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1.
Eksp Klin Farmakol ; 77(8): 34-8, 2014.
Article in Russian | MEDLINE | ID: mdl-25335389

ABSTRACT

We have studied specific features of lipid peroxidation in whole human blood under the action of aqueous solutions of xymedone (19.6 microM), phytic acid (117.9 microM) and its complex (237.6 microM) synthesized in distilled water and isotonic (0.9%) solution of sodium chloride. The estimated parameters included lipid peroxidation (LPO) rate, total antioxidant potential, superoxide dismutase (SOD) level, and malonic dialdehyde (MDA) level in blood plasma and erythrocytes. It was established that the effect of phytic acid on blood samples includes moderate stimulation of total antioxidant activity and SOD activity with predominant prooxidant effect. The phytic acid--xymedone complex synthesized in distilled water exhibits an antioxidant action, while its synthesis in saline solution yields a prooxidant.


Subject(s)
Antioxidants/pharmacology , Blood Cells/drug effects , Lipid Peroxidation/drug effects , Phytic Acid/pharmacology , Pyrimidines/pharmacology , Antioxidants/chemistry , Blood Cells/cytology , Blood Cells/metabolism , Cells, Cultured , Humans , Malondialdehyde/antagonists & inhibitors , Malondialdehyde/metabolism , Oxidation-Reduction , Phytic Acid/chemistry , Pyrimidines/chemistry , Reactive Oxygen Species/antagonists & inhibitors , Reactive Oxygen Species/metabolism , Superoxide Dismutase/metabolism
2.
Eksp Klin Farmakol ; 77(12): 26-32, 2014.
Article in Russian | MEDLINE | ID: mdl-25739190

ABSTRACT

A comparison of the relative bioavailability and intensity of penetration of glucosamine sulfate in oral, injection and topical administration of the dosage form Hondroxid Maximum as a cream containing micellar system for transdermal delivery of glucosamine in the experiment by Sprague-Dawley rats was carried out. On the base on the pharmacokinetic profiles data of glucosamine in rat blood plasma with daily administration in 3 times a day for 1 week by cream Hondroxid Maximum 400 mg/kg and the single injection solution of 4% Glucosamine sulfate 400 mg/kg was found that the relative bioavailability was 61.6%. Calculated penetration rate of glucosamine in the plasma through the rats skin in 4 hours, equal to 26.9 µg/cm2 x h, and the penetration of glucosamine through the skin into the plasma after a single dose of cream in 4 hours was 4.12%. Comparative analysis of literature and experimental data and calculations based on them suggest that medicine Hondroxid Maximum, cream with transdermal glucosamine complex in the treatment in accordance with the instructions can provide an average concentration of glucosamine in the synovial fluid of an inflamed joint in the range (0.7 - 1.5) µg/ml, much higher than the concentration of endogenous glucosamine human synovial joint fluid (0.02 - 0.07 µg/ml). By theoretical calculations taking into account experimental data it is shown that the medicine Hondroxid Maximum can reach the bioavailability level of the modern injection forms and exceed the bioavailability level of modern oral forms of glucosamine up to 2 times.


Subject(s)
Glucosamine/administration & dosage , Glucosamine/pharmacokinetics , Administration, Cutaneous , Administration, Oral , Animals , Biological Availability , Glucosamine/blood , Humans , Injections, Intramuscular , Male , Micelles , Models, Biological , Ointments , Rats, Sprague-Dawley , Synovial Fluid/metabolism , Tissue Distribution
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