Homogeneous preformulations containing high concentration of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations

Abstract

A homogeneous steroid-containing preformulation for production of solid and semi-solid pharmaceutical preparations containing a uniform constant dosage of at least one steroid in a range from 0.001 to 1 percent by weight is described. This steroid-containing preformulation contains of from 0.001 to 50 percent by weight of the at least one steroid. The homogeneous steroid-containing preformulation is made by a method including dissolving the at least one steroid in a solvent to form a dispersant; dispersing an adjuvant consisting of adjuvant particles in the dispersant in a mass ratio of the adjuvant to the at least one steroid of 1:1 to 1000:1 to form a suspension; and creating a spray-mist of the suspension so as to evaporate and remove the solvent from the suspension and thus to form a dried particulate which includes steroid-containing particles. The droplets in the spray mist have a droplet diameter greater than a mean diameter of the adjuvant particles. The maximum particle size of the dried particulate forming the steroid-containing preformulation is increased by less than 30 percent in comparison to an average particle size of the adjuvant particles.

1 . Homogeneous preformulations containing high concentration of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations having a concentration content of 0.1001 to 1 weight percent of steroid, obtainable by 
 evaporation of the dispersant, containing the steroidal active ingredient, from a suspension with dispersed pharmaceutically conventional adjuvant, in which 
 a spray mist is created, whose mean droplet diameter is greater than the mean diameter of the adjuvant particles,  
 and the maximum particle size of the dried particles of the steroid containing preformulation is increased by less than 30 percent in comparison to the particle size of the adjuvant.  
   
     
     
         2 . The homogeneous preformulations containing high concentration of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations of  claim 1 , characterized in that, 
 the concentration of the steroid active ingredient amounts to 0.001 to 50 weight percent.    
     
     
         3 . Homogeneous preformulations containing steroids in high concentration, of claims  1  and  2 , characterized in that 
 the pharmaceutically conventional adjuvant is present in micronized form.  
 
     
     
         4 . Homogenous preformulations containing steroids in high concentrations of claims  1 - 3 , characterized in that 
 the steroidal active ingredient represents at least one component selected from the group comprising the sexual hormones.    
     
     
         5 . A method for producing homogeneous preformulations containing high concentration of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations having a concentration content of 0.1001 to 1 weight percent of steroids, characterized in that 
 from a suspension with dispersed pharmaceutically conventional adjuvant, the dispersant containing the steroidal active ingredient is evaporated,    a spray mist is created, whose mean droplet diameter is greater than the mean diameter of the adjuvant particles,    and the maximum particle size of the dried particles of the steroid containing preformulation is increased by less than 30 percent in comparison to the particle size of the adjuvant.    
     
     
         6 . The method for producing homogeneous preformulations containing steroids in high concentration, of  claim 5 , characterized in that the pharmaceutically conventional adjuvant is present in micronized form.