Abstract
Introduction. The creating an effective and safe domestic neuroprotective medicines with a complex of pleiotropic effects realized through specific orphan receptors (SUCNR1, HCA2) of glial cells, is a pressing problem of modern pharmacology and a promising possibility of pharmacotherapy of brain injury and cerebrovascular diseases. Ideally, the medicine should helps restore lost cognitive functions and physical performance after damage to the central nervous system, and its use should improve the quality of life of patients and reduce the risk of complications.Aim. To develop composition and technology of a new medicine tablets with neuroprotective effect, using fractional factorial design of experiment and the Harrington desirability function.Materials and methods. The shape and size of particles, physicochemical (solubility, melting point) and technological properties (bulk density, compressibility factor, fractional composition, hygroscopicity) of the pharmaceutical substance of DEAE derivative were studied according to the methods described in the State Pharmacopoeia of the Russian Federation (14th edition). A three-factor fractional plan based on the 4 × 4 Latin square design for selection a scientifically based composition of solid dosage form was chosen. 16 experiments to test the significance of the factors were carried out. The tablets obtained according to the planning matrix were investigated for disintegration; tablet crush resistance, friability, and hygroscopicity. To optimize the quality of the tablets, the generalized Harrington desirability function was used.Results and discussion. The study of the physicochemical and technological properties of the DEAE derivative substance showed that it is a highly hygroscopic, amorphous, white or pale yellow, odourless powder, prone to the formation of agglomerates. The powder is very easily soluble in water. Taking into account the values of the general desirability function, the best result was shown by sample № 4 consisting of mannitol, calcium stearate, and partially pregelatinized maize starch.Conclusion. The physicochemical and technological properties of the DEAE derivative were studied. The DEAE derivative is a highly hygroscopic substance. Via the method of mathematical planning of the experiment the composition of DEAE derivative tablets was selected and scientifically grounded: DEAE derivative 60 mg, mannitol, partially pregelatinized maize starch, calcium stearate. The average tablet weight is 300 mg. The parameters of pressing tablets were selected.
Highlights
The creating an effective and safe domestic neuroprotective medicines with a complex of pleiotropic effects realized through specific orphan receptors (SUCNR1, HCA2) of glial cells, is a pressing problem of modern pharmacology and a promising possibility of pharmacotherapy of brain injury and cerebrovascular diseases
Перевод качественных параметров в соответствующие желательности производился для каждого параметра отдельно
Сборник материалов VI Всероссийской научно-практической конференции с международным участием «Инновации в здоровье нации», Санкт-Петербург, 14–15 ноября
Summary
Для разработки состава и технологии таблеток пДЭАЭ были изучены растворимость, физико-химические и технологические свойства фармацевтической субстанции согласно методикам, описанным в Государственной Фармакопеи XIV издания [8]. Были изучены гигроскопичность субстанции пДЭАЭ и напрессованных таблеток различного состава. В качестве критериев оптимизации были выбраны параметры, характеризующие качество таблеток: Y1 – прочность на раздавливание, Н; Y2 – время распадаемости таблеток, с; Y3 – истираемость таблеток, %; Y4 – количество поглощенной влаги таблетками, %. Влияющих на показатели качества таблеток, было проведено 16 опытов, предусмотренных матрицей планирования. Для оптимизации показателей качества таблеток использовали обобщенную функцию желательности Харрингтона [10], выраженную уравнением (1):. Где di – желательности показателей качества таблеток. Для построения графика зависимости желательности от значений критериев оптимизации использовали метод количественных оценок с интервалом значений желательностей от 0 до 1. Перевод качественных параметров в соответствующие желательности производился для каждого параметра отдельно
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