Abstract

The aim. To conduct a comprehensive study of biphasic-type suppositories that contain diosmin and hesperidin.
 Materials and methods. Samples of biphasic-type suppositories with a mass of 4.0 were objects of the study. Pharmacological, technological and analytical research methods were used to directly or indirectly analyze the strength and completeness of the drug activity. Thus, in this work we combined the study of the specificity of the pharmacological action of the drug, experimental verification of the quantitative content of API, analysis of the structural properties of suppositories and study of the profile of the release of active pharmaceutical ingredients.
 Results. Therefore, based on the obtained data, the most effective dose was 75 mg / kg (in terms of a human dose of 300 mg per suppository). The drug in the selected dose showed a significant therapeutic effect, which significantly exceeded that of the test sample at a lower dose and the reference agent. According to the results of technological studies, it was determined that all samples of suppositories had satisfactory structural and mechanical properties. Studies of the histological structure of the mucous membrane of rats proved that there is a positive effect of treatment with suppositories with diosmin and hesperidin due to the improvement of the normal condition of the mucous membrane, the absence of edema and ulcerative defect. Research of the release profile of active pharmaceutical ingredients showed that the best percentage of release is characteristic of sample 2 (99.8 %)
 Conclusions. Therefore, suppositories with diosmin and hesperidin in therapeutically dose of 75 mg/kg of animal weight can be used for further research and will be of interest in the treatment of hemorrhoids of both acute and chronic forms

Highlights

  • Hemorrhoids is a disease of anorectal area that could cause the decrease of person adaptation in the socio-cultural community of the modern world

  • At the first stage of our study, we studied the quantitative content of diosmin and hesperidin in suppositories by the spectrophotometric method

  • The obtained results allowed to conclude about the compliance of the quantitative content of rectal suppositories with diosmin and hesperidin to the regulatory documentation

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Summary

Introduction

Hemorrhoids is a disease of anorectal area that could cause the decrease of person adaptation in the socio-cultural community of the modern world. One of the possible factors in the relapse development is the use of therapy aimed solely at the symptomatic treatment of the disease [2]. Such underestimation of phleboprotective drugs in the treatment regimen contributes to a significant increase in the probability of surgery (hemorrhoidectomy) [3]. It was important to find new methods of conservative treatment of hemorrhoids by developing combined drugs, the active substances of which belong to the group of phleboprotectors. Their main advantage is the ability to act precisely at the site of the disease and purposefully reduce the pathological process [4]. Such drugs should be developed in the form of rectal suppositories, since their complex of structural, mechanical and mucoadhesive properties provide the necessary pharmacological effect [5, 6]

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