Abstract
Objective: Study the influence of the mechanical preparation methods (grinding, fluidization) of solid pharmaceutical substances (PS) and herbal raw material on their physicochemical properties and biological activities.
 Methods: Test substances and solvents-Lactose monohydrate (DFE Pharma, Germany). Sodium chloride, bendazol hydrochloride (all Sigma-Aldrich, USA) and herbal raw material (Callisia fragrans). The dispersity and native structure of pharmaceutical substances were analyzed by several methods: optical microscopy–Altami BIO 2 microscope (Russia); low angle laser light scattering (LALLS) method (Malvern Instruments, UK); Spirotox method–Quasichemical kinetic of cell transition of cellular biosensor Spirostomum ambiguum; Fourier-transform infrared spectroscopy–the analysis in the middle IR region was carried out using an IR Cary 630 Fourier spectrometer (Agilent Technologies, USA). The analysis of dried leaves of C. fragrans before and after mechanical activation was performed using Shimadzu EDX-7000 X-ray fluorescence spectrophotometer without mineralization (Shimadzu, Japan).
 Results: It was established that the mechanical change, such as dispersion and drying, alters the biological activity of PS and herbal raw materials. The observed increase in the influence of the dispersed substance on the biosensor S. ambiguum is quantitatively estimated from the values of the activation energy (obsEa), which turns to be valued 1,5 (P≤0,05) times more than for the native form substance. In the study of the dependence of the availability of chemical elements K, Ca, Zn on the degree of dispersion of herbal raw materials was established a quantitative 4-fold (P≤0,05) increase in the concentration of elements in mechano-activated raw materials.
 Conclusion: By the example of the biological model of Spirotox (single-celled biosensor S. ambiguum) and herbal raw materials obtained from C. fragrans, the increase of biological activity of PS at the dispersion of initial preparations was proved.
Highlights
The relationship between the particle size and the reaction rate is manifested in the course of kinetic processes and at the ratecontrolling step of diffusion through the reaction product layer [1]
The effect of the mechanochemical activation of pharmaceutical substances (PS) has theoretical and important practical applications. This applies to quality control where the possible contribution of PS mechanochemical activation to its biological activity should be taken into account
The biological activity of seven samples of lactose monohydrate was investigated: 1–ММ2571; 2–ММ2571 samples saturated with intense release-active dilutions (RAD) of IFN-γ Antibodies; 3–ММ2571 sample saturated with RAD of the NO-synthase enzyme antibodies; 4–ММ2571 sample saturated with phosphate buffered saline; 5–ММ2571 sample, saturated with water; 6–ММ2571 sample saturated with aqueousalcoholic solution; sample 7–ММ25717–was not subjected to saturation
Summary
The relationship between the particle size and the reaction rate is manifested in the course of kinetic processes and at the ratecontrolling step of diffusion through the reaction product layer [1]. The influence of particle size on the physical and chemical properties of a substance can be explained by the presence of surface pressure acting on the substance [2]. The effect of the mechanochemical activation of PS has theoretical and important practical applications. This applies to quality control where the possible contribution of PS mechanochemical activation to its biological activity should be taken into account. Development of methodological approaches to drugs quality control based on the possible change in mechanochemical activation of PS will improve pharmaceutical analysis and optimize their dosages, reducing the toxic load on the body
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