A method of treating gastric ulcers in experiment

 

(57) Abstract:

The invention relates to experimental and clinical medicine and medical concerns methods of prevention and treatment of peptic ulcer. The purpose of the invention is improving the efficiency of prevention of ulcerative lesions of the mucous membranes of the stomach and duodenum with different etiology of the disease. The essence of the proposed method is that as a preventive and drug use antidepressant sydnonimines number sidnofen in combination with the amino acid arginine. 4 Il.

The invention relates to experimental and clinical medicine and for the prophylaxis and treatment of peptic ulcer disease.

Peptic ulcer disease is extremely widespread and is one of the causes of the disability of a significant part of the population. Causes of peptic ulcers are diverse and etiological role to play as neurogenic disorders of the Central and peripheral mechanisms. In this regard, a variety of and approaches to prevention and treatment of this disease, involving the use of drugs acting on different functable released hydrochloric acid and pepsin with antacid drugs type of magnesium oxide, suppression of secretion of hydrochloric acid by using the anticholinergic type of atropine, pirenzepine (gastrochaena) or histamine receptors blockers, such as cimetidine, ranitidine;

regulation of motor functions of the stomach and duodenum, with the participation of drugs such as reglan;

stimulating the production of gastric mucus under the influence of drugs type of carbosilane sodium;

enhancing blood circulation and regeneration of the mucous membrane of the stomach using solkoserila, prostaglandin and similar drugs.

Because it is not always clear pathological mechanisms leading to the occurrence of peptic ulcer disease, an effective therapeutic tool sometimes you have to choose individually.

Closer to the proposed to the technical nature of the method of treatment of peptic ulcer disease is the impact on the Central mechanisms of regulation by psychotropic drugs with antidepressant activity, in particular, azafen. The relative lack closest analogue (prototype) of the proposed method is low efficiency of prevention of ulcerative lesions of the gastric mucosa.

Celestina goal is achieved by the use of psychotropic drugs with antidepressant activity, derived sydnonimines number, in combination with the amino acid arginine.

A typical representative of psychotropic drugs such can be considered the drug of sinoven allowed in the prescribed manner for use in medical practice.

Conducted research for the first time, it was found that psychotropic drug sidefan, has antidepressant activity and derives sydnonimines patterns, shows the ability to prevent the formation and development of damage of the gastric mucosa at the commencement or during the course of ulcer disease. This drug showed high protective activity in experimental cases of peptic ulcer induced by intragastric introduction of ethanol in animals (ethanol model) or immobilization by cold stress (immobilization and cold model). However, sidnie proved ineffective in protecting the mucous membrane of the stomach from ulcers in the simulation of peptic ulcer disease by administration of indomethacin blocker of prostaglandin synthesis (indomethacin model). It was found that a pronounced protective effect is due to the simultaneous influence what aspects of the action due to antidepressant activity, the result can be achieved normalization of regulatory mechanisms of the autonomic nervous system, peripheral violationsin action and increase the protective properties by increasing blood flow.

Inefficiency sidnofena and its analogues in the case of indomethacin model ulcers can presumably be explained by the fact that ulcers in this case, due to the deterioration of the microcirculation in the gastric mucosa.

In this regard, it is obvious that matrotrophy drugs with antidepressant activity derived sydnonimines patterns are not universal antiulcerogenic means and in some cases may not be therapeutic and prophylactic effect.

However, it was found that the combination mentioned neurotropic drugs with arginine antiulcerogenic effect in experimental peptic ulcer, simulated different methods used, including indomethacin model.

In addition, the protective effect of the combination sydnonimines adjunct and arginine in the case of an ethanol model ulcer disease is more pronounced than the protective effect antiulcerogenic activity sidnofena, arginine and their combination with indomethacin model ulcerative lesions of the stomach.

Sidnofen was administered to the experimental rats at the dose of 15 mg/kg, arginine at a dose of 300 mg/kg, and in the case of the combined effects of these doses were summed.

Y-axis (see Fig. 1) shows the magnitude of the reduction of the severity of the damage of the gastric mucosa, expressed as a percentage to the severity of mucosal injury in control animals. OF sidnofen; And arginine.

The results show that sidnofen virtually had no impact on the severity of the damage, arginine reduced this figure by 11% and the combination of sidnofena and arginine reduced the severity of injury to the mucosa by 45%

Experimentally it was found that the effectiveness of the combination sidnofena and arginine in terms of indomethacin models of peptic ulcer disease to a certain extent depends on the ratio of the doses of the drugs used.

For the Fig. 2 presents antiulcerogenic activity of the drug containing sidefan and arginine, with their different ratio in terms of indomethacin model ulcerative lesions of the stomach.

Sidnofen was administered to the experimental rats at the dose of 15 mg/ing the severity of gastric mucosal injury compared with the severity of damage control animals. OF sidnofen, And arginine.

The presented results show that the maximum active preparation containing 15 mg/kg sidnofena and 200 mg/kg of arginine.

