Pharmaceutical preparation and method of its production and use

Abstract

Thus, the present invention provides a composition in powder form comprising highly dispersed silica particles, polymethylsiloxane particles, and a cationic surfactant, wherein at least 25% by weight of the cationic surfactant is present in primary polymethylsiloxane particles carrying the cationic surfactant on their surface and/or in agglomerates of these primary particles.

1 . A composition in powder form comprising highly dispersed silica particles, polymethylsiloxane particles, and a cationic surfactant, wherein at least 25% by weight of the cationic surfactant is present in primary polymethylsiloxane particles carrying the cationic surfactant on their surface and/or in agglomerates of these primary particles. 
     
     
         2 . The composition according to  claim 1 , wherein at least 25% by weight of the cationic surfactant is present in primary polymethylsiloxane particles having the cationic surfactant mechanochemically immobilized onto their surface and/or in agglomerates of these primary particles. 
     
     
         3 . (canceled) 
     
     
         4 . A method of producing a composition in powder form comprising the following steps (a) to (c):
 (a) providing highly dispersed silica particles, polymethylsiloxane particles, and one or both of a cationic surfactant, and an antimicrobial substance;   (b) carrying out the following steps (b):
 (b 1) forming primary polymethylsiloxane particles carrying the cationic surfactant on their surface and/or agglomerates of these primary particles; and 
   (c) mixing the major part of the highly dispersed silica particles with the products obtained in step (b).   
     
     
         5 . The composition according to  claim 1 , wherein the composition comprises
 21.0 to 75.0 wt. % of the highly dispersed silica,   16.0 to 70.0 wt. % of the polymethylsiloxane, and   a cationic surfactant in an amount of 0.2 to 4.0 wt,   based on the total weight of the composition.   
     
     
         6 . The composition according to  claim 1 , wherein the composition further comprises at least one of the following agents:
 0.01 to 10.0 wt. % of at least one substance with tissue growth activity,   0.01 to 5.0 wt. % lidocaine,   0.01 to 5.0 wt. % of at least one phenothiazine derivative, and   0.01 to 3.0 wt. % of at least one proteolytic enzyme,   based on the total weight of the composition.   
     
     
         7 . The method according to  claim 4 , wherein the formation of the primary particles or their agglomerates in step (b 1) is achieved by milling the respective components. 
     
     
         8 . The method according to  claim 4 , wherein
 in step (b 1) the cationic surfactant is mechanochemically immobilized onto the polymethylsiloxane particles.   
     
     
         9 . (canceled) 
     
     
         10 . The composition according to  claim 1 , wherein the sum of the highly dispersed silica and the polymethylsiloxane represents 65 to 97 wt. %, preferably 80 to 95 wt. % of the total weight of the composition. 
     
     
         11 . A composition in powder form obtained by the method according to  claim 4 . 
     
     
         12 . A pharmaceutical preparation which is or comprises the composition of  claim 1 . 
     
     
         13 . An aqueous composition which comprises the composition according to  claim 1  in an amount of at least 2% by weight based on the total weight of the preparation. 
     
     
         14 . A medical article selected from the group consisting of a dressing, packets, or capsules, comprising the pharmaceutical preparation according to  claim 12 . 
     
     
         15 . The composition according to  claim 1  for use in the treatment of purulent wounds and necrotic wounds. 
     
     
         16 . The composition according to  claim 1  for use in the treatment of infected burn surfaces, putrid necrotizing phlegmons and noma in the maxillofacial region, wounds during a larynx or laryngopharynx resection after a cancer surgery, inflammatory diseases of the throat, mouth cavity and/or teeth, pharyngitis, tonsillitis, gingivitis and stomatitis, periodontitis, dental application and ultraphoresis, diseases of the rectum, the large intestine and organs of abdominal cavity, peritonitis, intra-abdominal and pancreatogenic abscesses, complications after pancreatonecrosis, extraperitoneal phlegmons, inflammatory diseases of the uterus and uterine adnexa, urinary bladder, pleura, bones, and other visceral organs, osteomyelitis, urethritis caused by gonococci, trichomonases and other infections, diseases in the front part of the eyes, a fistular in traumatic surgery, food intoxication, acute intestinal obstruction and intoxications by a virus, wounds and impetiginous diseases of the skin, acne, folliculitis and sycosis in the face and/or diseases provoked by irrational application of cosmetics, hemorrhoids, proctitis, anorectal abscesses, anal fissures, wounds after gynecological surgeries, non-specific trichomonal and fungal colpitis, vaginitis, vulvitis, metritis, parametritis, salpingitis, infectious diarrhea, infections caused by staphylococcus aureus, methicillin-resistant staphylococcus aureus (MRSA), multi-resistant gram-negative bacteria, enterobacteriaceae, and non-fermenting bacteria. 
     
