Shaped body and method for production of said body

Abstract

Water-dispersible or water-soluble polymers, particularly those of the family of compounds comprising the poloxamers or the polyesters or amphiphilic agents (emulsifiers), and also lipophilic materials are dispersed by melting the components at suitable temperatures with admixture of pharmaceutically active substances by mechanical procedures, i.e. a lipophilic dispers phase is distributed in a hydrophilic continuous polymer phase to form a stable dispersion. By controlled cooling, curing, and storage followed by high-pressure molding at defined temperatures and operating pressures there are produced, in addition to other types of shaped bodies, dispersed polymeric fatty sticks distinguished by particularly good fracture strength, flexibility, and variable time-specific dimensional stability.

1 . Shaped body for medical administration in body cavities and/or wound cavities in humans or animals, comprising at least one amphiphilic continuous phase, for example, a water-dispersible polymer, and at least one lipophilic component as disperse phase, and also comprising at least one pharmaceutically effective water-soluble or fat-soluble material, the continuous phase being a biologically neutral oligomer of a polyether, for example, a copolymer, wherein
 a) the continuous phase is a poloxamer, for example, poloxamer 124, poloxamer 188, poloxamer 237, poloxamer 338, or poloxamer 407,   b) the proportion of continuous phase is at least 40 wt % and the proportion of disperse phase is up to 50 wt %,   c) the continuous phase, the disperse phase and the pharmaceutically effective material being shaped as a dispersed solid composition following defined maturing or storage at constant temperature with liquefaction under compression   d) the shaped body having a diameter of down to 2 mm and a length of up to 100 mm.   
   
   
       2 . Shaped body as defined in  claim 1 , wherein the lipophilic component is a wax, particularly an ester of a long-chain fatty acid with a long-chain fatty alcohol, for example, officinal beeswax EuAB 98 or bleached beeswax EuAB 98, or that the lipophilic component is a fatty alcohol or a mixture of fatty alcohols, for example, stearyl alcohol or cetyl/stearyl alcohol. 
   
   
       3 . Shaped body as defined in  claim 1 , wherein the lipophilic component is a triglyceride mixture, for example, higher-melting suppository compositions having a melting point above 40° C. 
   
   
       4 . Shaped body as defined in  claim 1 , wherein the lipophilic component is a long-chain hydrocarbon mixture, for example, higher-melting paraffin compositions having a melting point above 40° C. 
   
   
       5 . Shaped body as defined in  claim 1 , wherein the proportion of active substance or combination of active substances does not exceed 10 wt %. 
   
   
       6 . Shaped body as defined in  claim 1 , wherein the active substance present is an antibiotic agent, e.g., benzyl penicillin procaine or gentamycin, an antiseptic agent, an antimycotic agent, and/or a virustatic agent, e.g., Aciclovir®. 
   
   
       7 . Shaped body as defined in  claim 1 , wherein the active substance present is a glucocorticoid, e.g., a hydrocortisol, an ester thereof, a betamethason, an ester thereof or a triamcinolone acctonide. 
   
   
       8 . Shaped body as defined in  claim 1 , wherein the active substance present is PVP iodine. 
   
   
       9 . Shaped body as defined in  claim 1 , wherein the active substance present is metronidazol. 
   
   
       10 . Shaped body as defined in  claim 1 , wherein the shaped body is a cylindrical or a conical or barrel-shaped stick. 
   
   
       11 - 15 . (canceled) 
   
   
       16 . Pharmaceutical preparation, characterized by a dispersed solid fat-in-polymer dispersion or fat-in-detergent dispersion as defined in at least  claim 1 . 
   
   
       17 . (canceled) 
   
   
       18 . The shaped body of  claim 1 , wherein the at least one amphiphilic continuous phase is a water-dispersible polymer. 
   
   
       19 . The shaped body of  claim 1 , wherein the poloxamer is poloxamer 124, poloxamer 188, poloxamer 237, poloxamer 338, or poloxamer 407. 
   
   
       20 . The shaped body of  claim 2 , wherein the wax is an ester of a long-chain fatty acid with a long-chain fatty alcohol or the lipophilic component is a fatty alcohol or a mixture of fatty alcohols. 
   
   
       21 . The shaped body of  claim 20 , wherein the ester of a long-chain fatty acid with a long-chain fatty alcohol is officinal beeswax EUAB 98 or bleached beeswax EUAB 98. 
   
   
       22 . The shaped body of  claim 20 , wherein the fatty alcohol is stearyl alcohol or cetyl/stearyl alcohol 
   
   
       23 . The shaped body of  claim 3 , wherein the triglyceride mixture is a suppository composition having a melting point above 40° C. 
   
   
       24 . The shaped body of  claim 4 , wherein the long-chain hydrocarbon mixture is a higher-melting paraffin compositions having a melting point above 40° C. ° C. 
   
   
       25 . The shaped body as defined in  claim 1 , wherein the proportion of the lipophilic component is between 25 and 50 wt %, and the proportion of the continuous phase is from 40 to 70 wt %. 
   
   
       26 . The shaped body of  claim 25 , wherein the proportion of the lipophilic component is between 40 and 50 wt %, and the proportion of the continuous phase is from 48 to 52 wt %. 
   
   
       27 . The shaped body of  claim 25 , wherein the proportion of the lipophilic component is between 25 and 50 wt %, and the proportion of the continuous phase is from 48 to 52 wt %. 
   
   
       28 . The shaped body as defined in  claim 1 , wherein the shaped body has the shape of a suppository or torpedo, or is in the form of a tablet. 
   
   
       29 . The shaped body of  claim 6 , wherein the antibiotic agent is a benzyl penicillin procaine or gentamycin. 
   
   
       30 . The shaped body of  claim 7 , wherein the virustatic agent is Aciclovir®. 
   
   
       31 . The shaped body of  claim 7 , wherein the active substance is a hydrocortisol.