CH239643A - Process for the preparation of an aqueous solution of a molecular compound of lactoflavin. - Google Patents

Description

  

  



  Process for the preparation of an aqueous solution of a molecular compound of lactoflavin.



   For certain therapeutic applications it is necessary to be able to use Laotonavin (vitamin Bs) in the form of an aqueous solution. However, lactoflavin is only slightly soluble in water. It is well known that lactoflavin in the form of its alkaline reacting salts dissolves easily in water. Such solutions, however, have a strongly alkaline reaction and are not stable. The use of solubilizers has therefore been proposed. The solubilizers known so far (cf., for example, D. R.

   P. No. 688 047) only cause a relatively modest increase in solubility and require the use of large volumes and large amounts of the solubilizer in relation to the active substance dissolved.



   It has now been found that the water-soluble salts of 2,4-dioxybenzoic acid, in particular their alkali and alkaline earth salts and the salts with aliphatic amines, are good solubilizers for lactodavine.



  From the lactoflavin and the water-soluble salts of 2,4-dioxybenzoic acid, new, stable, isolable molecular compounds of a certain composition are formed, which in water, especially if there are also alkali, alkaline earth or amine salts of 2,4 Contains dioxybenzoic acid, are easily soluble.

   The 6% solution of the sodium salt can dissolve about 0.5%, the 25% solution of the lithium salt can dissolve more than 3% lactoflavin; The magnesium or calcium salt can also be used successfully. So far it has not been possible to produce lactoflavin solutions of such high concentration.



   The salts of dioxybenzoic acid are completely non-toxic and well tolerated. Intravenous administration of 1.5 g / kg is tolerated by rabbits without any symptoms.



  The pu of such solutions is between 5 and 6, an area in which lactoflavin is completely stable.



   The subject of the present patent is a process for the preparation of an aqueous solution of a molecular compound of lactoflavin, which is characterized in that the sodium salt of 2,4-dioxybenzoic acid is allowed to act on lactoflavin.



   The resulting molecular compound of lactoflavin and 2,4-dioxybenzoic acid sodium can be isolated from the aqueous solution by partially evaporating the latter, filtering the solution and adding acetone to the filtrate. The crystals of the molecular compound that form after a short time are dark yellow in color and easily soluble in water. They only decompose at temperatures above 350¯C. The rotation of the 1% aqueous solution is ¯ 0¯.



   Lactoflavin alone forms pale yellow crystals that are difficult to dissolve in water. It melts at 314-316¯ with decomposition, its alkaline solution shows a rotation of α20 = - 116¯.



   The colorless crystals of the sodium salt of 2,4-dioxybenzoic acid dissolve in water; decomposition occurs when heated to 900 ".



   The obtained aqueous solutions of the lactoflavin molecular compound are intended to be used as medicaments.



   Example:
5.5 parts by weight of the sodium salt of 2.4 dioxyhenzoic acid are dissolved in 100 parts by weight of water and this solution is shaken with 0.5 parts by weight of lactonavin at constant temperature until it has completely dissolved.



     PATENT CLAIM:
Process for the production of an aqueous solution of a molecular compound of lactoflavin, characterized in that the sodium salt of 2,4-dioxybenzoic acid is allowed to act on lactoflavin.



   The molecular compound forms dark yellow crystals which only decompose at temperatures above 350¯. It is easily soluble in water. The rotation of the l "/ o aqueous solution is ¯ 0¯.

** WARNING ** End of DESC field could overlap beginning of CLMS **.



 

Claims (1)

** WARNING ** Beginning of CLMS field could overlap end of DESC **. Lactoflavins, which is characterized in that the sodium salt of 2,4-dioxybenzoic acid is allowed to act on lactoflavin. The resulting molecular compound of lactoflavin and 2,4-dioxybenzoic acid sodium can be isolated from the aqueous solution by partially evaporating the latter, filtering the solution and adding acetone to the filtrate. The crystals of the molecular compound that form after a short time are dark yellow in color and easily soluble in water. They only decompose at temperatures above 350¯C. The rotation of the 1% aqueous solution is ¯ 0¯. Lactoflavin alone forms pale yellow crystals that are difficult to dissolve in water. It melts at 314-316¯ with decomposition, its alkaline solution shows a rotation of α20 = - 116¯. The colorless crystals of the sodium salt of 2,4-dioxybenzoic acid dissolve in water; when heated to 900 ", decomposition occurs. The obtained aqueous solutions of the lactoflavin molecular compound are intended to be used as medicaments. Example: 5.5 parts by weight of the sodium salt of 2.4 dioxyhenzoic acid are dissolved in 100 parts by weight of water and this solution is shaken with 0.5 parts by weight of lactonavin at constant temperature until it has completely dissolved. PATENT CLAIM: Process for the production of an aqueous solution of a molecular compound of lactoflavin, characterized in that the sodium salt of 2,4-dioxybenzoic acid is allowed to act on lactoflavin. The molecular compound forms dark yellow crystals which only decompose at temperatures above 350¯. It is easily soluble in water. The rotation of the l "/ o aqueous solution is ¯ 0¯.