Emulsion performancesin compounds for medical purposes, the method of its preparation and methods of treatment and prevention of diseases using

 

Emulsion performancesin compounds (PFOS) for intravascular injection consists of rapidly displayed perfluorocarbons and slowly expelled perfluorinated tertiary amine and optionally contains at least three species taken in small amounts of impurities PFOS. PFOS impurities close to the structure and physico-chemical properties the main PFOS. The emulsion also contains minor impurities of N-performancenow. Emulsion PFOS stabilized copolymer polyoxyethylene-polyoxypropylene. Upon receipt of the emulsion stabilizing agent is heated at a temperature of up to 75oWith all the components is saturated with carbon dioxide and homogenization is carried out by blowing carbon dioxide. The proposed method allows to minimize the appearance of peroxides and thereby reduce reactogenicity of the emulsion. The composition determines the stability of the emulsion during storage and when injected into the bloodstream, as well as a low viscosity emulsion of PFOS, which provides a high dynamic oxygen storage capacity of the drug and improves delivery of oxygen to the tissues. It is proposed to use emulsions of PFOS as a means for treating the air of fat embolism, peripheral occlusive vascular lesions of anecdotal., 2 Il.

Description text in facsimile form. The

Claims

1. Emulsion performancesin compounds (PFOS) for medical purposes containing quickly displayed the perfluorocarbons and slowly expelled perfluorinated tertiary amine, a stabilizing agent, a physiologically acceptable water-salt solution with substrates of energy metabolism, characterized in that it further contains an impurity at least three quickly displayed perfluorocarbons With7-C10and at least three slowly flushed perpertrating amines With11-C13similar physicochemical properties to the main performancesin compounds, in particular on the critical temperature of dissolution in hexane, and minor impurities of N-performancenow, the content of impurities quickly out of perfluorocarbons is not more than 15% of the content of the main perfluorocarbons, the content of impurities slowly flushed perpertrating amines does not exceed 50% of the content of the main perpertrating amine, and the content of impurities of N-performancenow not exceed 0.1% vol.

2. Emulsion PFOS under item 1, characterized in that the CIS - and transform.

3. Emulsion PFOS under item 1, characterized in that as the primary slowly flushed photostating amine is used a mixture of isomers of PERFLUORO-N-4-(methylcyclohexyl)-piperidine.

4. Emulsion PFOS under item 1, characterized in that the impurities are quickly displayed perfluorocarbons With7-C10are a mixture of performativity, PERFLUORO-1-methyl-3-propylcyclohexane, PERFLUORO-indane, PERFLUORO-4-codecasino, perftorpolietilena, perftorpolietilena, performcalculation, performatic-cyclopentane, PERFLUORO-1-methyl-2-ethylcyclohexane.

5. Emulsion PFOS under item 1, characterized in that the impurities are slowly flushed perpertrating amines With11-C13are a mixture of the isomers CIS - and transform PERFLUORO-N-(4-methylcyclohexyl)-2-methylpyrrolidine, performativity-(4-methylcyclohexyl)-amine, performativity-(4-methylcyclohexyl)-amine, performativity-(Methylcyclopentane)-amine and PERFLUORO-N-(4-methylcyclohexyl)-1-methylpiperidin.

6. Emulsion PFOS according to any one of paragraphs.1-5, characterized in that the ratio of fast loud slowly and loud PFOS is 2:1 or 3:1.

7. Emulsion PFOS according to any one of paragraphs.1-5, characterized in that the stabilization of the PFOS under item 1 or 7, characterized in that the content of the stabilizing agent is 2-4%.

9. Emulsion PFOS according to any one of paragraphs.1-8, characterized in that the physiologically acceptable water-salt solution comprises NaCl, KCl, MgCl2, NaHCO3, NaH2PO4and D-glucose.

10. Emulsion PFOS according to any one of paragraphs.1-9, characterized in that in the preferred embodiment, it contains: main quickly displayed the perfluorocarbons in the form of a mixture of CIS - and TRANS-isomers of performanceline in the amount of 6 vol.%; impurities quickly out of perfluorocarbons, which are a mixture of performativity, PERFLUORO-1-methyl-3-propylcyclohexane, TRANS-pertarungan, PERFLUORO-4-codecasino, perftorpolietilena, perftorpolietilena, performcalculation, perftorpolietilena, CIS-PERFLUORO-1-methyl-2-ethylcyclohexane in the amount of 0.7 vol.%; primary slowly flushed perpertrating amine in the form of a mixture of isomers of PERFLUORO-N-4-(methylcyclohexyl)-piperidine in the amount of 2.3 vol.%; impurities perpertrating amines, representing a mixture of PERFLUORO-N-(4-methylcyclohexyl)-2-methylpyrrolidine, performer-(4-methylcyclohexyl)-amine, CIS - and TRANS-isomers of performativity-(4-methylcyclohexyl)-amine, a mixture of isomers performancepro Balkany in the amount of 0.02 about. %; copolymer of polyoxyethylene-polyoxypropylene mol.m. 8 thousand Yes 4% and the ratio of units of polyoxyethylene and polyoxypropylene in the copolymer of 4:1.

11. Emulsion PFOS according to any one of paragraphs.1-7, characterized in that in the case of use for cruiseline and/or perfusion bodies of water-salt solution contains 102 mm NaCl, 5.2 mm KCl, 1.8 mm MgCl27.7 mm NaHCO3, 1,65 mm NaH2PO4and 11 mm D-glucose.

12. Emulsion PFOS according to any one of paragraphs.1-8, characterized in that in the case of use for cardioplegia water-salt solution contains 102 mm NaCl, 5.2 mm KCl, 1.8 mm MgCl27.7 mm NaHCO3, 1,65 mm NaH2PO4and 11 mm D-glucose, 5 mm sodium pyruvate, 5 mm-sodium oxybutyrate, 5 mm sodium succinate, 5 mm of sodium glutamate and 5 mm taurine.

13. The method of preparation of the emulsion photorealistic compounds for medical purposes described in any of paragraphs.1-12, comprising mixing sterile pyrogen-free components by passing a mixture of liquid performancesin connections through an aqueous solution of a stabilizing agent and subsequently repeated homogenization received predementia to bypass the high-pressure homogenizer, namely, that before the carbon dioxide, then heated aqueous solution of a stabilizing agent at a temperature not exceeding 75oC; serves a mixture of liquid performancesin compounds in the solution is cooled stabilizing agent, at least two jets in the atmosphere of carbon dioxide; intensively stirred prizemoney while passing through the first circuit of the homogenizer at a pressure of 300-450 kg/cm2; put the multiple emulsion homogenization in the second circuit of the homogenizer at a pressure of 400-600 kg/cm2; add a physiologically acceptable aqueous saline solution, in this case, the process of making predementia and subsequent homogenization is carried out in a carbon dioxide atmosphere.

14. The method of preparation of the emulsion on p. 13, characterized in that in the preferred embodiment, the solution of the stabilizing agent is heated at 70oWith over 12 hours

15. The method of preparation of the emulsion on p. 13, characterized in that prizemoney passed through the first circuit of the homogenizer 3-4 times, and then pass the emulsion through the second circuit 4-5 times.

16. The means of dissolving air and fat emboli in the bloodstream, which is the emulsion performancesin compounds on p. 1.

17. With hanicheskih compounds on p. 1.

18. Agent modulating the conversion of toxic lipophilic xenobiotics depending on the timing of the introduction of xenobiotics and the specified funds, representing emulsion performancesin compounds on p. 1.

19. Means on p. 18, which represents an adsorbent of toxic lipophilic xenobiotics in the blood stream.

 

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