New formulation for retinoid-containing soft gelatin capsules

Abstract

A new pharmaceutical formulation for retinoid-containing soft gelatin capsules is disclosed. The new formulation comprises a soft gelatin capsule filled with a fill mass comprising a retinoid as an active ingredient, a natural vegetable oil, a partially hydrogenated natural vegetable oil and medium chain triglycerides. Optionally, the new formulation also comprises a natural wax. In a particularly preferred embodiment, the soft gelatin capsule comprises pig gelatin in the capsule shell in combination with the above fill mass.

1 . Pharmaceutical formulation for retinoids comprising a soft gelatin capsule filled with a fill mass comprising a retinoid as an active ingredient, a natural vegetable oil, a partially hydrogenated natural vegetable oil and medium chain triglycerides.  
     
     
         2 . (Originally Presented) Pharmaceutical formulation according to  claim 1 , wherein the fill mass in addition comprises a natural wax.  
     
     
         3 . The pharmaceutial formulation of  claim 1 , wherein the fill mass in addition comprises an antioxidant.  
     
     
         4 . The pharmaceutial formulation of  claim 1 , wherein the natural vegetable oil is selected from soybean oil, corn oil, sunflower oil, rape seed oil, linseed oil, sesame oil, olive oil, coconut oil, peanut oil, safflower oil, castor oil and cottonseed oil or mixtures of two or more of these oils.  
     
     
         5 . The pharmaceutial formulation of claims  1 , wherein the natural vegetable oil is soybean oil.  
     
     
         6 . The pharmaceutial formulation of  claim 1 , wherein the medium chain triglycerides are selected from triglycerides of saturated fatty acids containing 8 to 10 carbon atoms.  
     
     
         7 . The pharmaceutial formulation of  claim 2  wherein the natural wax is yellow wax.  
     
     
         8 . The pharmaceutial formulation of  claim 3  wherein the antioxidant is selected from DL-α-tocopherol, butylhydroxy toluene (BHT) and butylhydroxy anisole (BHA).  
     
     
         9 . The pharmaceutial formulation of  claim 1 , wherein the capsule shell comprises gelatin, one or more plasticizers and water.  
     
     
         10 . The pharmaceutial formulation of  claim 9 , wherein the plasticizer is selected from the group consisting of glycerol, sorbitol, propylene glycol, and mixtures of these components.  
     
     
         11 . The pharmaceutial formulation of  claim 10 , wherein the plasticizer comprises a mixture of glycerol and sorbitol.  
     
     
         12 . The pharmaceutial formulation of  claim 9 , wherein the gelatin is pig gelatin, in particular derived from pig skin.  
     
     
         13 . The pharmaceutial formulation of claims  1  wherein the retinoid is selected from the group consisting of retinol, retinal, retinoic acid and derivatives thereof.  
     
     
         14 . The pharmaceutial formulation of  claim 13 , wherein the retinoid is 9-cis retinoic acid.  
     
     
         15 . The pharmaceutial formulation of  claim 1 , wherein the fill mass comprises about 50 to 80 percent by weight of the natural vegetable oil, about 15 to 35 percent by weight, of the hydrogenated natural vegetable oil, and about 3 to 20 percent by weight, of the medium chain triglycerides.  
     
     
         16 . The pharmaceutial formulation of  claim 2 , wherein the fill mass comprises about 1 to 10 percent by weight, of the natural wax.  
     
     
         17 . The pharmaceutial formulation of  claim 15 , wherein the natural vegetable oil is soybean oil.  
     
     
         18 . The pharmaceutial formulation of  claim 16 , wherein the natural wax is yellow wax.  
     
     
         19 . The pharmaceutical formulation of  claim 6 , wherein said saturated fatty acid is caprylic or capric acid.  
     
     
         20 . The pharmaceutical formulation of  claim 12 , wherein said pig gelatin is derived from pig skin.  
     
     
         21 . The pharmaceutical formulation of  claim 15 , wherein said fill mass comprises from about 60 to 70 percent by weight of the natural vegetable oil and from about 20 to 30 percent by weight of the hydrogenated vegetable oil and from about 6 percent by weight to 12 percent by weight of the medium chain triglycerides.  
     
     
         22 . The pharmaceutical formulation of  claim 21 , wherein said fill mass comprises 62 to 64 percent of weight of natural vegetable oil, 24 to 25 percent by weight of hydrogenated natural vegetable oil and from about 8 to 9 percent by weight of medium chain triglycerides.  
     
     
         23 . The pharmaceutical formulation of  claim 16 , wherein the fill mass comprises of about 3 to 6 percent weight of natural wax.  
     
     
         24 . The pharmaceutical formulation of  claim 23 , wherein the fill mass comprises from about 4 percent by weight of the natural wax.