Method for obtaining biologically active fraction s-1-10, a tremor-decreasing pharmaceutical composition at parkinsonism and convulsive activity-decreasing at epilepsy

FIELD: medicine.

SUBSTANCE: the present innovation deals with obtaining a biologically active peptide fraction out of poultry blood serum being useful at some human and animal diseases and disorders. It is necessary to carry out electrostimulation of a bird's head at the mode of about 70-80 V for about 2-3 sec to sample blood and incubate it at 4-8°C for about 18-24 h, then the serum sampled should be irradiated with C0 60 at the mode of 25±5.0 kGy and extracted after irradiation with 0.5 mM solution of phenylmethane sulfonyl fluoride in distilled water at the ratio of 1:10 to be mixed at 5°C for 1 h and centrifuged at 12000 rot./min for 30 min, then the residue should be repeatedly centrifuged under the same conditions, supernatant should be filtered successively through the membrane at pore's diameter being 0.45 mcm and 10 kDa, and a target product being a peptide fraction at molecular weight up to 10 kDa should be lyophilized and kept at about 4-8°C. The suggested pharmaceutical composition is characterized by the fact that as an active substance it contains efficient quantity of peptides of molecular weight up to 10 kDa obtained to a certain technique and a pharmaceutically acceptable carrier or filler. The innovation enables to obtain new biologically active peptide fraction up to 10 kDa and develop its medicinal form.

EFFECT: higher efficiency.

2 cl, 2 ex, 3 tbl

 

The technical field to which the invention relates.

The present invention relates to medicine, can be used to obtain biologically active peptide fraction from the serum of birds useful for a number of diseases and disorders in humans and animals (physical fitness, coordination of movements, parkinsonism, epilepsy, stress, etc.)

The level of technology

Widely known methods for producing biologically active blood serum based on drawing blood from donors and animals, incubation, separation and subsequent preservation. The methods involve obtaining a serum that increases the body's resistance to such exogenous and endogenous factors, such as atmospheric pressure, temperature, gravity, light, etc. as well as hunger, thirst, sleep and sexual needs, etc. (Japan Patent No. 2123287, EP 0542303 A2, Patent of Russia №2096041, 2120301).

Serum obtained from blood donor, previously entered into a certain functional state, in this case, depending on the nature of the impact, get a serum with the biological activity of different nature: myogenic, somnolence, oftalmologii, audioactive, thermosetting, detectivey, exactive, antihypoxic, anti-alcohol and antinicotine.

Serum from animals subjected to g of the MMA-processing to enhance biological activity (patent PCT/RU00/00073 - Russia and the EP).

The objective of the invention was to obtain biologically active peptide fractions up to 10 kDa from stun the blood serum of chickens.

Summary of the invention

It turned out that if you stun the serum of birds to be irradiated in the range of 20-30 kGy, filtered through a membrane of 0.45 mm and 10 kDa, it is possible to obtain low molecular weight biologically active peptide fraction having a range of activities (will be disclosed hereinafter), which are useful under certain unfavorable conditions of the patient (will be revealed later).

Thus, the aim of the present invention is to develop a new method of obtaining biologically active peptide fractions S-1-10.

Another objective of the present invention is the development of dosage forms of new biologically active serum. The invention involves various dosage forms, including oral, parenteral, nasal, buccal, in the form of suppositories and thepwnageninja.

The invention provides for the use of suitable physiologically acceptable carriers (such as distal. water, Fiziol. R-R), fillers (for example, cocoa butter, witepsol), biologically active peptide fractions. Stun biologically active peptide fraction can be used both independently and in which Oceanie with other therapeutic agents.

An additional aim of the invention is a pharmaceutical composition in which the active principle is a peptide fraction according to the present invention. This pharmaceutical composition should contain the active ingredient in a quantity sufficient to exert a positive influence on the patient's body, i.e., to contain it in an effective amount.

Another aim of the invention is the determination of the effective dose of the peptide fraction in accordance with this invention. It is believed that this dose is in the range from 0.1 to 50 mg/kg weight of the patient. It is obvious that the specific dose will be determined by the attending physician depending on the patient's condition, its age, weight and treatment.

Detailed disclosure of the invention

Further, the invention disclosed in detail preferred embodiments, specific performance, with examples of the active peptide fraction, pharmaceutical compositions, dosage forms should not become the basis for the limitations of the claims, and is intended only to demonstrate the feasibility of the invention and implementation(s) destination(s). Every specialist in this field will certainly make sure that can be offered numerous modifications of the described embodiment of the invention that fall is under claim, reflected forth in the claims.

1. Obtaining biologically active peptide fractions S-1-10.

For obtaining biologically active peptide fractions S-1-10 used the blood of birds (chickens), taken after 3-4 s after the stimulation of the head within 2-3 with the voltage of 70-80 C. Blood was collected by samotekom in polyethylene bottles after transection of the carotid arteries and veins and incubated at a temperature of 4-8°C for 18-24 h, the serum was aspirated and was irradiated With060mode 25±of 5.0 kGy.

The treated serum was extracted with distilled water containing 0.5 mm phenylmethane sulfonyl fluoride (PMSF) at a ratio of 1:10, stirred for 1 h at a temperature of 5°C. the resulting suspension was centrifugally at 12000 rpm for 30 minutes the Precipitate was extracted again with water PMSF and again centrifuged at 12000 rpm for 30 minutes the Supernatant was filtered through a membrane with pore diameter of 0.45 μm, and then the filtrate was again filtered through a 10 kDa membrane. The final filtrate (peptide fraction) liofilizirovanny conventional method and kept at a temperature of 4-8°C.

