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An experimental study of the systemic bioavailability of the drug "Harmin hydrochloride, capsules" in comparison with native garmin on chinchilla rabbits

https://doi.org/10.37489/2587-7836-2020-2-22-27

Abstract

An experimental comparative study of the relative bioavailability of plant alkaloid harmine (native, in the form of a base) in comparison with its derivative harmine hydrochloride was carried out on chinchilla rabbit. Both substances was administered in capsules, containing an equimolar amount of harmine (50 mg, p.o.). Harmin hydrochloride was shown to have some pharmacokinetic advantages in comparison with native harmin due to a relatively rapid achievement of the maximal plasma concentration (Tmax) and a significantly higher maximum concentration of the active substance in the blood. At the same time, there was shown that the chemical modification of harmine does not significantly affect on such pharmacokinetics parameter as the area under the curve (AUC), which indicates the absence of a difference in the degree of absorption in the compared dosage forms.

About the Authors

S. M. Adekenov
JSC "International Research and Production Holding "Phytochemistry"
Kazakhstan

Adekenov Sergazy M. – D. Sci. in Chemical, professor, Academician of the National Academy of Sciences of the Republic of Kazakhstan, General Director

Karaganda



V. S. Schnaukshta
Republican State Enterprise on the Right of Economic Management "National Center for Expertise of Medicines and Medical Devices" of the Ministry of Health of the RK
Kazakhstan

Schnaukshta Valentina S. – Candidate of Biological Sciences, Associate Professor, Head of the Laboratory of Pharmacological Testing (LFI)

Nur-Sultan



E. V. Epifantseva
"Астана Medical University" Non-commercial joint-stock company
Kazakhstan

Epifantseva Elena V. – PhD doctoral student. SPIN code: 5243-3894

Nur-Sultan



D. A. Abaimov
Research Center of Neurology
Russian Federation

Abaimov Denis A. – Candidate of Biological Sciences, Senior Researcher at the Laboratory of Hemorheology, Hemostasis and Pharmacokinetics with Clinical and Laboratory Diagnostics. SPIN code: 7548-0933

Moscow



M. G. Abdrakhmanova
"Астана Medical University" Non-commercial joint-stock company
Kazakhstan

Abdrakhmanova Mayra G. – D. Sci. in Medicine, professor, Department of Neurology

Nur-Sultan



A. K. Sariev
FSAEI HE I.M. Sechenov First MSMU MOH Russia (Sechenovskiy University)
Russian Federation

Sariev Abrek K. – D. Sci. in Medicine, professor, Department of Neurology. SPIN code: 3945-1271

Moscow



References

1. Zetler G, Back G, Iven H. Pharmacokinetics in the rat of the hallucinogenic alkaloids harmine and harmaline. Naunyn-Schmiedeberg's archives of pharmacology. 1974;285(3):273–292. DOI: 10.1007/bf00498996

2. Guan Y, Louis ED, Zheng W. Toxicokinetics of tremorogenic natural products, harmane and harmine, in male Sprague-Dawley rats. Journal of toxicology and environmental health. Part A. 2001;64(8):645–660. DOI: 10.1080/152873901753246241

3. Tweedie DJ, Burke MD. Metabolism of the beta-carbolines, harmine and harmol, by liver microsomes from phenobarbitone- or 3-methylcholanthrenetreated mice. Identification and quantitation of two novel harmine metabolites. Drug metabolism and disposition: the biological fate of chemicals. 1987;15(1):74–81.

4. Yu AM, Idle JR, Krausz KW, Kupfer A, Gonzalez FJ. Contribution of individual cytochrome P450 isozymes to the O-demethylation of the psychotropic beta-carboline alkaloids harmaline and harmine. The Journal of pharmacology and experimental therapeutics. 2003;305(1):315–322. DOI: 10.1124/jpet.102.047050


Review

For citations:


Adekenov S.M., Schnaukshta V.S., Epifantseva E.V., Abaimov D.A., Abdrakhmanova M.G., Sariev A.K. An experimental study of the systemic bioavailability of the drug "Harmin hydrochloride, capsules" in comparison with native garmin on chinchilla rabbits. Pharmacokinetics and Pharmacodynamics. 2020;(2):22-27. (In Russ.) https://doi.org/10.37489/2587-7836-2020-2-22-27

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ISSN 2587-7836 (Print)
ISSN 2686-8830 (Online)