Lipophilic active oral film formulation and method of making the same

Abstract

Disclosed is a description and methods for formulating oral films containing lipophilic active ingredient(s), more particularly lipophilic active having a positive logP. The method involves dispersing the lipophilic active(s) in a carrier oil and uniformly distributing them as emulsified oil droplets into a polymer matrix. The methods reported here produce oral films containing a stable emulsion with up to 40% oil phase. The oil phase consists of the carrier oil and lipophilic active(s). This offers the possibility to enhance the amount of lipophilic actives to be included in the film formulation while preserving the film characteristics. The resulting oral films offer a standardized dosage form for lipophilic actives as well as easier and more convenient administration, transportation, handling, and storage.

1 - 20 . (canceled) 
     
     
         21 . An oral film dosage form for human or animal administration comprising:
 a film layer formed with an oil-in-water emulsion comprising;
 a safe and effective amount of a lipophilic active selected from cannabinoids; 
 a carrier oil selected from selected from medium-chain triglyceride (MCT) oil,  cannabis  oil, castor oil, and mixtures thereof; 
 a water soluble film forming polymer selected from selected from cellulose derivatives, polyvinyl alcohol, polyvinyl pyrrolidone, polyethylene oxide, starches, polyacrylates, gums and mixtures thereof, and 
 from about 2% to about 10% (wt/wt) of a combination of surfactants including a small-molecule surfactant selected from polysorbate and sorbitan, and a phospholipid; 
 wherein the combined quantity of carrier oil and lipophilic pharmaceutical active is from about 25% to about 40% (wt/wt) of the oral film dosage form; and wherein the contact angle of the film is from about 39 degrees to about 90 degrees. 
   
     
     
         22 . The oral film dosage form of  claim 21 , wherein the film layer has a surface pH from about 4 to less than 5.5. 
     
     
         23 . The oral film dosage form of  claim 21 , wherein the combined quantity of carrier oil and lipophilic active is about 30% (wt/wt) of the oral film dosage form. 
     
     
         24 . The oral film dosage form of  claim 21 , wherein the combined quantity of carrier oil and lipophilic active is about 35% (wt/wt) of the oral film dosage form. 
     
     
         25 . The oral film dosage form of  claim 21 , wherein the film layer further comprises a viscosity modifier. 
     
     
         26 . The oral film dosage form of  claim 21 , wherein the film layer retains at least 95% of the oil and lipophilic active. 
     
     
         27 . The oral film dosage form of  claim 21 , wherein the contact angle of the film is from about 39 degrees to about 80 degrees. 
     
     
         28 . The oral film dosage form of  claim 21 , wherein the contact angle of the film is from about 39 degrees to about 70 degrees. 
     
     
         29 . The oral film dosage form of  claim 21 , wherein the contact angle of the film is from about 39 degrees to about 60 degrees. 
     
     
         30 . The oral film dosage form of  claim 21 , wherein the lipophilic active is THC, CBD or mixtures thereof. 
     
     
         31 . The oral film dosage form of  claim 21 , further comprising pectin in the film layer comprising the lipophilic active or in a one or more protective layers joined to the film layer comprising the lipophilic active, the pectin being present in an amount effective to provide targeted enteric delivery of the lipophilic active to the colon or large intestine upon administration. 
     
     
         32 . The oral film dosage form of  claim 21 , wherein the lipophilic active is THC, CBD or mixtures thereof. 
     
     
         33 . The oral film dosage form of  claim 21 , wherein the wherein the combined quantity of carrier oil and lipophilic pharmaceutical active is from about 25% to about 40% (wt/wt) of the oral film dosage form. 
     
     
         34 . The oral film dosage form of  claim 21 , wherein the contact angle of the film is from about 39 degrees to about 90 degrees. 
     
     
         35 . An oral film dosage form comprising:
 a film layer formed with an oil-in-water emulsion including:   a safe and effective amount of a lipophilic active agent selected from selected from cannabinoids;   a carrier oil selected from selected from selected from medium-chain triglyceride (MCT) oil,  cannabis  oil, castor oil and mixtures thereof; and   a water soluble film forming polymer selected from selected from cellulose derivatives, polyvinyl alcohol, polyvinyl pyrrolidone, polyethylene oxide, starches, polyacrylates, gums and mixtures thereof;   wherein the carrier oil content is greater than the lipophilic active agent content;   wherein the film layer has a surface pH from about 4 to less than 5.5,   
       and wherein a disintegration time of the oral film dosage form upon administration is from about 1 minute to about 20 minutes. 
     
     
         36 . The oral film dosage form of  claim 35 , wherein the combination of surfactants being present in an amount no more than 10% of the combined weight of the carrier oil and the lipophilic active. 
     
     
         37 . The oral film dosage form of  claim 35 , wherein the contact angle of the film is from about 39 degrees to about 52 degrees. 
     
     
         38 . The oral film dosage form of  claim 35 , wherein the lipophilic active is THC, CBD or mixtures thereof. 
     
     
         39 . The oral film dosage form of  claim 35 , wherein the wherein the combined quantity of carrier oil and lipophilic pharmaceutical active is from about 25% to about 40% (wt/wt) of the oral film dosage form. 
     
     
         40 . The oral film dosage form of  claim 35 , wherein the contact angle of the film is from about 39 degrees to about 90 degrees.