Vol 6, No 4 (2018)

This article presents results of the study and modeling of solvent influence on isosalipurposide extraction from Helichrysi Arenarii flowers.The aim of this work is to study the influence of the solvent on isosalipurposide extraction from Helichrysi arenarii flowers and suggest a theoretical model for description of the results obtained.Materials and methods. The basic materials were: a ground plant raw material of Helichrysi arenarii flowers. water solutions of ethanol (26, 43, 59, 72, 81, 97±1% v/v.), methanol, 1-propanol, 2-propanol, acetone and ethyl acetate. The extracts were obtained from the plant raw materials / solvent at the ratio of 1:5 (wt./vol.) by maceration for 24 hours at the temperature of 24±1°С. The analysis of the extracts was carried out by reversed-phase high performance liquid chromatography and isosalipurposide reference substance.Results and discussion. A dependence of isosalipurposide concentration in ethanol-water extracts on ethanol concentration in the solution was studied. It has been found out that maximum concentration of isosalipurposide is observed in the solutions with ethanol concentration of 75±5% v/v. This range of ethanol concentrations corresponds to solvent’s dielectric constant value of 38±3 units. The regression equation of dependence between isosalipurposide concentration in the extract and dielectric constant of ethanol-water solution has been obtained. Optimal concentration of the solvent has been theoretically predicted and experimentally verified as in the case of   water solutions of methanol, acetone, 1-propanol, and 2-propanol.Conclusion. It has been determined that solvent’s dielectric constant has the most significant influence on the extraction process of phytocompound from the plant raw material. A mathematical model for description of the dependence of isosalipurposide concentration on dielectric constant of ethanol-water solutions has been substantiated theoretically and tested. The optimal range of solvent’s dielectric constant to obtain maximum concentration of isosalipurposide in the extract has been found.

The search for new drugs providing effective and safe therapy of acid-dependent diseases of the gastrointestinal tract, continues to be an actual problem of modern pharmacotherapy. One of the most significant pathogenetic mechanisms of these diseases is associated with Helicobacter pylori damage to the gastric mucosa.The aim of this study is the experimental investigation of the antiulcer effect of 2-phenyl-9-diethylaminoethylamine [1,2-a] benzimidazole substance (hereinafter a Benzimidazole derivative substance) on the model of Helicobacter pylori-like gastric mucosal injury in combination with immobilization stress (a restraint).Materials and methods. For modeling a mucous membrane damage to experimental animals (white Wistar male rats), they were injected 120 mmol/l ammonia solution after a 24-hour immobilization stress (restraint). As reference drugs, the following officinal anti-ulcer drugs widely used in clinical practice, had been chosen: Rranitidine (30 mg/kg, 10 mg/kg and 3 mg/kg) and Omeprazole (3 mg/kg, 1 mg/kg and 0.3 mg/kg). The study substance was used in the doses of 30 mg/kg, 10 mg/kg and 3 mg/kg. The maximum doses of the reference drugs were calculated on the basis of maximum daily doses for humans, taking into consideration the interspecies conversion factor. The maximum dose of the substance under study was selected experimentally. The logarithmic dose range was used for the convenience of further calculations of the ED50 value. All the studied objects were introduced intragastrically through a non-traumatic tube.Results and discussion. It has been established that the studied substance significantly reduced the area of mucosal damage relative to the control values in modeling Helicobacter pylori-like gastric mucosal injury provoked by the administration of ammonia solution against the background of gastric mucosal ischemia after a 24-hour restraint. At the same time, the inhibition of ulceration reached 78%, while in the groups receiving Ranitidine and Omeprazole, it reached 66% and 50%, respectively. The calculated ED50 values were the following: for the substance under study – 16.03 mg/kg, and for Ranitidine – 15.99 mg/kg.Conclusion. The gained results indicate that the studied Benzimidazole derivative is superior to analogs in its ability to suppress gastric mucosal ulceration provoked by Helicobacter pylori-like gastric mucosal injury, which confirms the relevance of further study of anti-ulcer activity and the development of the pharmaceutical dosage form based on it.

Introduction. This study deals with the problem of similarity of the principles and approaches of drug technologies in the medieval manuscript “Antidotarium Nicolai” by Nicholas of Salerno with modern pharmaceutical technologies.The aim of study is a textual investigation of “Antidotarium Nicolai”, a detailed research of the content of the manuscript, recipes and technologies for making medicines.Materials and methods. In order to achieve this goal, eighty-five recipes of “Antidotarium Nicolai” have been identified, systematized and analyzed in a documentary translation from medieval French. An interdisciplinary study of the content of the manuscript was carried out with the help of factor analysis of the historical source and modern scientific literature.Results and discussion. Having described the content and aspects of the prescriptions of “Antidotarium Nicolai”, the authors note the similarity of the technologies of drugs and galenical preparations with modern pharmaceutical technology, in particular, with the technology of pharmacy production. In “Antidotarium Nicolai” it is stated that preparations based on herbal medicinal raw materials may be second-line therapy agents for completing treatment after the application of basic pharmacological preparations.Conclusion. The results of this work reveal the potential for the use of herbal medicines in the conditions of modern evidence-based medicine, in particular, in the organization of long-term treatment and secondary prevention of chronic diseases in patients who need to maintain their ability to work, and provide them with a sufficiently high level of quality of life. A detailed translation of the full text of the manuscript, the analysis of its content in accordance with the requirements of rational pharmacotherapy and phytotherapy, further favors to identify the prospects for the development of new drugs, multi-component in their chemical composition with a wide range of therapeutic effects.