Determination of clemastine by the HPLC method in the blood

Topicality. Сlemastine fumarate (tavegil)-1-methyl-2 [2-α-methyl-p-chlorobenzhydryloxy)-ethyl]-pyrrolidine is the first generation H1-histamine receptor blocker. selectively inhibits histamine H1 receptors and reduces capillary permeability. The drug has a pronounced anti-allergic antipruritic effect. Clemastine prevents development of vasodilation smooth muscle contraction induced by histamine. an isignificant anticholinergic activity, causes sedation. used to treat pruritus in psoriasis, multiple sclerosis optic neuritis. characterized following side effects: increased fatigue, drowsiness, sedation, weakness, lethargy, impaired coordination movements; nausea, vomiting, decreased blood pressure, palpitations, hemolytic anemia, skin rash, anaphylactic shock. In case overdose, neurotoxic effect, which manifests itself consciousness with generalized convulsive syndrome. urgent task for monitoring treatment effectiveness population сlemastine diagnosis intoxication choice highly sensitive selective research methods its analysis pharmaceuticals biological matrices during treatment. Aim. To develop algorithm directed clemastine extracts from using unified method HPLC research. Materials methods. extraction was performed chloroform at Ph 9.0. were purified impurities combination TLC hexane. purification identification carried out under optimal conditions: system organic solvents – methanol 25 % solution ammonium hydroxide (100 : 1.5) chromatographic plates Sorbfil PTLC-AF-A, Rf = 0.60 ± 0.03. detect clemastine, most location reagents –UV light (λ 254 nm) Dragendorff’s reagent modified Mounier. on “Milichrome A-02” microcolumn liquid chromatograph (EkoNova, Closed Joint-Stock Company, Russia) standardized reversed-phase variant metal column non-polar absorbent Prontosil 120-5C 18 AQ, 5 μm; mobile phase linear gradient mode eluent А (5 acetonitrile 95 buffer 0.2 М lithium perchlorate 0.005 perchloric acid) B acetonitrile) 40 min. Regeneration conducted 2 min mixture solvents; flow rate 100 μl/min, injection volume 4 μl. multichannel detection substance two-beam multi-wave UV spectrophotometer 8 wavelengths 210, 220, 230, 240, 250, 260, 280, 300 nm; value temperature 37-40 °С pump pressure 2.8-3.2 MPa. Results discussion. Isolation according developed, including pH 9.0; hexane impurities; clemastine. Using identified retention parameters spectral ratios. For quantitative determination, calibration graph or straight line equation corresponding this used. results obtained indicated reliability reproducibility method. It found that relative uncertainty average result ε 4.63 %, standard deviation RSDx 1.67 %. Conclusions. extracted 9.0 blood. Purification co-extractive compounds combining been when isolating developed it possible determine 36.05-39.55 (ε %). biogenic tested 1.5), use light, Mounier, 0.03 (Sorbfil PTLC-AF-A). quantification developed. can be time 25.997-26.011 min; 2599.7-2601.1 μl; ratios 0.741; 0.536; 0.096; 0.023; 0.027; 0.005; 0.003. content determined S 0.15 · 10-3 С + 0.14 10-3; correlation coefficient equal 0.9998. Chromatographic recommended implementation practice Bureau Forensic Medical Examination, poison control centers, clinical laboratories regarding study medicinal substances objects.