FORMULATION FOR RETINOID-CONTAINING SOFT GELATIN CAPSULES
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 . A pharmaceutical formulation for retinoids comprising a soft gelatin capsule filled with a fill mass comprising 9-cis retinoic acid or a pharmaceutically acceptable salt thereof, a natural vegetable oil, a partially hydrogenated natural vegetable oil, a medium chain triglyceride, and a natural wax, optionally further an antioxidant, and other pharmaceutically acceptable additives.
2 . The pharmaceutical formulation according to claim 1 , wherein the antioxidant is selected from DL-α-tocopherol, butylhydroxy toluene (BHT) and butylhydroxy anisole (BHA).
3 . The pharmaceutical formulation according to 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.
4 . The pharmaceutical formulation according to claim 3 , wherein the natural vegetable oil is soybean oil.
5 . The pharmaceutical formulation according to claim 1 , wherein the partially hydrogenated 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 or cottonseed oil, or mixture of two or more of these oils.
6 . The pharmaceutical formulation according to claim 5 wherein the partially hydrogenated natural vegetable oil is soybean oil.
7 . The pharmaceutical formulation according to claim 1 , wherein the natural vegetable oil is soybean oil and the partially hydrogenated natural vegetable oil is soybean oil.
8 . The pharmaceutical formulation according to claim 1 wherein the fill mass comprises from about 50 to 80% by weight of a natural vegetable oil.
9 . The pharmaceutical formulation of claim 8 , wherein the fill mass comprises from about 60 to 70% by weight natural vegetable oil.
10 . The pharmaceutical formulation according to claim 8 , wherein the natural vegetable oil is soybean oil.
11 . The pharmaceutical formulation according to claim 1 , wherein the fill mass comprises from about 15 to 3% by weight of partially hydrogenated vegetable oil.
12 . The pharmaceutical formulation according to claim 10 , wherein the fill mass comprises from about 20 to 30% by weight of partially hydrogenated vegetable oil.
13 . The pharmaceutical formulation according to claim 10 , wherein the partially hydrogenated natural vegetable oil is soybean oil.
14 . The pharmaceutical formulation according to claim 1 , wherein the natural wax is yellow wax.
15 . The pharmaceutical formulation of claim 1 , wherein the fill mass comprises from about 3 to 6% by weight of natural wax.
16 . The pharmaceutical formulation of claim 1 , wherein the fill mass comprises from about 3 to 6% by weight of natural wax and the natural wax is yellow wax.
17 . The pharmaceutical formulation according to claim 1 , wherein the capsule has a shell comprising gelatin, one or more plasticizers and water.
18 . The pharmaceutical formulation according to claim 17 , wherein the plasticizer is selected from the group consisting of glycerol, sorbitol, propylene glycol, and mixtures of these components.
19 . The pharmaceutical formulation according to claim 18 , wherein the plasticizer comprises a mixture of glycerol and sorbitol.
20 . The pharmaceutical formulation according to claim 17 , wherein the gelatin is pig gelatin.
21 . The pharmaceutical formulation according to claim 17 , wherein the gelatin is bovine gelatin.
22 . The pharmaceutical formulation according to claim 1 wherein the triglyceride is a saturated fatty acid containing from 8 to 10 carbon atoms.
23 . The pharmaceutical formulation according to claim 22 wherein the triglyceride is a saturated fatty acid containing from 8 to 10 carbon atoms and is selected from caprylic acid, capric acid, or a mixture of caprylic acid and capric acid.
24 . The pharmaceutical formulation according to claim 1 , wherein the fill mass comprises from about 1 to 10 percent by weight of the medium chain triglyceride.
25 . The pharmaceutical formulation according to claim 22 , wherein the fill mass comprises from about 1 to 10 percent by weight of the medium chain triglyceride.
26 . The pharmaceutical formulation according to claim 25 wherein the fill mass comprises from about 6 to 12 percent by weight of the medium chain triglyceride.
27 . The pharmaceutical formulation according to claim 2 , wherein the antioxidant is selected from DL-α-tocopherol.
28 . The pharmaceutical formulation according to claim 1 , wherein the fill mass comprises from about 50 to 80 percent by weight natural vegetable oil which is soybean oil, and from about 15 to 35 percent by weight of partially hydrogenated vegetable oil which is soybean oil.
29 . The pharmaceutical formulation according to claim 28 wherein the triglyceride is a saturated fatty acid containing from 8 to 10 carbon atoms, and from about 3 to 6 percent of the natural wax which is yellow wax.
30 . The pharmaceutical formulation according to claim 29 wherein the antioxidant is selected from DL-α-tocopherol, butylhydroxy toluene (BHT) and butylhydroxy anisole (BHA).
31 . The pharmaceutical formulation according to claim 30 wherein the capsule has a shell comprising gelatin, one or more plasticizers and water.
32 . The pharmaceutical formulation according to claim 31 wherein the gelatin is selected from pig or bovine gelatin.
33 . The pharmaceutical formulation according to claim 1 wherein the dermatologically acceptable additives are selected from a colorant, flavoring agent, stabilizer, or emulsifying agent.
34 . A method of treatment of a dermatological disease in a patient in need thereof, comprising administering to said patient a pharmaceutical formulation according to claim 1 .