Comparative Study of the Dose-Dependent Effects of the Osmoregulators Sorbitol and Mannitol in Asaparkam-L on Diuresis a
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Pharmaceutical Chemistry Journal, Vol. 54, No. 7, October, 2020 (Russian Original Vol. 54, No. 7, July, 2020)
MOLECULAR BIOLOGICAL PROBLEMS OF DRUG DESIGN AND MECHANISM OF DRUG ACTION COMPARATIVE STUDY OF THE DOSE-DEPENDENT EFFECTS OF THE OSMOREGULATORS SORBITOL AND MANNITOL IN ASAPARKAM-L ON DIURESIS AND SALURESIS IN RATS A. A. Spasov,1 L. I. Bugaeva,2 V. V. Bagmetova,2,3,* S. A. Lebedeva,2 and A. Yu. Getmanenko2 Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 7, pp. 3 – 9, July, 2020.
Original article submitted October 12, 2019. The effects of the osmoregulators D-sorbitol and D-mannitol in Asparkam-L solution for infusion on diuresis and urinary K+ and Mg2+ excretion were studied in white mongrel rats. Animals received single i.v. doses of samples of the formulation Asparkam-L: 1) with osmoregulator D-sorbitol; 2) with osmoregulator D-mannitol, 3) without osmoregulator, at the recommended one-time dose (1ROTD, calculated from the dose of 10 ml for a human with the average body weight of 70 kg) and at doses 2, 4, and 6 times greater than 1ROTD. Use of all study doses produced a background of minor oscillations in diuresis, with the smallest levels of urinary K+ and Mg2+ excretion with sample 1 and the largest with sample 2. Levels of K+ and Mg2+ excretion in rats given sample 2 were statistically significantly greater than those in control animals given 0.89% NaCl at a volume equivalent to that of 6 ROTD. Increased K+ and Mg2+ excretion after use of sample 2 probably indicated lower efficacy and the inadvisability of using mannitol as osmoregulator in the formulation intended to make up for deficit of these cations. Keywords: potassium, magnesium D-sorbitol, D-mannitol, Asparkam-L.
the L-isomers of amino acids and incorporates them into biochemical processes more actively, while D-stereoisomers arriving in the body are metabolized by D-amino acid oxidase to form a-hydroxy acids [1]. The new Russian formulation Asparkam-L, developed by Volgograd pharmacologists in collaboration with Bioamid (Saratov, Russia), contains only the active levorotatory optical stereoisomer of aspartic acid [2]. L-Aspartic acid is an endogenous metabolically active amino acid, which operates as an “electrolyte transporter” – it promotes delivery of potassium and magnesium into cells and increases their assimilation by the tissues [1, 3]. Use of L-aspartic acid as a chelating agent for potassium and magnesium in Asparkam-L provides greater bioavailability and more complete uptake of potassium and
With the aim of compensating for deficiencies of potassium and magnesium, medicine makes wide use of formulations of the potassium and magnesium salts of aspartic acid (Asparkam, Panangin, Pamaton, potassium and magnesium asparaginates), which were developed on the basis of racemic mixes of L- and D-stereoisomers of aspartic acid. Current studies have shown that the human body assimilates 1 2 3 *
Volgograd State Medical University, Ministry of Health of the Russian Federation, 1 Pavshikh Bortsov Square, 400131 Volgograd, Rus
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