Pharmacokinetic studies of new antiparkinsonian drug Rapitalam

Authors

Abstract

Parkinson's disease is the most common neurodegenerative disorder after Alzheimer's disease. The aim of this study was to investigate the pharmacokinetic parameters of the mGluR4 receptor blocker Rapitalam on rabbits. There was developed the method of the quantitative determination of Rapitalam in the blood plasma of rabbits using high performance liquid chromatography with tandem mass spectrometric detection. The study was performed on 12 rabbits (males, weighing between 3,300 to 3,500 g). In intragastric dosing of the substance was administered using a gastric tube in the form of suspension in water 0.9 mg/ml, 9 mg/ml, and 90 mg/ml at a dose of 0.3 mg/kg, 3 mg/kg and 30 mg/kg. After the administration of the substance blood was sampled through a catheter in a volume of 0.5 ml in polypropylene tubes containing 20 µl of 5% EDTA before and 10, 15, 30, 60, 120, 240, 480, 1440 minutes after administration. The mean absorption time (MAT) of Rapitalam was 268.1 minutes or 4.5 hours. The half-life is longtime and it was 176.4 minutes (2.9 hours) for intravenous and 362.2 minutes (6.0 hours) for intragastric administration. The absolute bioavailability of the intragastric dosing was 26.8%. The main pharmacokinetic parameters of the substance was established on rabbits that allow you to optimize the future use of it's as a potential drug for the treatment of Parkinson's disease.

Keywords:

Rapitalam, Parkinson's disease, the blood plasma of rabbits, high performance liquid chromatography, pharmacokinetic, metabotropic glutamate receptors

Author Contribution

Natalya V. Avdeeva, Kursk State Medical University

PhD of Medical Sciences, Assistant of Department of internal diseases №2 of Kursk State Medical University, Kursk, 305041, Russia 

Alexandr L. Kulikov, Belgorod National Research University

Postgraduate student of the Department of Pharmacology of Medical institute of Belgorod State University, Belgorod, Russia

Mikhail V. Pokrovskii, Belgorod National Research University

Doctor of Medicine, Prof., Head of the Department of Pharmacology of Belgorod State University,
Belgorod, Russia 

Tatyana V. Avtina, Belgorod National Research University

PhD in Pharmaceutical Sciences, Associate Professor, Department of Pharmacology of Belgorod State National Research University, Belgorod, Russia Scopus

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Published

30-12-2016

How to Cite

Avdeeva NV, Kulikov AL, Pokrovskii MV, Avtina TV (2016) Pharmacokinetic studies of new antiparkinsonian drug Rapitalam. Research Results in Pharmacology 2(4): 3–8

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Section

Review article

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