Use of modified lysozyme c to prepare medicinal compositions for the treatment of some serious diseases

Abstract

Use of modified lysozyme c or its pharmaceutically acceptable salts and its industrial production for the preparation of medicinal compositions, suitable for oral, parenteral and topical administration, for prophylaxis and therapy of some serious diseases in mammalians.

1 . A pegylated lysozyme c having the, formula: 
       [CH 3 O—(CH 2 —CH 2 —O) n —CH 2 —CH 2 ] x —(NH) y Lysozyme c. (Z)m wherein:    (NH) y Lysozyme c is human lysozyme c;    y is the number of free amino groups of lysine units present in a molecule of human lysozyme c, and varies from 5 to 30;    x is between 1 and y;    n is between 5 and 1000;    Z is a pharmaceutically acceptable acid; and    m is between 1 and y.    
   
   
       2 . A pegylated lysozyme c according to  claim 1 , wherein n is between 120 and 200.  
   
   
       3 . A pegylated lysozyme c according to  claim 1 , wherein said pharmaceutically acceptable acid is hydrochloric acid.  
   
   
       4 . A pegylated lysozyme c according to  claim 1 , wherein natural lysozyme c is modified with monomethoxypolyethylene glycol.  
   
   
       5 . A method for producing a pegylated lysozyme c as claimed in  claim 1 , which method consists of: 
 a. reacting monomethoxypolyethylene glycol with tresylated chloride; and    b. reacting the resulting compound with human lysozyme c in a phosphate buffer saline or in a borate buffer in a slightly basic medium.    
   
   
       6 . A method according to  claim 5 , further comprising a final production of a physiologically acceptable salt complex resulting from a dialysis process of an aqueous solution of Z acid, admixed for 6-8 hours, at room temperature, with the corresponding pegylated lysozyme c.  
   
   
       7 . A regime or regimen for inducing increased levels of free TNF-α (Tumor Necrosis Factor-alpha) in plasma, comprising orally administering to a mammalian organism in need of such treatment, a thus effective amount of a pegylated lysozyme c or its salts having the formula: 
       [CH 3 O—(CH 2 —CH 2 —O) n —CH 2 —CH 2 ] x —(NH) y Lysozyme c. (Z)m wherein:    (NH) y Lysozyme c is human lysozyme c;    y is the number of free amino groups of lysine units present in the molecule of human lysozyme c, and varies from 5 to 30;    x is between 1 and y;    n is between 5 and 1000;    Z is a pharmaceutically acceptable acid; and    m is between 1 and y.    
   
   
       8 . A regime or regimen according to  claim 7 , wherein said pegylated lysozyme c is mixed with a pharmaceutically acceptable inert carrier to form a pharmaceutical composition suitable for oral administration.  
   
   
       9 . A regime or regimen according to  claim 8 , wherein said pharmaceutically acceptable inert carrier is a solid, a liquid, or a mixture thereof.  
   
   
       10 . A regime or regimen according to  claim 8 , wherein said pharmaceutical composition is of a form selected from the group consisting of tablets (with prompt or sustained release), capsules, granules, powder, syrup, a suspension, an emulsion, and drops.  
   
   
       11 . A regime or regimen according to  claim 8 , wherein from about 5% to about 80% by weight of said pegylated lysozyme c is present in said pharmaceutical composition.  
   
   
       12 . A regime or regimen according to  claim 8 , wherein from about 40% to about 60% by weight of said pegylated lysozyme c is present in said pharmaceutical composition.  
   
   
       13 . A regime or regimen according to  claim 8 , wherein said pharmaceutical composition further includes an adjuvant.  
   
   
       14 . A regime or regimen according to  claim 7 , wherein the replication speed of the tumoral proliferative process is inhibited.  
   
   
       15 . A regime or regimen according to  claim 7 , wherein said pegylated lysozyme c is in the form of a pharmacologically acceptable salt.  
   
   
       16 . A regime or regimen according to  claim 7 , wherein a daily dosage of between about 150 mg and about 6 g of said pegylated lysozyme c or its salts is administered.  
   
   
       17 . A regime or regimen according to  claim 7 , wherein a daily dosage of between about 500 mg and about 2.5 g of said pegylated lysozyme c or its salts is administered.