2. Evidence of biological activity of peptide fractions S-1-10.

2.1. Physical endurance of animals

Physical endurance was determined by the influence of peptide fractions on the duration of the plan the project of Wistar rats at 25° With a weight at the base of the tail mass to 10% by weight of the animal. In the experiment used 40 rats weighing 180-200 g Rats were divided into 4 groups of 10 animals in each group. group 1 - control, rats were injected with 1.0 ml of physiological solution, II, III and IV groups were injected peptide fraction at doses of 0,1; 1,0; 50.0 mg/kg of body weight, dissolved in 1.0 ml of saline.

All the investigated solutions was injected intraperitoneally 30 min before testing.

The results are presented in table 1.

Table 1
The influence of peptide fractions on the physical endurance of animals (M+m)
Statistician. indicatorsControlThe dose of peptide fractions (mg/kg)
0,11,050
M+m3′31±24′′4′23±26′′4′36′′±29′′5′27±36′′
P>0,05>0,05<0,05

Thus, the peptide fraction in a dose of 50 mg/kg of body weight increases physical endurance for 54% of the control.

2.2. Parkinson's disease

When modeling disease Parks the Sona was used similar 6-DG - oxotremorine, which caused the animal changes, typical for Parkinson's disease: tremor of the limbs, the latent period beginning total tremor (whole body), periods of absence of tremor, cessation of tremor.

Oxotremorine was administered intraperitoneally at a dose of 1.0 mg/kg body weight in saline solution taken in a volume of 1.0 ml of the Peptide fraction was injected in doses of 0,1; 1,0; 10,0; and 50 mg/kg of body weight, also dissolved in 1.0 ml of saline. The fraction was administered 45 minutes before applying oxotremorine. In the experiment were used 49 Wistar rats weighing 200-220 g

The results are presented in table 2.

Table 2
The influence of peptide fractions on tremor in Parkinson's disease (M±m)
Indicators of tremorControlDose fraction (mg/kg)
0,11,010,050,0
1. The latent period beginning tremors of the extremities (C)64,4±3,885,0±7,1

>0,05
92,8±7,3

<0,05
126,4±17,7

<0,01
157,1±26,0

<0,01
2. The latent period beginning total tremor animals (C)216,4±21,7294,4±19,< 0,05NoNoNo
3. The occurrence of periods of absence of General tremor (min)7,4±0,56,7±1,0

>0,05
NoNoNo
4. Cessation of tremor of the extremities (min)32,1±5,721,3±2,5

<0,05
21,2±2,3

<0,05
23,1±3,1

<0,05
14,9±4,0

<0,01

Thus, the peptide fraction entered for 45 min to modeling Parkinson's disease, even at a dose of 0.1 mg/kg of body weight lengthens the period of the beginning of the total tremor (tremor of the limbs and trunk) by 31% and reduces the time of the disappearance of tremor of the limbs 50% of control. Doses in the range of from 1.0 to 50 mg weight are most effective, not only changing the parameters specified in 2 times (at a dose of 50 mg/kg), but completely prevent common tremor animals (dose: 1,0; 10.0 and 50.0 mg/kg).

2.3. Epilepsy

Investigated the effect of various concentrations of peptide fractions at the beginning of the appearance of tonic and clonic seizures in the simulation of epilepsy by intraperitoneal administration of 0.5 ml of 20% solution of camphor.

Lyophilized samples of peptide fractions, dissolved in 0.5 ml of physiological solution, also the were performed intraperitoneally 45 minutes before injection of camphor.

Were investigated 4 sample peptide fraction at doses of 0,1; 1,0; and 10.0 and 50.0 mg/kg of body weight of the animal.

Just used 50 Wistar rats weighing 220-230,

The results are presented in table 3.

Table 3
The influence of peptide fractions on seizures and epilepsy (M+t)
Parameters seizure activityControl (camphor)Dose fraction(mg/kg)
0,11,010,050,0
1. The beginning of tonic convulsion (min)
6,7±0,87,1±1,1

>0,05
9,0±1,0

<0,05
10,4±1,1

<0,01
11,0±1,4

<0,01
2. Beginning clonic seizures (min)14,3±1,015,7+1,618,7+1,420,0±1,920,6±1,0
>0,05<0,05<0,01<0,01

Thus, the peptide fraction, entered za minutes before modeling epilepsy, taken in doses of from 1.0 to 50 mg/kg of animal weight, lengthen the time of manifestation of tonic and clonic seizures by 30-50%, respectively, i.e. reduce seizure manifestation of epileptic disease.

1. The method of obtaining biologically active peptide fractions, reducing tremor in Parkinson's disease, seizures and epilepsy, characterized by the fact that conduct the electrical stimulation of the bird's head mode In 70-80 2-3 with, take blood, incubated at 4-8°C for 18-24 h, and then selected the serum is irradiated With060mode 25±of 5.0 kGy, extracted after exposure to 0.5 mm solution phenylmethane sulfonyl fluoride in distilled water at a ratio of 1:10, stirred at 5°C for 1 h, centrifuged at 12000 rpm for 30 min, then the precipitate is re-extracted with a solution phenylmethane sulfonyl fluoride, re-centrifuged under the same conditions, the supernatant was filtered successively through a membrane with pore diameter of 0.45 μm and 10 kDa, and the target product, which represents the peptide fraction with a molecular mass of 10 kDa, and lyophilizers stored at 4-8°C.

2. Pharmaceutical composition for reducing tremor in Parkinson's disease, seizures and epilepsy, characterized in that the active agent contains an effective amount of PE is the Chida with a molecular mass of 10 kDa, received according to claim 1 and a pharmaceutically acceptable carrier or excipient.



 

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