All-natural enteric soft capsules comprising active ingredients

Abstract

Described herein are soft capsules and enteric soft capsules comprising cationic Type A gelatin and acid insoluble enteric polymers. In particular, the compositions and methods for manufacturing all-natural enteric soft capsules comprising Type A gelatin and matrix fills are described. In one embodiment, the enteric soft capsules comprise active ingredients such as non-steroidal anti-inflammatory drugs (NSAIDs). In another embodiment, the enteric soft capsule comprises matrix fills of omega-3 fatty acids.

1 . An all-natural oral enteric soft capsule shell formed from a gel mass composition comprising:
 (a) a gelatin composition;   (b) at least one anionic polymer;   (c) at least one plasticizer; and   (d) water.   
     
     
         2 . The composition of  claim 1 , wherein the gelatin composition comprises about 20% to about 40% of the total gel mass. 
     
     
         3 . The composition of  claim 1 , wherein the gelatin composition comprises Type A gelatin. 
     
     
         4 . The composition of  claim 3 , wherein the Type A gelatin comprises acid bone, pig skin, poultry, fish, gelatin hydrolysate, or acid hide. 
     
     
         5 . The composition of  claim 4 , wherein the Type A gelatin has a Bloom strength of about 150 grams to about 350 grams. 
     
     
         6 . The composition of  claim 4 , wherein the Type A gelatin comprises pig skin gelatin. 
     
     
         7 . The composition of  claim 4 , wherein the Type A gelatin comprises about 22% to about 37% of the total gel mass. 
     
     
         8 . The composition of  claim 1 , wherein the anionic polymer comprises about 2% to about 7% of the total gel mass. 
     
     
         9 - 14 . (canceled) 
     
     
         15 . The composition of  claim 1 , wherein the total weight percentage of plasticizer comprises about 8% to about 30% of the total gel mass. 
     
     
         16 - 41 . (canceled) 
     
     
         42 . A soft capsule pharmaceutical composition comprising a matrix fill comprising:
 (a) at least one solubility enhancing agent;   (b) at least one plasticizer;   (c) water; and   (d) at least one active pharmaceutical ingredient.   
     
     
         43 . The composition of  claim 42 , wherein the one or more solubility enhancing agents comprises about 10% to about 85% of the matrix fill mass. 
     
     
         44 . The composition of  claim 42 , wherein the one or more solubilizing plasticizers comprises about 2.5% to about 10% of the matrix fill mass. 
     
     
         45 . The composition of  claim 42 , wherein water comprises about 2.5% to about 20% of the matrix fill mass. 
     
     
         46 . The composition of  claim 42 , wherein the one or more active pharmaceutical ingredients comprises about 5% to about 80% of the matrix fill mass. 
     
     
         47 . The composition of  claim 42 , wherein:
 (a) the one or more solubility enhancing agents comprises polyethylene glycol having a molecular weight of about 200 to about 800;   (b) the one or more solubilizing plasticizers comprises glycerol or propylene glycol;   (c) the one or more active pharmaceutical ingredients comprises a non-steroidal anti-inflammatory drug.   
     
     
         48 . The composition of  claim 42 , wherein:
 (a) the one or more solubility enhancing agent comprises polyethylene glycol have a molecular weight of about 600 comprising about 80% of the matrix fill mass;   (b) the one or more solubilizing plasticizer comprises glycerol comprising about 5% of the matrix fill mass or propylene glycol comprising about 5% of the matrix fill mass;   (c) water comprises about 5% of the matrix fill mass; and   (d) the one or more active pharmaceutical ingredient comprises diclofenac potassium comprising about 11% of the matrix fill mass.   
     
     
         49 - 59 . (canceled) 
     
     
         60 . The composition of  claim 47 , wherein the non-steroidal anti-inflammatory drug comprises diclofenac in its salt or free acid form comprising diclofenac potassium, diclofenac sodium, diclofenac hydrochloride, or diclofenac free acid. 
     
     
         61 . The composition of  claim 60 , wherein diclofenac comprises a weight of about 25 mg to about 150 mg. 
     
     
         62 - 63 . (canceled) 
     
     
         64 . An oral pharmaceutical composition comprising an enteric soft capsule shell comprising:
 (a) pig skin Type A gelatin comprising about 33.2% of the shell mass or acid bone Type A gelatin comprising about 36% of the shell mass;   (b) pectin comprising about 3.3° A of the total gel mass or EUDRAGIT® L 100 comprising about 11% of the shell mass;   (c) a plasticizer comprising glycerol comprising about 16% or about 18% of the shell mass;   (d) an optional alkali neutralizing agent comprising about 1.7% of the shell mass; and   (e) a solvent comprising about 47% or about 44% of the shell mass; and   
       wherein, the oral pharmaceutical composition further comprises a matrix fill comprising:
 (a) polyethylene glycol 600 comprising about 80% of the matrix fill mass; 
 (b) propylene glycol comprising about 5% of the matrix fill mass; 
 (c) water comprising about 5% of the matrix fill mass; and 
 (d) diclofenac potassium comprising about 11% of the matrix fill mass; 
 
       or
 (e) lecithin comprising about 1.5% of the matrix fill mass; 
 (f) vegetable oil comprising about 12.5% of the matrix fill mass and soybean oil comprising about 53% of the matrix fill mass; 
 (g) bee's wax comprising about 3% of the matrix fill mass; 
 (h) chitosan comprising about 5% of the matrix fill mass; 
 (i) Carbopol® 971 comprising about 5% of the matrix fill mass; and 
 (j) diclofenac potassium comprising about 20% of the matrix fill mass. 
 
     
     
         65 . (canceled) 
     
     
         66 . The composition of  claim 64 , wherein the fatty acid comprises omega-3 fatty acids, polyunsaturated omega-3 fatty acids, hexadecatrienoic acid (HTA), alpha-linolenic acid (ALA), stearidonic acid (SDA), eicosatrienoic acid (ETE), eicosatetraenoic acid (ETA), eicosapentaenoic acid (EPA, timnodonic acid), heneicosapentaenoic acid (HPA), docosapentaenoic acid (DPA), clupanodonic acid), docosahexaenoic acid (DHA, cervonic acid), tetracosapentaenoic acid, tetracosahexaenoic acid (nisinic acid), arachidonic acid and free acids, etheyl esters, or other esters or salts and combinations thereof. 
     
     
         67 - 72 . (canceled)