Capillary-restorative agent

FIELD: medicine, pharmacology.

SUBSTANCE: invention relates to using the natural triterpenoid of the lupan order, namely betulin, as a capillary-restorative agent. It was found capillary-restorative properties of 1% alcoholic solution of betulin being without its toxic effect on organism. Betulin as 1% alcoholic solution decreases penetrability of mouse skin vessels by 2 times more effective as compared with the known capillary-restorative agent dihydroquercetin. The new agent can be used in treatment of many diseases.

EFFECT: valuable medicinal properties of agent.

2 tbl, 2 ex

 

The invention relates to medicine and pharmacology and the application of natural triterpenoids number of Lupan - betulin as capillary means.

The content of betulin in birch bark is from 10 to 30%. Betulin (loop-20(29)-ene-3, 28-diol) has the following chemical formula: C30H50O2.

Betulin is a crystalline white powder, soluble in hot chloroform, pyridine, tetrahydrofuran, slightly soluble in alcohol and most organic solvents, practically insoluble in water. Betulin has a high thermal stability, its melting point ranges from 251 to 261°C, depending on purity.

A method of obtaining betulin, including activation bark at a temperature of 180-260°C, a pressure of 2-5 MPa for 1-5 min simultaneously with the alkaline hydrolysis, followed by boiling in alcohol (EN 2131882, 20.06.99). Described is a method of obtaining betulin, involving the extraction of 90-95% ethyl alcohol at a temperature of 70-75°in the presence of activated charcoal (EN 2172178). A method of obtaining betulin by extraction with isopropyl alcohol pre-milled in an aqueous-alkaline medium birch bark (SU 382657). Method for obtaining betulin extraction of birch bark Wye the spirit within 2 hours at a temperature of 155° With further processing of the extract aqueous concentrated solution of sodium hydroxide (RU 2138508). A method of obtaining Betulinol, including extraction of birch bark hexane within 3-5 hours followed by treatment of the extract with an equal volume of water (EN 2206572, 20.06.2003).

Recently, intensive research is being conducted pharmacological activity of betulin and other triterpenoids lupanovo series. Known protivovirusnaya activity of betulin and its derivatives (Pavlova N.I.; Savinova .V.; Nikolaeva S.N et.al. Antiviral activity ofbetulin, betulinic and betulonic acids against some enveloped and non-enveloped viruses // Fitoterapia, 74(5), 489-492, 2003). Studied anti-inflammatory properties of betulin and its derivatives (Zdzisinska Barbara; Rzeski Wojciech; Roman Paduch, et.al. Differential effect of betulin and betulinic acid on cytokine production in human whole blood cell cultures // Journal of Pharmacology, 55(2), 235-238 2003). To investigate its choleretic and hepatoprotective action (Ukiwasiliana and other Pharmacological properties of triterpenoids of birch bark // Experimental and clinical pharmacology. - 1993, Vol 56, No. 4, P.53-55).

Object of the invention is the extension of the spectrum of pharmacological activity of betulin and its use as a capillary means.

Known capillary means - rutin, quercetin, dihydroquercetin. Closest to the proposed appointment of the drug is dihydroquercetin. Capillaroscopy the e effect of dihydroquercetin was studied in laboratory mice according to the method Ovina and Monakova (1953). Criterion vascular permeability was time tepanovoi blue in the inflammation caused by drawing on nepilirovanny the skin surface 0.05 ml of xylene. At the dose of 100 mg/kg dihydroquercetin slowed output tepanovoi blue on 53.0%, and at a dose of 300 mg/kg - 73.5% (EN 2014841, 30.06.94).

The toxicity study of betulin.

Acute toxicity of betulin was investigated in experiments on outbred mice. Betulin was introduced into the stomach in doses of 3000 to 9000 mg/kg in the form of a 15% starch suspension. Toxicity was assessed by clinical symptoms, physiological tests and survival of animals within 2 weeks. After intragastric administration of betulin in doses of 3000 mg/kg to 7500 mg/kg it was expressed only in a slight depression of the Central nervous system (CNS). The death of a part of the animals was observed with the introduction of betulin dose of 7500 mg/kg, and in the picture of acute poisoning prevailed symptoms of CNS depression, respiratory failure, reduction of motor activity.

Based on the results of Toxicological studies concluded that the company is not poisonous and in accordance with international Toxicological classification belongs to the 4th class of low-toxic substances: sredneseriynoe dose (LD50) betulin is more than 9000 mg/kg (table 1).

Example 1. Study Kapil okrepshego actions betulin.

Study of the effect of betulin on vascular permeability of the skin were performed on mice according to the method Ovina and Monakova (1953). Criterion vascular permeability was time output 1% aqueous methylene blue in the inflammation caused by drawing on nepilirovanny the skin surface 0.05 ml of xylene. Experimental mice 1 hour before intraperitoneal injection of 0.25 ml of 1% solution of methylene blue was administered intragastrically 1% alcoholic solution of betulin in the dose of 200 mg/kg, which corresponded to 0.2 ml of the Control group of mice in the stomach was administered to 96% ethyl alcohol. We registered the time allocation of methylene blue in inflammation. Data on the biological activity of betulin on vascular permeability in the skin of mice in comparison with dihydroquercetin are shown in table 2. In the control group of animals the time of methylene blue was 14.7 sec, whereas in the experimental group time was significantly large, which indicates the manifestation of the betulin capillary effect.

Example 2. The research was carried out analogously to example 1, only the experimental group of mice was injected with 1% alcoholic solution of betulin in a dose of 400 mg/kg, which corresponded to 0.4 ml of the solution (table 2).

At a dose of betulin 400 mg/kg capillary effect was 146.9% of control, i.e. in this dose capillary 3 times higher than the dose of 200 mg/kg At a dose of 400 mg/kg - capillary effect was 2 times higher than the well-known capillary tool dihydroquercetin in the dose of 300 mg/kg

Based on the results of the research showed that betulin has a pronounced dose-dependent capillary action.

Increased permeability of the walls of blood vessels, including capillaries, is one of the pathogenetic stages of viral, bacterial, allergic, autoimmune, endocrine and other diseases. Therefore, the company is a substance of vegetable origin, having capillary properties and non-toxic, can be used in the treatment of capillariasis and hemorrhagic diathesis, allergic, autoimmune, bacterial and viral diseases.

Table 1

Main indicators of acute toxicity of betulin and digitalverein intraperitoneal injection
SubstanceIndicators of toxicity, mg/kg
LD16LD50
Betulin6500>9000
Dihydroquercetin 28103630
Table 2

The effect of betulin and dihydroquercetin on vascular permeability of the skin
SubstanceDose, mg/kgTime output methylene blue, sCapillary effect, the difference in % of control
1234
Control-14.7±1.5*-
Betulin20021.7±3.8*47.6
40036.3±4.0*146.9
Dihydroquercetin10021.5±2.6*33.9
30025.4±2.8*77.7
*p<0.05 with respect to control

Application of 1%alcohol solution of betulin as capillary means.



 

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