Abstract
The aim. Development of optimal, high-precision and reproducible methods for quantitative determination of the main substance in the substance Epimidin - 1-(4-methoxyphenyl)-5-[2-[4-(4-methoxyphenyl)piperazin-1-yl]-2-oxo-ethyl]pyrazolo[3,4-d]pyrimidin-4-one by high performance liquid chromatography.Materials and methods. High performance liquid chromatography (HPLC) was performed using a ShimadzuNexeraX2 LC-30AD system (Shimadzu, Japan) equipped with a SPD-M20A diode array detector (DAD). ACE C18 column, size 250 x 4.6 mm, YMC with pre-column, particle size 5 μm, filled with octylsilyl silica gel for chromatography P. During the work acetonitrile and trifluoroacetic acid of HPLC class (Sigma-AldrichGmbH, Switzerland) were used, other chemicals and solvents were of analytical grade. In the study an analytical ware class A were used that meet the requirements of SPhU.Results. The following optimal conditions of chromatographic distribution are established: column C18 (250*4.6 mm); the speed of the mobile phase 1 ml / min; column thermostat temperature 35 °С; injection volume 10 μl; mobile phase A - 0.1 % trifluoroacetic acid; mobile phase B - acetonitrile P; the detection wavelength is 270 nm, the retention time of the test compound is 7.22 minutes. The performance of the column was determined for its main indicators, such as the number of theoretical plates (more than 25410) and the coefficient of symmetry (about 1.00). The technique was tested for the influence of various factors, such as flow rate, mobile phase composition and column thermostat temperature. It was established that the influence of these factors is insignificant and does not affect the results obtained by this method. The method was validated in accordance with the recommendations of SPhU on the parameters of specificity, linearity, correctness, precision, robustness (stability).Conclusions. For the first time, a high-precision and reproducible method for quantitative determination of the main substance in the substance Epimidin with anticonvulsant activity by high-performance liquid chromatography was developed. Conditions for chromatographic analysis (HPLC) were standardized. The requirements for the test “System suitability test criteria for chromatographic methods” are set. Statistical processing of the experimental results shows that the relative uncertainty of the average result is within acceptable limits. The correctness of the method was confirmed by validation studies. The developed technique will be used for pharmaceutical development and standardization of dosage form
Highlights
In the treatment of epilepsy and other pathological conditions accompanied by convulsions, the use of drugs remains the leading method of treatment
The strong anticonvulsant activity of Epimidin has been proven in various models of seizures: on the pentylenetetrazole (PTZ) model at a dose of 200 mg / kg exceeds the effect of the comparison drug sodium valprotate at a dose of 300 mg / kg [3, 4], a pronounced effect on seizures caused by caffeine and picrotoxin, moderate on strychnine convulsions [5]; high efficiency under conditions of experimental chronic epileptogenesis – model of PTZ-kindling; on the model of the maximum electroshock shows moderate activity
Wide range of effective anticonvulsant doses, favourable concomitant pharmacological profile: weak sedative and anxiolytic effect without muscle relaxant properties, positive effect on cognitive functions, no effect on depressive behaviour, no antihypoxic properties [5] and belonging to the V class of toxicity justifies the need for further study of Epimidin as a potential API
Summary
In the treatment of epilepsy and other pathological conditions accompanied by convulsions, the use of drugs remains the leading method of treatment. Despite the wide choice of antiepileptic drugs (AEDs) with different mechanisms of action, including prolonged, satisfactory control of seizures is achieved in only 65–70 % of patients [1]. It is the development of refractory forms of epilepsy [2], the need for simultaneous administration of several AEDs, the lack of drugs that would meet the criteria of high efficacy with a favourable safety profile, prompts the search for anticonvulsants among new classes of compounds. Wide range of effective anticonvulsant doses, favourable concomitant pharmacological profile: weak sedative and anxiolytic effect without muscle relaxant properties, positive effect on cognitive functions, no effect on depressive behaviour, no antihypoxic properties [5] and belonging to the V class of toxicity justifies the need for further study of Epimidin as a potential API
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