Pharmaceutical compositions for treating acne

Abstract

The present application relates to pharmaceutical compositions comprising retinoic acid or its derivatives such as isotretinoin and processes for preparing thereof. It also provides methods for treating acne by administering such pharmaceutical composition to a patient in need thereof.

We claim: 
     
         1 . A method of treating acne in a patient in need thereof, comprising orally administering to the patient a once daily solid oral pharmaceutical composition of isotretinoin, comprising:
 (a) an extended release (ER) portion comprising,
 (i) isotretinoin or a pharmaceutically acceptable salt thereof; 
 (ii) a solubility improving polymer; and 
 (iii) a rate controlling agent; and 
   (b) an immediate release (IR) portion comprising,
 (i) isotretinoin or a pharmaceutically acceptable salt thereof; and 
 (ii) a solubility improving polymer; 
 wherein said solubility improving polymer and isotretinoin are present in a weight ratio of at least about 2.0:1.0. 
   
     
     
         2 . The method of  claim 1 , wherein said solubility improving polymer is selected from ionizable polymer, non-ionizable polymer and mixtures thereof. 
     
     
         3 . The method of  claim 1 , wherein said solubility improving polymer comprises from about 10% w/w to about 40% w/w of the composition. 
     
     
         4 . The method of  claim 1 , wherein said composition said rate controlling agent is selected from pH independent polymer, pH dependent polymer and mixtures thereof. 
     
     
         5 . The method of  claim 1 , wherein said rate controlling agent comprises from about 5% w/w to about 20% w/w of the composition. 
     
     
         6 . The method of  claim 1 , wherein said composition further comprises wetting agents. 
     
     
         7 . The method of  claim 6 , wherein said composition comprises solubility improving polymer and wetting agent present in a weight ratio of not more than about 10.0:1.0. 
     
     
         8 . The method of  claim 1 , wherein said composition comprises solid oral dosage form selected from powder, granules, pellets, mini-tablets, tablets, capsules or caplets. 
     
     
         9 . The method of  claim 1 , wherein said once daily composition exhibits at least about 10% less food effect compared to the commercially available twice daily isotretinoin oral capsules. 
     
     
         10 . The method of  claim 1 , wherein said composition is stable for at least about 3 months when kept at 40° C./75% Relative Humidity (RH) and at 25° C./60% Relative Humidity (RH). 
     
     
         11 . A method of treating acne in a patient in need thereof, comprising orally administering to the patient a once daily solid oral pharmaceutical composition of isotretinoin, comprising: (a) an extended release (ER) portion and (b) a delayed release (DR) portion, wherein said release portions each comprise,
 (i) isotretinoin or a pharmaceutically acceptable salt thereof;   (ii) a solubility improving polymer; and   (iii) a rate controlling agent;   wherein said solubility improving polymer and isotretinoin are present in a weight ratio of at least about 2.0:1.0.   
     
     
         12 . The method of  claim 11 , wherein said solubility improving polymer is selected from ionizable polymer, non-ionizable polymer and mixtures thereof. 
     
     
         13 . The method of  claim 11 , wherein said solubility improving polymer comprises from about 10% w/w to about 40% w/w of the composition. 
     
     
         14 . The method of  claim 11 , wherein said composition said rate controlling agent is selected from pH independent polymer, pH dependent polymer and mixtures thereof. 
     
     
         15 . The method of  claim 11 , wherein said rate controlling agent comprises from about 5% w/w to about 20% w/w of the composition. 
     
     
         16 . The method of  claim 11 , wherein said composition further comprises wetting agents. 
     
     
         17 . The method of  claim 16 , wherein said composition comprises solubility improving polymer and wetting agent present in a weight ratio of not more than about 10.0:1.0. 
     
     
         18 . The method of  claim 11 , wherein said composition comprises solid oral dosage form selected from powder, granules, pellets, mini-tablets, tablets, capsules or caplets. 
     
     
         19 . The method of  claim 11 , wherein said once daily composition exhibits at least about 10% less food effect compared to the commercially available twice daily isotretinoin oral capsules. 
     
     
         20 . The method of  claim 11 , wherein said composition is stable for at least about 3 months when kept at 40° C./75% Relative Humidity (RH) and at 25° C./60% Relative Humidity (RH).