Radiolabeling and biodistribution of amiodarone and desethylamiodarone

Bellen, Johan C.; Penglis, S.; Tsopelas, Chris

doi:10.1016/0969-8051(95)94367-m

Cited by 11 publications

(6 citation statements)

References 7 publications

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“…Figure 5 exhibits the simulated plasma or blood AMD and DEA concentration-time curves, at various single IV dosing regimens. Our model simulations were in good agreement with the observed concentration-time data, after bolus loading of AMD at 10,20,25,30,45,50,60,80,100 or 200 mg/kg (Fig. 5a), infusion loading of AMD at 220 mg/kg in 0.275, 0.55 or 10 h (Fig.…”

Section: Model Evaluationsupporting

confidence: 85%

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A Physiologically Based Pharmacokinetic Model of Amiodarone and its Metabolite Desethylamiodarone in Rats: Pooled Analysis of Published Data

Cai

Chen

et al. 2015

Eur J Drug Metab Pharmacokinet

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Section: Model Evaluationsupporting

confidence: 85%

“…Although numerous pharmacokinetic studies have been conducted in mice [30], rats [31,32], and dogs [33,34], no PBPK model in these species is available. Herein, we report the development of a PBPK model for both AMD and DEA in rats, based on pooled data from multiple pharmacokinetic studies.…”

Section: Introductionmentioning

confidence: 99%

A Physiologically Based Pharmacokinetic Model of Amiodarone and its Metabolite Desethylamiodarone in Rats: Pooled Analysis of Published Data

Cai

Chen

et al. 2015

Eur J Drug Metab Pharmacokinet

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“…Due to the known side effects of chronic amiodarone therapy, investigators have studied distribution and accumulation of amiodarone in different organ tissues. 18,31,32 However, there is no information as to whether amiodarone accumulates in vascular tissue in vivo, whether vascular disease affects tissue uptake, and if the kinetics of tissue uptake require chronic amiodarone treatment. Interestingly, clinical data suggest that the pharmacodynamic effect of amiodarone more closely correlates with the cumulative ingested dose than with plasma concentrations.…”

Section: Discussionmentioning

confidence: 99%

Antioxidant Activity and Sex Differences of Acute Vascular Effects of Amiodarone in Advanced Atherosclerosis

Traupe

Keller

Fojtu

et al. 2007

Journal of Cardiovascular Pharmacology

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Sexual dimorphisms of atherosclerosis and the susceptibility to arrhythmias and antiarrhythmic treatment have been reported. This study investigated acute effects of amiodarone on endothelium-dependent relaxation in the aorta of male and female apoE0 mice with advanced atherosclerosis. Amiodarone tissue uptake was quantified by high-performance liquid chromatography, and xanthine oxidase-dependent superoxide anion formation was investigated in vitro in presence or absence of amiodarone. Incubation with amiodarone for 30 min improved endothelium-dependent relaxation, which was associated with rapid vascular accumulation of amiodarone (P < 0.001) that was sex-dependent. In males, reduced endothelium-dependent relaxation was improved by amiodarone (from 88 +/- 3% to 100 +/- 2%, P < 0.01). Spontaneous phasic contractions, which were greater in females than in males (P < 0.001), were completely abolished by amiodarone (P < 0.0001). Amiodarone also inhibited generation of superoxide anion (P < 0.0001). These data show that amiodarone rapidly accumulates in atherosclerotic vascular tissue, abolishes vascular autorhythmicity, and improves endothelium-dependent function in atherosclerotic arteries. Antioxidant and vasodilator effects following amiodarone administration may contribute to its antiarrhythmic effects.

