Antihypoxic complex

 

(57) Abstract:

The invention relates to medicine, specifically to pharmacology. A new antihypoxic drug with combined action. As a new antihypoxic drug offered anticoagulant complex of heparin with serotonin in wt.% 3:1. A new tool for many indicators of resistance to hypoxia than the known drug-similar - Mexidol. table 1.

The invention relates to the use of known substances for a new purpose and can be used in medicine, physiology and preparation of athletes.

Hypoxia is accompanied by virtually any pathology. Acute hypoxic hypoxia generated in a pressure chamber is a rapid decline in oxygen tension while reducing the overall partial pressure. Currently, the search continues for antihypoxants, preference is given to drugs that have a combined effect.

Known antihypoxic substance, have an effect on animals and humans, for example, heparin [1].

The disadvantage of this substance is low antihypoxic activity.

As the prototype of the ka and animals [2].

The prototype has the following disadvantages:

1) the necessity of using large doses of Mexidol - not less than 40 mg/kg of body weight,

2) low efficacy, expressed in a small increase in the lifetime of animals in acute hypoxia,

3) the presence of contraindications to the use - expressed in the human liver and kidneys, if you are allergic to pyridoxine (vitamin B6).

As antihypoxic drug is offered a certain complex of heparin with serotonin, having anticoagulant properties [3]. This complex has pronounced antihypoxic properties and does not possess the disadvantages of the known solutions and prototype.

The goal is achieved by taking the complex of heparin:the serotonin (the weight. %) 1-3: 1-1,5, prepare a 0.1% solution. Take 10 rats, each of which is administered 0.3 ml of 0.1% solution of the complex for 10 min before placing them in terms of the pressure chamber, then create a negative air pressure corresponding to 12 thousand meters above sea level, record the time to loss of posture (rat motionless), fix the lifetime of the rats to the last agonal breathing, then rats quickly removed from the chamber and record the time restituition K, count how many out of 10 Wistar rats survive - it's called survival.

The proposed complex is used in comparison with the prototype in much smaller concentrations. Thus, the table shows that the complex you can enter animals in 111 times lower dose than the prototype - Mexidol. Indicators of adaptation to acute hypoxic hypoxia produced in rats using hyperbaric chambers have a better offer complex: thus, in comparison with the prototype, the complex increases the time to loss of posture 3.9 times, the lifetime is 3.3 times, K is 1.6 times the survival rate is 1.1 times. The proposed drug and the prototype, as you can see, does not affect the time of restitution, the appearance of muscle tone in rats.

Example 1. Take 1 g of heparin dissolved in 1000 ml of distilled water, taking 1.5 g of serotonin, dissolved in 1500 ml of distilled water, two solutions are mixed in these quantities, the mixture is placed in a thermostat at a temperature of 37oC for 15 min, after which the mixture from thermostat removed and adjusted pH with the aid of 0.1 H NaOH to 5.5, add 5-fold volume of chilled acetone, put the mixture in the refrigerator at a temperature of +4oC for 60 min, then the mixture is centrifuged for 15 min at 3000 rpm, the supernatant W is tonine in wt.% 1:1,5. Take 3 mg of dry complex, is brought up to 3 ml of 0.85% saline solution (pH of 7.2), get a 0.1% solution of the complex. Take 10 rats, each of which is administered 0.3 ml of a solution of the complex for 10 min before placing them in terms of the pressure chamber, then the chamber creates a negative air pressure corresponding to 12 thousand meters above sea level, record the time before the loss of the animal poses (rat motionless), loss of posture comes through 647,6 32,5 (average value calculated from the data obtained on 10 rats), then fix the lifetime of the rats to the last agonal breathing, it comes through 873,4 30,1 (average value), after that, rats quickly removed from the chamber and record the time of restitution, when I had muscle tone in the legs - it is to 129.3 15,9 c (average), dividing the time of life at the time of restitution, get the K - 5,2 1,9 (average value). Out of 10 Wistar rats survive 8, which is 80% - it's called survival.