Clearly seen that at a lower dose of arginine (200 mg/kg) antiulcerogenic activity is not shown because the effect of the combination sidnofena and arginine does not differ from the effect provided only by arginine. It is important to note the fact that for individual use only arginine its effectiveness is markedly reduced with increasing doses of arginine over 200 mg/kg.

The above can conclude that the maximum protective effect of combination sidnofena and arginine due to not total, and synergene effect in a certain concentration range.

Previously arginine as such for the treatment of peptic ulcer disease has not been applied and information on the strengthening of arginine antiulcerogenic activity of neuroleptics sydnonimines number was not available.

Some antiulcerogenic activity of the arginine and strengthening them antiulcerogenic activity of neuroleptics sydnonimines nature may be due to the fact that arginine increases blood flow to the mucous membrane, uluchshit due to quite other causes.

A more pronounced antiulcerogenic effect of combination sidnofena with arginine in comparison with similar effects sidnofena and arginine has occurred in the conditions of ethanol model ulcer disease.

In Fig. 3 presents antiulcerogenic activity sidnofena and its combination with arginine in ethanol model ulcerative lesions of the stomach. On the x-axis denoted by a separate series of experiments, on the axes of ordinates: left the lesion (TA) and ulcer index (YAI) to the right frequency of lesions (PE).

Dose sidnofena changed (I 2.5 mg/kg, III 12.5 mg/kg; V 25 mg/kg), the dose of arginine was constant at 200 mg/kg (II, IV, VI in combination with sidnofena at a dose of 2.5, 12.5 and 25 mg/kg, respectively). In optimal dose of 12.5 mg/kg sidnofen reduced the severity of the damage to 0.7 points (III) and in combination with arginine to 0.3 points (IV), control (VII) 2.4 points. More than twice decreased and the frequency of damage when using this combination in comparison with the case of using only sidnofena.

In other words, as in the case of indomethacin model, arginine increased antiulcerogenic activity sidnofena.

In comparison with classical antiulcer drugs, sydnonimine the major side effects.

In Fig. 4 shows the comparison of the antiulcer action of gastrochaena (1), atropine sulfate (2) and combinations sidnofena with arginine (3). Along the ordinate axis the value of reduction of damage of the gastric mucosa with ethanol model of ulcer formation in damage control animals. Dose pirenzepine, atropine sulfate and sidnofena 15 mg/kg, arginine 200 mg/kg clearly shows that widely currently used in the clinic gastrotsepin reduced damage just by 37% and the combination of sidnofena with arginine 83%

Thus, the protective function of the mucous membrane of the stomach from ulcers proposed remedy has advantages and provides on the one hand the reduction of aggressive factors (reduces the secretion of hydrochloric acid and pepsin), and on the other hand potentional antiulcerogenic effect of protective factors for each component of the composition.

It should be noted that pronounced antiulcerogenic effect was achieved at doses sydnonimines antidepressants order of magnitude below the dose required for the manifestation of antidepressant activity.

All studies on the Central action sidnofena in rats in conditions of vnutrivennogo is doing in doses of at least 2 mg/kg weight of the animal. By experimentation it was found that protective antiulcer effect is already at the dose of 0.01 mg/kg weight of the animal, i.e. almost three orders of magnitude in a smaller dose, and in conditions intramuscular (not intravenous) administration.

As for practical advice on the use of sidnofena and arginine in clinical medicine, the optimal dosage of the drug should provide content sidnofena level permitted therapeutic doses or below it, and the dosage of arginine should be at the level of physiological needs of the organism in this amino acid.

It is advisable to assign sidefan and arginine in the form of an integrated product, but it is possible their simultaneous reception separately.

P R I m e R 1. Experimental rats were divided into four groups of 5 animals and all animals were simulated ulcerative lesions of the mucous membrane of the stomach, entering intragastric absolute ethanol (1 ml/100 g mass.

Animals of the control group at 24 h and 1 h prior to the introduction of ethanol was injected intramuscularly with 0.2 ml of physiological solution, and the experimental animal or 0.2 ml sidnofena (25 mg/kg), or 0.2 ml arginine (200 mg/kg), ilinykh control group was 150 mm, animals treated only sidnofen 28 mm, in animals receiving only 80 mm arginine; animals treated total drug sidnofena and arginine 5 mm

P R I m m e R 2. Experimental animals were divided into 4 groups of 5 animals in each group and all animals were simulated ulcerative lesions of the gastric mucosa subcutaneous administration of indomethacin (30 mg/kg).

Animals of the control group at 24 h and 1 h before injection of indomethacin was injected intramuscularly with 0.2 ml of physiological solution, and the experimental animal or 0.2 ml sidnofena (15 mg/kg), or 0.2 ml arginine (200 mg/kg), or 0.2 ml amounts of these drugs.

The average damage of the mucosa in animals of the control group amounted to 120 mm, in animals receiving only sidnofen 80 mm, in animals treated with only 23 mm arginine, in animals treated with total drug sidnofena and 10 mm arginine

A METHOD of TREATING GASTRIC ULCERS IN the EXPERIMENT by injecting drugs antidepressant action, characterized in that impose sidefan in combination with arginine.

 

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