E.A. Krasnov, E.E. Nazmutdinova, T.G. Khoruzhaya, V.A. Shelekhova

Mediborol (dibornol), 4-methyl-2,6-diisobornylphenol is a new semi-synthetic sterically hindered phenol. Mediborol possesses antioxidative, antithrombogenic, neuroprotective and retinoprotective activity, combined with low toxicity. The purpose of this study was to develop methods of analysis for pharmaceutical quality control of tablets «Mediborol 125 mg». Mediborol-s tablets are white, right, flat-circular solid cylinders, the edges of which are bevelled. They have break-marks. Geometric dimensions of the tablets: height - 3,75 ± 0,01 mm, diameter - 11,28 mm. The maximum deviation of the mass of tablets from the average - 2,29 %. Resistance to crushing of tablets was 64,0 ± 1,5 H, friability of tablets ranged 99,49 ± 0,15%. Disintegration time of mediborol-s tablets was 3 min 8 sec ±7 sec. Quantitative determination of mediborol-s tablets were determined by UV-spectrophotometry. Contents of mediborol per tablet ranged from 0.1219 g to 0.1270 g and the deviation from the declared content did not exceed 5 %. Since mediborol practically insoluble in water, such substances are recommended as the dissolution medium using aqueous solutions with the addition of surface-active compounds or organic solvents. As the dissolution medium of mediborol-s tablets investigated phosphate buffer with sodium dodecyl sulfate in different concentrations (solution with a surfactant) and a mixture of 0.1 M solution of hydrochloric acid with 95% ethanol in different proportions (solution with an organic solvent). When used as the dissolution medium phosphate buffer with sodium dodecyl sulfate in different concentrations increase in the concentration of sodium dodecyl sulfate has little effect on the release of mediborol of tablets and did not exceed 35 %. As the dissolution medium was also investigated a mixture of 0.1 M solution of hydrochloric acid and ethyl alcohol 95 % in the ratio of 1:9, 2:8 and 3:7. In addition, to increase the release of mediborol from tablets was adjusted the velocity of rotation of the basket. The best results were obtained using a mixture of 0.1 M solution of hydrochloric acid and ethyl alcohol 95 % at a ratio of 2:8 and the rotational speed of the basket 200 rpm. Under these conditions the release of the active ingredient from the tablets was 86,74 - 4,75%, which meets the requirements of State Pharmacopoeia of USSR XI and the General Monographs 42-0003-04 «Dissolve». Thus, on the basis of these studies developed techniques of analysis of mediborol-s tablets to allow quality control.