Pharmacokinetics of Probucol in Male Rats

Heeg, Joel F.; Hiser, Michael F.; Satonin, Darlene K.; Rose, James Q.

doi:10.1002/jps.2600731225

Cited by 31 publications

(13 citation statements)

References 6 publications

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“…In one study, gelatin-acacia microcapsules were prepared by using a special coacervation method and were studied for encapsulating microdroplets of oil solution containing PB; this resulted in better bioavailability 15. PB’s low and variable oral bioavailability, and its nonlinear distribution and clearance, contribute to the variability in its pharmacokinetic (PK) and pharmacodynamic properties, as well as its adverse effects 16,17. Thus, despite its huge potential, its variable and poor absorption kinetics remain major obstacles to its potential use in T2D 16…”

Section: Introductionmentioning

confidence: 99%

Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

Mooranian¹,

Negrulj²,

Chen-Tan³

et al. 2014

DDDT

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IntroductionIn previous studies, we successfully designed complex multicompartmental microcapsules as a platform for the oral targeted delivery of lipophilic drugs in type 2 diabetes (T2D). Probucol (PB) is an antihyperlipidemic and antioxidant drug with the potential to show benefits in T2D. We aimed to create a novel microencapsulated formulation of PB and to examine the shape, size, and chemical, thermal, and rheological properties of these microcapsules in vitro.MethodMicroencapsulation was carried out using the Büchi-based microencapsulating system developed in our laboratory. Using the polymer, sodium alginate (SA), empty (control, SA) and loaded (test, PB-SA) microcapsules were prepared at a constant ratio (1:30). Complete characterizations of microcapsules, in terms of morphology, thermal profiles, dispersity, and spectral studies, were carried out in triplicate.ResultsPB-SA microcapsules displayed uniform and homogeneous characteristics with an average diameter of 1 mm. The microcapsules exhibited pseudoplastic-thixotropic characteristics and showed no chemical interactions between the ingredients. These data were further supported by differential scanning calorimetric analysis and Fourier transform infrared spectral studies, suggesting microcapsule stability.ConclusionThe new PB-SA microcapsules have good structural properties and may be suitable for the oral delivery of PB in T2D. Further studies are required to examine the clinical efficacy and safety of PB in T2D.

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Section: Introductionmentioning

confidence: 99%

Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

Mooranian¹,

Negrulj²,

Chen-Tan³

et al. 2014

DDDT

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“…Heeg et al reported the bioavailability of [ 14 C]probucol in an oil-water emulsion in rats. 9) Shudo et al reported on the pharmacokinetic profile of probucol after oral administration of various nanoparticles prepared by co-grinding probucol with PVP of various molecular weights and sodium dodecyl sulfate (SDS) in rats. 10) Pongpeerapat et al reported on the mechanism of formation of colloidal nanoparticles obtained from a probucol/PVP/SDS ternary ground mixture.…”

Section: -7)mentioning

confidence: 99%

Enhanced Bioavailability of Probucol Following the Administration of Solid Dispersion Systems of Probucol-Polyvinylpyrrolidone in Rabbits

Kubo

Terashima

Yagi

et al. 2009

Biological & Pharmaceutical Bulletin

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“…Radioisotopes (typically 14 C, but also 32 P, 34 S, etc.) incorporated into drug molecules allow them to be systemically tracked via scintillation counting 15 . Radioimmunoassays are competitive inhibition techniques where an unlabelled drug competes for antibody binding with its radioactive counterpart (typically labeled with 3 H, 75 Se, 125 I, etc.)…”

Section: Introductionmentioning

confidence: 99%

A simple method to determine the elimination half-life of drugs displaying noncumulative toxicity

Nagarajan

Venkatesh

Thakur

et al. 2019

Preprint

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The pharmacokinetic characterization of a drug, especially the determination of its biological half-life, is an essential step during the early phases of drug development. An adequate half-life is amongst the many properties needed for selecting a drug candidate for clinical trials. Conversely, drug candidates possessing inadequate half-lives may be modified or eliminated from the drug discovery pipeline altogether. Several methods exist for determining the half-lives of drugs, namely HPLC, fluorescence assays, radioassays, radioimmunoassays, and elemental mass spectrometric assays. However, all these techniques are resource and labor-intensive, and cannot be used for the high-throughput half-life determination of hundreds of drug candidates. Here, we describe TOX HL : a simple technique to determine the half-lives of compounds displaying noncumulative toxicity. To calculate the half life, TOX HL only relies on the survival outcomes of three experiments performed on an animal model: an acute toxicity experiment, a cumulative toxicity experiment, and a multi-dose experiment at different dosing intervals. As a proof of concept, we use TOX HL to determine the peritoneal half-life of Ω76, an antimicrobial peptide. The half-life of Ω76 determined by TOX HL is in good agreement with results from a standard mass spectrometric method, validating this approach.

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Pharmacokinetics of Probucol in Male Rats

Cited by 31 publications

References 6 publications

Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

Microencapsulation as a novel delivery method for the potential antidiabetic drug, Probucol

Enhanced Bioavailability of Probucol Following the Administration of Solid Dispersion Systems of Probucol-Polyvinylpyrrolidone in Rabbits

A simple method to determine the elimination half-life of drugs displaying noncumulative toxicity

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