Enteric bisacodyl softgel capsule
Softgel capsules comprise a fill material and a shell composition, wherein the fill composition includes bisacodyl and the shell composition includes a film forming material and an enteric polymer. The softgel capsules further include 5 parts by weight of bisacodyl based on 100 parts by weight of the fill material. A method for producing the softgel capsule using a gel conversion is also provided.
1 . A softgel capsule comprising: (a) a fill material comprising bisacodyl or a pharmaceutically acceptable salt, a lipid comprising soybean oil, and a suspending agent comprising hydrogenated vegetable oil; and (b) a shell composition comprising a film forming material, a plasticizer comprising sorbitol and sorbitan, and an enteric polymer comprising pectin;
wherein the fill material comprises about 5 parts by weight to about 10 parts by weight of bisacodyl based on 100 parts by weight of the fill material;
wherein the fill material comprises from about 90 wt % to about 95 wt % of lipid based on a total composition of the fill material;
wherein the softgel capsule remains intact for at least about 15 minutes when a disintegration test is performed in a USP Apparatus II with paddles at a speed of 50 rpm in pH 1.2 medium; and
wherein the softgel capsule has an assay stability of at least about 90% when tested at 40° C./75% RH at 1 month.
2 . The softgel capsule of claim 1 , wherein the film forming material comprises an animal derived polymer or a non-animal derived polymer.
3 . The softgel capsule of claim 2 , wherein the animal derived polymer comprises gelatin.
4 . The softgel capsule of claim 2 , wherein non-animal derived polymer comprises gellan gum.
5 . The softgel capsule of claim 1 , wherein the shell composition further comprises dextrose.
6 . The softgel capsule of claim 1 , wherein the enteric polymer is methyl acrylic acid copolymer.
7 . The softgel capsule of claim 3 , wherein the shell composition comprises about 30 wt % to about 80 wt % of a gelatin.
8 . The softgel capsule of claim 1 , wherein the shell composition comprises about 2 wt % to about 20 wt % of pectin.
9 . The softgel capsule of claim 6 , wherein the shell composition comprises about 2 wt % to about 16 wt % of methyl acrylic acid copolymer.
10 . The softgel capsule of claim 5 , wherein the shell composition comprises about 0.01 wt % to about 4 wt % of dextrose.
11 . The softgel capsule of claim 3 , wherein the gelatin comprises Type A gelatin, Type B gelatin and mixtures thereof.
12 . The softgel capsule of claim 1 , wherein the shell composition further comprises water.
13 . The softgel capsule of claim 1 , wherein the fill material further comprises an antioxidant.
14 . The softgel capsule of claim 13 , wherein the fill material further comprises butylated hydroxytoluene (BHT).
15 . The softgel capsule of claims 13 , wherein the fill material further comprises butylated hydroxyanisole (BHA).
16 . The softgel capsule of claim 13 , wherein the fill material comprises about 0.001 parts by weight to about 2 parts by weight of antioxidant based on 100 parts by weight of the fill material.
17 . The softgel capsule of claim 14 , wherein the fill material comprises about 0.001 parts by weight to about 0.5 parts by weight of BHT based on 100 parts by weight of the fill material.
18 . The softgel capsule of claim 15 , wherein the fill material comprises about 0.1 parts by weight to about 2 parts by weight of BHA based on a 100 parts by weight of the fill material.
19 . The softgel capsule of claim 1 , wherein the softgel capsule has an assay stability of at least about 90% when tested at 25° C./60% RH at 1 month.
20 . The softgel capsule of claim 1 , wherein the softgel capsule has an assay stability of at least about 90% when tested at 30° C./65% RH at 1 month.
21 . The softgel capsule of claim 1 , wherein the softgel capsule remains intact for at least about 15 minutes in pH 1.2 medium and disintegrate in pH 6.8 buffer in about 60 minutes or less.
22 . The softgel capsule of claim 1 , wherein the total impurity does not exceed about 0.5%, wherein the total impurity is measured per current USP Monograph test method.