the development, , and evaluation of a novel intranasal mucoadhesive in-situ gel of vinpocetine (VIN) with the aim to target the brain. An innovative gel formulation composed of poloxamer 407, HPMC E15 LV, and citric acid as a solubilizer was developed by 2 Factorial Design.
View Article and Find Full Text PDFNat Commun
May 2024
Medical Research Institute, College of Pharmaceutical Sciences, Southwest University, Chongqing, PR China.
Despite advances in active drug targeting for blood-brain barrier penetration, two key challenges persist: first, attachment of a targeting ligand to the drug or drug carrier does not enhance its brain biodistribution; and second, many brain diseases are intricately linked to microcirculation disorders that significantly impede drug accumulation within brain lesions even after they cross the barrier. Inspired by the neuroprotective properties of vinpocetine, which regulates cerebral blood flow, we propose a molecular library design centered on this class of cyclic tertiary amine compounds and develop a self-enhanced brain-targeted nucleic acid delivery system. Our findings reveal that: (i) vinpocetine-derived ionizable-lipidoid nanoparticles efficiently breach the blood-brain barrier; (ii) they have high gene-loading capacity, facilitating endosomal escape and intracellular transport; (iii) their administration is safe with minimal immunogenicity even with prolonged use; and (iv) they have potent pharmacologic brain-protective activity and may synergize with treatments for brain disorders as demonstrated in male APP/PS1 mice.
View Article and Find Full Text PDFJ Pharm Biomed Anal
February 2024
Federal Research Centre "Fundamentals of Biotechnology" of the Russian Academy of Sciences (Research Centre of Biotechnology RAS), 33-1 Leninsky prospect, 119071 Moscow, Russia. Electronic address:
The eburnamine-vincamine alkaloids exhibit a range of pharmacological activities. There is a limited understanding of the pharmacokinetics and pharmacodynamics of vindeburnol, a synthetic derivative of this chemical class of alkaloids. A fast and reliable UPLC-HRMS method was developed and validated to quantify vindeburnol in Soviet Chinchilla rabbit plasma from pharmacokinetics studies.
View Article and Find Full Text PDFPharmaceutics
October 2023
Department of Pharmacological Sciences, Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-004 Lisboa, Portugal.
This paper examines the use of vinpocetine in the context of clinical pharmacology. The main and active metabolite of vinpocetine is apovincaminic acid (AVA). Due to the scarce information in the literature on AVA pharmacokinetics, we propose a population pharmacokinetic (PopPK) model for AVA based on a study in healthy volunteers with three different formulations of vinpocetine.
View Article and Find Full Text PDFDrug Deliv
August 2022
Department of Drug and Health Sciences, University of Catania, Catania, Italy.
Vinpocetine (VNP), a semisynthetic active pharmaceutical ingredient, is used for oral management of cerebrovascular diseases because of its ability to enhance the blood flow to the brain. However, despite that, the therapeutic application of VNP is restricted due to its reduced bioavailability and diminished brain levels that could be attributed to its low aqueous solubility, short half-life, and presystemic metabolism exposure. Accordingly, the goal of this work was to explore the ability of surface-tailored intranasal emulsomes to boost brain delivery of the drug.
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