     
         17 . The aqueous solution of  claim 13  for use in the treatment of chronic inflammations of the urinary tract or the bladder. 
     
     
         18 . (canceled) 
     
     
         19 . A composition in powder form comprising highly dispersed silica particles and an antimicrobial substance, wherein at least 25% by weight, preferably 25 to 80% by weight, more preferably 40 to 80% by weight, most preferably 40 to 60% by weight of the antimicrobial substance is present in primary highly dispersed silica particles carrying the antimicrobial substance on their surface or in agglomerates of these primary particles. 
     
     
         20 . The composition in powder form according to  claim 19  comprising highly dispersed silica particles and an antimicrobial substance, wherein at least 25% by weight, preferably 25 to 80% by weight, more preferably 40 to 80% by weight, most preferably 40 to 60% by weight of the antimicrobial substance is present in primary highly dispersed silica particles having the antimicrobial substance mechanochemically immobilized onto the surface of a part of the highly dispersed silica and/or in agglomerates of these primary particles. 
     
     
         21 . The composition according to  claim 20 , wherein the part of the highly dispersed silica onto which the antimicrobial substance is mechanochemically immobilized is 5 to 30 wt. %, preferably 10 to 20 wt. %, more preferably 11 to 15 wt. % of the total weight of the highly dispersed silica comprised in the composition. 
     
     
         22 .- 25 . (canceled) 
     
     
         26 . A method of producing a composition in powder form comprising the following steps:
 (a) providing highly dispersed silica particles and an antimicrobial substance;   (b2) forming primary highly dispersed silica particles carrying the antimicrobial substance on their surface and/or in agglomerates of these primary particles using a minor part of the highly dispersed silica particles; and   (c) mixing the major part of the highly dispersed silica particles with the products obtained in step (b2).   
     
     
         27 . The method according to  claim 26 , wherein at least 25% by weight, preferably 25 to 80% by weight, more preferably 40 to 80% by weight, most preferably 40 to 60% by weight of the antimicrobial substance is present in primary highly dispersed silica particles carrying the antimicrobial substance on their surface or in agglomerates of these primary particles. 
     
     
         28 . The method according to  claim 26 , wherein the major part of the highly dispersed silica particles employed in step (c) represents 70 to 95 wt. %, preferably 80 to 90 wt. %, more preferably 85 to 89 wt. % of the total weight of the highly dispersed silica comprised in the composition. 
     
     
         29 . The composition according to  claim 19 , wherein the composition comprises:
 80.0 to 99.5 wt. % of the highly dispersed silica, and   0.5 to 20 wt. % of the antimicrobial substance,   based on the total weight of the composition.   
     
     
         30 . A composition in powder form obtained by the method according to  claim 26 . 
     
     
         31 . A kit comprising separately:
 (a) the composition according to  claim 19  and highly dispersed silica particles;   (b) the composition according to  claim 19  and polymethylsiloxane particles; or   (c) the composition according to  claim 19 .   
     
     
         32 . A method for preparing polymethylsiloxane comprising the steps of:
 (i) performing hydrolysis of methyltrichlorosilane to obtain a hydrogel of methylsilicic acid;   (ii) drying the obtained hydrogel of methylsilicic acid whereby a coarsely dispersed product in the form of granules and pieces is obtained; and   (iii) milling the coarsely dispersed product.   
     
     
         33 . Polymethylsiloxane obtained by the method according to  claim 32 .