Example 2. Take 3 g of heparin dissolved in 3000 ml of distilled water, taking 1.5 g of serotonin, dissolved in 1500 ml of distilled water, two solutions are mixed in these quantities, the mixture is placed in a thermostat at a temperature of 37oC for 15 min after CEG is on, put the mixture in the refrigerator at a temperature of +4oC for 60 min, then the mixture is centrifuged for 15 min at 3000 rpm, the supernatant liquid is poured, the precipitate is dried freeze, get a white crystalline powder of a complex of heparin:serotonin in wt.% 3:1,5. Take 3 mg of dry complex, is brought up to 3 ml of 0.85% saline solution (pH 7,4), get a 0.1% solution of the complex. Take 10 rats, each of which is administered 0.3 ml of a solution of the complex for 10 min before placing them in terms of the pressure chamber, then the chamber creates a negative air pressure corresponding to 12 thousand meters above sea level, record the time to the loss of animal posture, loss poses a rat comes in 698,2 47,6 with (an average value of data obtained on 10 rats), then fix the lifetime of the rats to the last agonal breathing, the life time is 902,2 31,3 (average value), after that, rats quickly removed from the chamber and record the time of restitution - when you receive the muscle tone in the limbs, the time of restitution is to 131.4 15,2 (average value), by dividing the time of life at the time of restitution, get the K - 6,8 2,1 (average value). Out of 10 Wistar rats survives 9 that 90%.

Example 3. Take 3 g of heparin, dissolve the and mix in these quantities, the mixture is placed in a thermostat at a temperature of 37oC for 15 min, after which the mixture from thermostat removed and adjusted pH with the aid of 0.1 H NaOH to 5.5, add 5-fold volume of chilled acetone, put the mixture in the refrigerator at a temperature of +4oC for 60 min, then the mixture is centrifuged for 15 min at 3000 rpm, the supernatant liquid is poured, the precipitate is dried freeze, get a white crystalline powder of a complex of heparin:serotonin in wt.% 3:1. Take 3 mg of dry complex, is brought up to 3 ml of 0.85% saline solution (pH of 7.2), get a 0.1% solution of the complex. Take 10 rats, each of which is administered 0.3 ml of a solution of the complex for 10 min before placing them in terms of the pressure chamber, then the chamber creates a negative air pressure corresponding to 12 thousand meters above sea level, record the time to the loss of animal posture, loss poses a rat comes in 712,4 41,3 (average value calculated from the data obtained on 10 rats), then fix the lifetime of the rats to the last agonal breathing, it comes through 951,2 24,2 (average value), after that, rats quickly removed from the chamber and record the time of restitution - when you receive the muscle tone in the legs - it is 128,5 17,5 c (average sachinidis survives 9, what is 90%.

Example 4. Take 1 g of heparin dissolved in 1000 ml of distilled water, take 1 g of serotonin, dissolved in 1000 ml of distilled water, two solutions are mixed in these quantities, the mixture is placed in a thermostat at a temperature of 37oC for 15 min, after which the mixture from thermostat removed and adjusted pH with the aid of 0.1 H NaOH to 5.5, add 5-fold volume of chilled acetone, put the mixture in the refrigerator at a temperature of +4oC for 60 min, then the mixture is centrifuged for 15 min at 3000 rpm, the supernatant liquid is poured, the precipitate is dried freeze, get a white crystalline powder of a complex of heparin: serotonin in wt.% 1:1. Take 3 mg of dry complex, is brought up to 3 ml of 0.85% saline solution (pH of 7.2), get a 0.1% solution of the complex. Take 10 rats, each of which is administered 0.3 ml of a solution of the complex for 10 min before placing them in terms of the pressure chamber, then the chamber creates a negative air pressure corresponding to 12 thousand meters above sea level, record the time to the loss of animal posture, loss poses a rat comes in 562,6 48,9 (average value calculated from the data obtained from 10 rats), then fix the lifetime of the rats to the last agonal breathing, time II restitution - when you receive the muscle tone in the limbs, the time of restitution is 118,7 21,3 sec (average), dividing the time of life at the time of restitution, get the K - 7,3+1,7 (average value). Out of 10 Wistar rats survive 8, which is 80%.

Sources used

1. Lyubimov B. I., Sholokhov C. M., N. Samoilov.H. Chigaev E. C. Pharmacological protection hypoxidaceae of autodermotransplantat//Materials of the 2nd all-Union conference "Pharmacological correction of hypoxic States", Grodno, 1991. S. 107-108.

2.Mashkovsky M. D. Medicines, 1993. 2nd, C. 216-217.

3. Kondashevskaya M. C., Lyapina L. A., Smolina T. Y. Complexes of high and low molecular weight heparin with serotonin and their physiological properties //Vestnik MGU, ser. 16 biological. 1996. N 2, S. 17-21.

The application of the known anticoagulant heparin complex: serotinin in wt.% 1-3:1-1,5 as antihypoxic drug.

 

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