Pharmaceutical composition having immunomodulatory and hypolipidemic effect

 

(57) Abstract:

The proposed active pharmaceutical composition containing as active principle of natural zeolite, which is represented by clinoptilolite contained in the volcanic tuff Chuguev field. Technical result: immunomodulatory and hypolipidemic action of the drug for a number of diseases. 1 C.p. f-crystals, 2 tab.

The invention relates to medicine, more specifically to medicines of natural origin, which have immunomodulatory and hypolipidemic activity, and can be used for the treatment and prevention of a wide range of diseases.

It is established that the normalization of the physiological state of a person can be done either directly by acting on the pathology with etiopathogenetic drugs (hormones, neurotransmitters, growth factors, antibiotics, and so on) that allow direct effects on target cells by the reception or indirect effects on body systems immunomodulators responsible for maintaining the parameters of homeostasis.

We know a significant number of immunomodulators, floor(N 0068513), from thymus (NS 4571336, CH 659586, DE 3128503), from human urine (EP 0069232), medicinal plants (WO N 9201401), brain, spleen (3679798).

It is also known drug, effective at the dysfunction of the immune system in the treatment of coronary heart disease, which represents the active fraction of lipids derived from omentum (N 4474773, WO 87/03811).

To normalize the physiological parameters of the whole body are very successfully used medicines derived from components of the cell membranes of animal tissue that is able to respond to changes in the parameters of homeostasis of the body with their introduction, i.e., in the case of normalization of homeostasis action of the drug is terminated due to the effect of bilateral relations (EP 0157424 - prototype).

A characteristic disadvantage of known drugs is the way they are received, which is a technologically complicated procedure, as well as significant variability in their physical and chemical properties, which make difficult to standardize.

Another disadvantage of most known biologically active agents is the presence of immunosuppressive drugs and dietary fibers, which can cause ava, possessing immunomodulatory effects, which leads to normalization of parameters of homeostasis and lipid metabolism.

It is established that the known mineral zeolite can be used for the treatment of secondary immunodeficiencies, developing, for example, in cancer patients, and patients suffering from ischemic heart disease and bronchial asthma.

Zeolite is known as a valuable natural raw materials, which due to the unique sorption, breeding and catalytic properties are widely used in industry and in agriculture (WO 8700049 1987, WO 91/01737); "Mineralogical encyclopedia", Nedra, 1985), including as an additive in animal feed (WO 84/04682). Now it has been confirmed the usefulness of the zeolite in medicine as a drug in bone diseases (WO 89/06965).

In the invention was used natural zeolite Chuguev deposits of Russia, which is a clinoptilolite (Na6[Al6Si30O72] 24 H2O) with a small admixture of mordenite (Na3[Al8Si40O96] 24 H2O) at 82-85% clinoptilolite content.

In accordance with the size of the Eastern part of the reach 9,43 and set the predominant cations of zeolite-containing rocks Chuguev deposits are moderately-high-silicon calcium-sodium-potassium.

Preparation of funds is carried out in the factory traditional volume-weight method. Meanwhile, the technological process of preparation involves the sterilization of powder sharanam method at 180-200oC for 20-30 minutes

Upon receipt dosage forms of pharmaceuticals to the current beginning immediately before use add the appropriate solvent.

The solvent may be used in any pharmaceutically acceptable carrier suitable for oral administration, including distilled water, saline solution, starch, glucose, glycine and other solvents that do not cause gastrointestinal discomfort.

The drug contains zeolite in an amount, effective for the manifestation of immunomodulatory and hypolipidemic actions. The preferred zeolite in the preparation for oral administration of 10 to 60%, because at this concentration provides optimal pharmacological effect.

The study of toxicity.

The drug in the finished dosage form was administered to animals orally daily at a dose of 0.3 g/kg body weight over a 7-10 day animals was carried out for 1.5-3 months after the end of injection. Clinical and biochemical blood tests and investigated the composition of urine. Daily throughout the experiment determined the body weight of animals.

The death of animals was not observed in any case. The animals tolerated the drug well and gained weight.

