Drug with membrane-stabilizing efficacy

FIELD: pharmacology.

SUBSTANCE: invention proposes use of polysorb as drug with membrane-stabilizing efficacy supplementing early known antioxidant and sorption properties of this substance.

EFFECT: enabled use of polysorb for monotherapy to treat a large number of diseases.

1 tbl

 

The invention relates to medicine and can be applied in pharmacology, in particular, refers to drugs used as antioxidant.

Lipid peroxidation is a normal part of oxidative processes constantly occurring in the body. Excessive activation of lipid peroxidation has a damaging effect on the level of subcellular structures. Powerful damaging effect on the cell have a high reactivity of the lipid gidroperekisi, which are formed as a result of lipid peroxidation (LPO) by free radicals.

With dysregulation of processes of free radical lipid peroxidation associated mechanism for the development of many pathological conditions and diseases related to socially significant, including aging, cancer, atherosclerosis, diabetes, Alzheimer's disease.

Not to give free radicals accumulate in the body and prevent the FLOOR can antioxidants. Antioxidants are antioxidants, i.e. substances capable of inhibiting free-radical oxidation processes.

The body has natural antioxidant system enzymes - superoxide dismutase, catalase, peroxidase etc.; macromolecular nonenzymatic components - Suvereto the major proteins; low molecular weight components - thyroxine, female sex hormones, vitamins a, E, K and other

But this system is in a state of oxidative stress is overloaded. It is therefore necessary to compensate for a deficiency of antioxidants from the outside.

As antioxidants of natural origin are used: Tocopherols, ubiquinone, carotenoids, hossipole, sesamol, esters of Gallic acid, quercetin, guaiac and ascorbic acid (see Buldakov A.S., Food additives., C.-P.: Ut, 1996, pp.92).

Some of them, such as Tocopherols, ubiquinone, carotenoids are not soluble in water, making them difficult to use.

Closest to the claimed technical solution and taken as a prototype is widely used in medicine natural hydrophilic, water-soluble antioxidant ascorbic acid (see Captains A.B. Pimenov A.M. antioxidant Carotenoids as modulators of cellular metabolism J. Successes of modern biology. 1996. -T.116. - V.2, s-179.).

The present invention is the expansion of the range of antioxidants.

The problem is solved by applying Polisorb as antioxidant

Polisorb is a drug on the basis of highly dispersed silica. In the aquatic environment on the surface of the microparticles of Polisorb produce large quantities of active groups silox is on, which in the simplified formula look like this:

the covalent bond in this compound is very unstable:

next, the action of H+in the usual way: H2O2+2H+=>2H2O+O2.

Thus, the mechanism of action of Polisorb belongs to the category of antioxidants to“scavengers” (scavenger of free radicals), which cleanse the body of free radicals, restoring them to free inactive ingredients.

Conducted patent research did not reveal identical and similar technical solutions that allows to draw a conclusion about the novelty and inventive step of the claimed technical solution.

The inventive tool is CJSC “Polisorb”, Chelyabinsk under the trademark “Polisorb MP (medical, pills) and represents a high-purity silica, hydrophilic. Applied in the form of a 1-10% aqueous suspension

The study of the antioxidant activity of POLYSORB was carried out by two methods.

Weakly peroxide chemiluminescence (PHL).

Adding hydrogen peroxide to many organic and inorganic substances leads to the development of flash chemiluminescence. The mechanism PHL explained by the reactions resulting from the decomposition of H2About2active Faure is oxygen: BUT +O2+, HO2+O2.

The table presents PHL blood serum of rats using POLYSORB.

Table
GroupNo. of animals% Polisorb in aqueous suspensionsS (sutasoma)I max (amplitude glow)St max (duration of the glow)
Experimental group (POLYSORB)1529,143,790,76
 2116,450,770,54
 3527,421,911,42
 41061,501,321,41
 57is 41.451,301,35
 Cf635,1921,8181,096
The control group11-11,751,100,64
 12-26,791,381,26
13-19,531,550,90
 14-14,871,190,95
 Cf.18,2351,3050,9375

The table shows that the maximum amplitude of the outbreak have been reported with the use of POLYSORB that characterizes him as a powerful antioxidant.

2. The study of complementary activity of blood serum (indirect method).

Activation of complement occurs on the basis of proton and electron transfers, depending on the potential difference of the molecules participating immune responses. The use of antioxidants increases the activity of complement due to the directional change of redox potential.

The activity of complement was determined by recording the time constant lysis of sheep erythrocytes. The initial activity of complement amounted to 6.4% When using POLYSORB in a daily dose of 150 mg/kg of body weight constant was 8.3%

The dosage of POLYSORB can vary widely without any negative side effects. The harmlessness of POLYSORB were studied on animals Institute of surface chemistry of NAS of Ukraine. It is established that at which the base introduction 10 times therapeutic dose (1.0 g/kg) did not register any deviations from the indices of metabolism, hematological parameters of blood and immune system. The long introduction of POLYSORB in doses of 0.1, to 0.33 and 1.0 g/kg total protein content was not significantly changed in any series of experiments. The introduction of POLYSORB up to 90 days at a dose of 0.1 and 0.33 g/kg has no effect on the indices of nonspecific protection and immunity. None of the tested doses POLYSORB has no teratogenic, embryotoxic and teratogenic action.

Therefore, pharmacological tool POLYSORB can be used as an antioxidant long courses and, if necessary, in large doses, without toxic effects on the body.

In addition, it is known that in the pathogenesis of a large number of diseases are important syndrome of endogenous intoxication and violation of redox processes. Also proved the effectiveness of the joint application of chelators and antioxidants. High sorption activity of POLYSORB, its adaptogenic, anti-allergic, antioxidant, membrane-stabilizing effect mutually enhance the effects on the body and allow the use of POLYSORB as monotherapy instead of using multiple drugs. The result is a reduction in the number of drugs used and how sledstvennaya frequency is oznacevanje side effects.

The use of Polisorb as a means of membrane-stabilizing effect.



 

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