Multiparticulate L-menthol formulations and related methods
An L-menthol pharmaceutical dosage form includes an effective amount of L-menthol for treating a gastrointestinal disorder. The L-menthol is within a plurality of particulates having a core and an enteric coating over the core. The core includes an L-menthol source that is at least 80% pure L-menthol. The dosage form may be used to treat gastrointestinal disorders, such as irritable bowel syndrome.
1. An L-menthol pharmaceutical dosage form comprising an effective amount of L-menthol for treating a gastrointestinal disorder, the L-menthol being within a plurality of particulates having:
(a) a spheronized extrudate core including solid crystalline L-menthol intermixed with a pharmaceutically acceptable binder and a pharmaceutically acceptable filler; and
(b) an enteric coating over the core, the enteric coating being effective to substantially prevent release of the L-menthol from the core into a gastric pH environment and to release L-menthol from the core into an intestinal pH environment;
wherein the effective amount of L-menthol is about 10 mg to about 200 mg;
wherein the plurality of particulates are combined in a capsule or packet-type dosage form for oral delivery.
2. The L-menthol pharmaceutical dosage form of claim 1 , wherein the solid crystalline L-menthol is micronized crystalline L-menthol.
3. The L-menthol pharmaceutical dosage form of claim 1 , wherein the enteric coating includes a methacrylic acid based copolymer.
4. The L-menthol pharmaceutical dosage form of claim 1 , wherein the particulates are spheroidal and have a diameter of 0.1 mm to 3 mm.
5. The L-menthol pharmaceutical dosage form of claim 1 , wherein:
the particulates are spheroidal and have a diameter of 0.1 mm to 3 mm;
the solid crystalline L-menthol is micronized crystalline L-menthol; and
the enteric coating includes a methacrylic acid based copolymer.
6. The L-menthol pharmaceutical dosage form of claim 1 , wherein the core includes about 30% w/w to about 70% w/w L-menthol, about 25% w/w to about 60% w/w microcrystalline cellulose as the pharmaceutically acceptable filler, and about 0.5% w/w to about 4% w/w hypromellose as the pharmaceutically acceptable binder.
7. A method of treating a gastrointestinal disorder, the method comprising:
administering the L-menthol pharmaceutical dosage form of claim 1 in an effective amount for treating a gastrointestinal disorder to a subject having a gastrointestinal disorder.
8. The method of claim 7 , wherein the gastrointestinal disorder is irritable bowel syndrome.
9. The method of claim 7 , wherein the gastrointestinal disorder causes inflammation of the subject's gastrointestinal tract.
10. The method of claim 7 , wherein the solid crystalline L-menthol is micronized crystalline L-menthol.
11. The method of claim 8 , wherein the enteric coating includes a methacrylic acid based copolymer.
12. The method of claim 7 , wherein the particulates are spheroidal and have a diameter of 0.1 mm to 3 mm.
13. The method of claim 7 , wherein:
the particulates are spheroidal and have a diameter of 0.1 mm to 3 mm;
the solid crystalline L-menthol is micronized crystalline L-menthol; and
the enteric coating includes a methacrylic acid based copolymer.
14. The method of claim 7 , wherein the core includes about 30% w/w to about 70% w/w L-menthol, about 25% w/w to about 60% w/w microcrystalline cellulose, and about 0.5% w/w to about 4% w/w hypromellose.
15. The L-menthol pharmaceutical dosage form of claim 1 , wherein the spheronized extrudate core is spheroidal.
16. The L-menthol pharmaceutical dosage form of claim 1 , wherein the solid crystalline L-menthol, pharmaceutically acceptable binder, and pharmaceutically acceptable filler are within the extrudate of the spheronized extrudate core.