At necropsy macroscopic changes in the organs is not marked. It was found that the dose of 0.045 g, component 490 therapeutic doses for humans, does not lead to death.

In the study of the peripheral blood system, significant changes were not found, all values varied within the physiological norm. Urinalysis revealed a lack of nephrotoxicity of the proposed drug.

The research results allow to conclude that the claimed product is non-toxic and well tolerated by the animals, even in high doses.

Information, warning of the possibility of carrying out the invention.

1. Immunomodulatory effects of zeolite in the treatment of patients with bronchial asthma.

For the evaluation of immunomodulatory activity of zeolite used the dynamics of the clinical picture, the volume change etiotropic icev with infectious-allergic and atopic form of bronchial asthma at the age of 32-50 years, which the zeolite was administered once a day for half an hour before meals and medicines at a dose of preferably 50 g / day to achieve clinical effect, and then 15-20 g in the next 3 months.

To assess the effectiveness of the treatment studied the dynamics of the clinical picture, conducted clinical biochemical and immunochemical studies of the blood, the study of respiratory function, the change of volume of etiotropic and pathogenetic therapy.

When assessing the clinical picture in the treatment claimed by the drug marked the cessation of attacks of breathlessness, as well as their duration on the 1st-3rd day, stop using pocket inhaler within one week from the start of the reception, the decrease in attacks within 2-5 days and complete cessation after the 7th day of admission. After the 5th day of admission was stopped, and then disappeared completely shortness of breath, cough, significantly increased phlegm and decreased its viscosity, thus reducing the need for sympathomimetics marked on 14-20 days, and in patients with hormonal dependence of the hormone dose was decreased from 3-4 days of reception of the zeolite to a complete halt within 2-4 weeks followed by a complete rejection of hormones during 6-7 esni during flowering herbs and other situations causing aggravation. Remission was approximately 8 months, with the reception of the zeolite in the treatment period amounted to 600 g per month.

When using the claimed drug therapeutic effect was observed both in monotherapy and in combination with other treatments, did not depend on duration of disease. While side effects and drug intolerance were observed.

Immunomodulatory effects claimed the drug was evaluated in the dynamics before and during treatment. When this was investigated following indicators: number of serum immunoglobulins Ig A, Ig M, Ig G, the content of B-lymphocytes, T-lymphocytes, the absolute content of T-helpers and T-suppressors and their relationship.

In table. 1 shows the results of a study of the effect of zeolite on the immunological characteristics of the blood of patients with bronchial asthma. Values are calculated from the average indicator values (P 0.05).

The results obtained indicate recovery in peripheral blood content of a subpopulation of T-lymphocytes to the level of normal values. The main indicator of immunomodulatory activity is the ratio of T-helpers and T-suppressors, is katalogowanie zeolite for correction of immune deficiency in cancer patients.

It is known that cytotoxic and radiation therapy, which constitutes the basis of drug treatment for cancer often causes depression hemopoesis. Toxic mielodeprescia registers in the peripheral blood as leukopenia, thrombocytopenia and anemia next, while there has been development of immunodeficiency, which manifests itself in a sharp decrease in the content of immunological factors.

Tested the claimed preparation in 10 cancer patients aged 52 to 69 years. The zeolite was administered once or twice in a dose of from 30 to 60 g per day. Drug use led to improvement of the General condition in 3 days, the disappearance of clinical signs of endotoxemia.

Four of the examined patients took the drug at a dose of 50 g per day during the year, remaining in the same dose from 4 to 7 months.

Analysis of immunological parameters held in the dynamics, showed that the use of zeolite caused normalization of the content in the peripheral blood total lymphocyte fraction of T-lymphocytes and a subpopulation of T-lymphocytes helper.

Data normalization ratio of T-helpers and T-suppressors also confirm VOSSTANOVITEL, evaluated in the diagnosis of pathogenic form of the disease, are normalized under the influence of the requested drug.

3. Hypolipidemic or normalizing lipid metabolism effect of zeolite in the treatment of patients with ischemic heart disease.

