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As one of the commonly used vasoprotective drugs, Diosmin is often used in the treatment of various peripheral vascular diseases. Clinical studies have shown that Diosmin can improve the circulation of blood and lymphatic fluids, reduce oedema, and it is often used in the treatment of the following four diseases in modern clinics.
1, varicose veins of the lower limbs: clinical research shows that Diosmin can effectively improve the clinical symptoms of patients with varicose veins of the lower limbs, reduce pain, activity inconvenience, relieve venous stasis of the lower limbs, improve venous return.
2, acute or chronic haemorrhoids: clinical studies have shown that for patients with chronic haemorrhoids, Diosmin can effectively improve the size of their haemorrhoids, reduce the number of bleeding and anal prolapse, and effectively prevent and treat their acute attacks; secondly, for patients with acute haemorrhoidal attacks, the application of Diosmin on the basis of haemostatic and other symptomatic treatments can quickly control bleeding and reduce perianal pain, thus effectively alleviating the patient's pain and improving the prognosis. Improve the prognosis.
3, lymphatic reflux disorder, lymphoedema: Diosmin can effectively improve lymphatic reflux and reduce limb swelling. Clinical studies have shown that after taking Diosmin, patients with lymphoedema will have a significant reduction in limb swelling and pain, making lymphatic circulation smooth and improving patients' quality of life and health.
4, peripheral skin ulcers: clinical studies have shown that on the basis of promoting skin healing treatment, with the use of Diosmin, can effectively accelerate the prognosis of skin wounds or ulcers, reduce the local inflammatory response, alleviate skin pain, thereby effectively improving the prognosis of the disease.
Uses and functions of Diosmin.
1.Enhancement of venous toneDiosmin enhances venous wall tone, even in high temperature, it causes stronger venous contraction than other drugs such as rutin, and still enhances venous tone when the body is acidotic.
Diosmin has specific affinity for veins without affecting the arterial system.
2. Improve microcirculation, Diosmin can significantly reduce the adhesion of leukocytes and vascular endothelial cells, migration, disintegration and release of inflammatory substances, such as histamine, bradykinin, complement, leukotrienes, prostaglandins and excessive free radicals, etc., so as to reduce the permeability of the capillaries and enhance their tension, Diosmin also has the function of reducing blood viscosity and enhancing the flow rate of erythrocytes, so as to reduce the stagnation of the microcirculation.
3.Promote lymphatic refluxDiosmin increases the speed of lymphatic drainage.
A flavonoid found in citrus fruits and an agonist of the aryl hydrocarbon receptor (AhR).
Pharmacological Effect of Diosmin.
Diosmin, also known as Avellan, is a medicine for the treatment of various symptoms associated with acute attacks of haemorrhoids, and also for the treatment of various symptoms associated with veno-lymphatic insufficiency (heaviness, pain in the legs, morning soreness and discomfort). The action characteristics of Diosmin are as follows:
1. It has specific affinity to the venous system and enhances the tension of the veins without affecting the arterial system; 2. It can reduce the viscosity of the blood in the microcirculatory system and increase the flow rate to reduce stagnation;
3、It can enhance the contraction of lymphatic vessels and the speed of lymphatic drainage in the lymphatic system, and accelerate the reflux to reduce oedema.
4、The commercially available Diosmin adopts micronisation technology, which increases the contact area after the use of the drug, more absorption and higher bioavailability.
It is suitable for all kinds of haemorrhoids and acute episodes of haemorrhoids, and can also treat chronic venous insufficiency, such as varicose veins, lower limb ulcers and so on.
Product Method of Bulk Diosmin Powder.
The specific steps are as follows: add hesperidin (glycoside) to a mixed solvent of pyridine and dimethyl sulfoxide, then add potassium iodide and sulfuric acid for dehydrogenation reaction, obtaining a reaction intermediate product; add a methanol solution containing sodium hydroxide to the reaction intermediate product for the reaction; and then add acid to adjust the pH, and then precipitate the crystals by static precipitation, obtaining deoxymethane.
The purity of Diosmin produced by this method is generally lower than 95%, and is not suitable for sale as a drug, and further separation and purification is required.
CN201810382522.0 proposes a method for preparing high purity deosmin.
In order to achieve the above purpose, the technical solution of the present invention is as follows: the present invention adopts a column chromatography method for the purification and preparation of the crude product of Diosmin, and the filler in the column is a polymer chromatographic packing.
The polymer chromatographic packing refers to a chromatographic packing with a particle size of less than 100 um and a pore size of less than 100 um by precise control of particle size, morphology, particle size distribution, specific surface area, pore structure and surface functional groups, etc. with styrene, methacrylate and copolymer of styrene and methacrylate as the substrate.
Said polymer chromatographic packing adopts chromatographic packing PSN30-300.
The described method specifically contains the following steps:
1) Preparation of sample solution: take the crude product of diosmet, add it to an alkaline solvent and stir it thoroughly, dissolve it and then filter it to obtain the solution of the crude product of diosmet, and set it aside;
2) chromatographic separation process: the polymer chromatographic packing was loaded on the chromatographic column, rinsed with deionised water, after equilibrium, the deosmin crude solution obtained in step 1) was injected into the chromatographic column with a pump to take samples, after taking samples, it was drenched with deionised water, and then it was successively eluted with the first eluent and the second eluent, and each eluent was collected and tested for purity, and the deosmin eluents with purity greater than 99% were combined Then precipitate deoxamine with acid, filter and wash, and finally dry to get high purity deoxamine product.
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