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“…The section of strip below the origin (at 5 mm to bottom edge = 1.5 cm) was blotted dry on both sides with dry thick absorbent paper (Solvent Saturation Pads; 51334; PALL Life Sciences, Victoria, Australia) for 15 s. The absorbent paper Figure 1. Double-developing method -The ITLC-SG strip was marked for development in HCl (pH 5.6) to SF 1 . Amid the test, the area below O was blotted dry with absorbent paper, and then developed in MeOH to SF 2 (10 × 4 cm) was folded in half as a "flap"; the strip section was placed between the flaps, and the top was pressed down firmly but carefully, to avoid any tearing or compromising its integrity.…”

Section: Instant Thin Layer Chromatographymentioning

confidence: 99%

“…[1] These radiopharmaceuticals are still used in nuclear medicine practice today. The more recent commercial availability of a 68 Ga-generator internationally has resulted in renewed interest to advance 68 Ga-chemistry in the laboratory, to invent new positron emitting tomography (PET) tracers for their potential translation into the clinical domain.…”

Section: Introductionmentioning

confidence: 99%

An improved assay for ⁶⁸Ga‐hydroxide in ⁶⁸Ga‐DOTATATE formulations intended for neuroendocrine tumour imaging

Ali

Hsieh

Tsopelas

2015

Labelled Comp Radiopharmac

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The objective of this study was to identify a more rapid assay for (68)Ga(OH)3 impurity in (68)Ga-DOTATATE formulations. Three methods were used to prepare (68)Ga(OH)3 reference material (pharmacopoeial, bench titration and automated radiosynthesis), and four quality control methods for its assessment (thin layer chromatography, membrane filtration, HPLC and solid phase extraction). The optimal method of preparing (68)Ga(OH)3 was by titrating (68)Ga(3+) with buffered sodium hydroxide solutions to pH 5.6 ± 0.2. The precipitate was quantitatively isolated by membrane filtration (0.02 µm)/hydrochloric acid (HCl; pH 5.6) solvent, and also it remained 100% at the origin on instant thin layer chromatography with silica gel paper/HCl (pH 5.6) solvent. For (68)Ga-DOTATATE samples, the thin layer chromatography technique was used with a single paper strip developed separately on two occasions, once in HCl (pH 5.6) and next in methanol solvent. This so-called double-developed (DD) method separated (68)Ga(OH)3 impurity located at the origin, from (68)Ga-DOTATATE plus (68)Ga(3+) at ~Rf 0.4, and it was superior to the other methods. It assayed for the impurity similarly to the pharmacopoeial method. The advantages of the DD method were that it required inexpensive test materials and it reproducibly determined % (68)Ga(OH)3 in (68)Ga-DOTATATE in 12 min, 13 min earlier than the pharmacopoeial method. This time efficiency resulted in a surplus of 12% (68)Ga-DOTATATE counts in the product vial, and this provided a contingency of radioactivity or time for the injection/imaging processes in the Nuclear Medicine Department.

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Radiolabeling and biodistribution of amiodarone and desethylamiodarone

Cited by 11 publications

References 7 publications

A Physiologically Based Pharmacokinetic Model of Amiodarone and its Metabolite Desethylamiodarone in Rats: Pooled Analysis of Published Data

A Physiologically Based Pharmacokinetic Model of Amiodarone and its Metabolite Desethylamiodarone in Rats: Pooled Analysis of Published Data

Antioxidant Activity and Sex Differences of Acute Vascular Effects of Amiodarone in Advanced Atherosclerosis

An improved assay for ⁶⁸Ga‐hydroxide in ⁶⁸Ga‐DOTATATE formulations intended for neuroendocrine tumour imaging

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Radiolabeling and biodistribution of amiodarone and desethylamiodarone

Cited by 11 publications

References 7 publications

A Physiologically Based Pharmacokinetic Model of Amiodarone and its Metabolite Desethylamiodarone in Rats: Pooled Analysis of Published Data

A Physiologically Based Pharmacokinetic Model of Amiodarone and its Metabolite Desethylamiodarone in Rats: Pooled Analysis of Published Data

Antioxidant Activity and Sex Differences of Acute Vascular Effects of Amiodarone in Advanced Atherosclerosis

An improved assay for 68Ga‐hydroxide in 68Ga‐DOTATATE formulations intended for neuroendocrine tumour imaging

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An improved assay for ⁶⁸Ga‐hydroxide in ⁶⁸Ga‐DOTATATE formulations intended for neuroendocrine tumour imaging