To evaluate the hypolipidemic actions alleged drug used dynamics of the clinical picture, the volume change etiotropic and pathogenetic therapy, as well as indices of lipid content in the peripheral blood of patients-volunteers suffering from ischemic heart disease, atherosclerosis of the coronary vessels in the presence of angina and against the background of myocardial infarction aged 35-59 years.

All patients were treated zeolite at a dose of 30 to 60 g per day, preferably 30-40 grams per day against medical and non-medical treatment for 7 days, then the dose was reduced to 15-20 grams per day. The drug was administered to patients within 3-5 months with a break of 2-3 weeks.

When assessing therapeutic effect observed ischemia and termination of the arrhythmia on the 3-5th day, ischemia angina, reduce the dose of nitrates in 5-8 days. During stopping and the diet recommended by the doctor tietoleonia lipid components in blood, evaluating the results of the use of zeolite for 5 months (given the average). When this was investigated following indicators: total lipids (OL), HDL (high density lipoprotein), LDL (low density lipoprotein), triglycerides, and atherogenic index (IA).

These data indicate normalizing effect of treatment with zeolite on lipid metabolism, which is manifested in the increase in the content of HDL while reducing LDL.

Thus, the pharmaceutically active composition containing zeolite, shows a pronounced immunomodulating and hypolipidemic effect that makes the promising use of this non-toxic, affordable and good standard of natural treatment for a wide range of diseases, as it implies the rejection massive pharmacotherapy, allows to have a stable and reproducible pharmacological effect.

Example 1. Patient E., K. D., 43, was admitted to the hospital with a diagnosis of primary liver cancer.

A course of chemotherapy: cyclophosphamide, prednisolone and other patient was noted immunodeficiency, which developed on the background of the underlying disease. Zeolite application is impositon increased from 300 to 1800/mm3T-lymphocytes from 22.9 to 60.5%, and T-lymphocyte helper cells from 13.2 to 45.3%.

Conclusion: significant improvement in General condition, achieved prolonged disease remission.

Example 2. Patient K. A. I., 1953 birth. Diagnosis: ischemic heart disease, acute peredneperegorodochnoj myocardial infarction, atherosclerotic cardiosclerosis, arterial hypertension.

The patient was admitted on the 5th hour from the beginning of the development of pain, localized in the chest, not stopping nitroglycerin. Objectively, when ECG lifting ST(V1-V5), heart rate 98 in 1 min, a/D 10/90 mm RT.article.

The patient was conducted therapy with nitrates - blockers and zeolite 60 g per day 1 to day 7. In the future, the dose was reduced to 20 grams per day. The acute period was without complications, the content of HDL and LDL was at receipt is respectively 1.3 and 9.3 g/l, and at discharge, respectively, 1.7 and 5.7 g/l Marked improvement in hemodynamic parameters, content E4C POK 66%, E POK 19%, CEC 21,93 g/ml; at discharge, respectively 43%, 14%, to 11.9 g/ml.

Example 3. Patient A. B. C., 1964 birth, was admitted to the hospital with a diagnosis of bronchial asthma in acute phase. Ill for 7 years, the observed symptoms: recurrent attacks of breathlessness, OTE is their hormones; sympathomimetics parenteral (0.15 ml 1% R-RA adrenaline); drip isotonic solutions. The course of conducting zeolite (in the early days of 50 g/day to achieve clinical effect, then the dose was reduced to 20 g/day for 3 months) has led to the following results: asthma was stopped on the 3rd day; after 2 weeks of receiving a reduced dose of hormones to the complete cessation of the use of handheld nebulizer to the end of the month. Marked stable remission within 6 months from the start of the reception of the zeolite. Data immunological blood tests are given in table. 1.

Pharmaceutical composition having immunomodulatory and hypolipidemic action, including the active ingredient and a pharmaceutically acceptable carrier to provide oral administration, characterized in that, as an active ingredient contains natural zeolite in an effective amount.

2. The composition according to p. 1, characterized in that the zeolite is represented by clinoptilolite contained in the volcanic tuff Chuguev field.

 

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