Enteric coated composition comprising prostaglandin analogs as chloride channel opener
View Patent ↗The present invention provides an enteric coated composition for oral administration of a chloride channel opener which can provide improved pharmaceutical activity with reduced adverse side effect such as nausea.
1. A composition for oral administration, comprising a bicyclic compound of
as an active ingredient thereof and an enteric coating,
wherein the bicyclic compound is present in the composition together with its monocyclic tautomer in a bicyclic:monocyclic ratio of at least 20:1.
2. The composition as described in claim 1 , wherein said composition exhibits reduced nausea inducing effect than that of a composition without the enteric coating.
3. The composition as described in claim 1 , wherein said enteric coating is selected from the group consisting of carboxymethyl ethylcellulose, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, cellulose acetate butylate, cellulose acetate trimellitate, hydroxypropyl methylcellulose acetate succinate, and a methacrylic acid copolymer.
4. The composition as described in claim 1 , wherein said composition is for preventing irritation of upper gastric organs.
5. The composition as described in claim 1 , wherein said composition is for improving pharmacological effect of the bicyclic compound to a living body.
6. The composition as described in claim 1 ; wherein the composition further comprises a solvent comprising a fatty acid or its mono, di or triglyceride.
7. A composition for oral administration, comprising a bicyclic compound of
as an active ingredient thereof and an enteric coating,
wherein the bicyclic compound is present in the composition together with its monocyclic tautomer in a bicyclic:monocyclic ratio of at least 20:1, and
wherein the composition further comprises a solvent comprising a fatty acid or its mono, di or triglyceride.
8. The composition as described in claim 7 , wherein said composition exhibits reduced nausea inducing effect than that of a composition without the enteric coating.
9. The composition as described in claim 7 , wherein said enteric coating is selected from the group consisting of carboxymethyl ethylcellulose, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, cellulose acetate butylate, cellulose acetate trimellitate, hydroxypropyl methylcellulose acetate succinate, and a methacrylic acid copolymer.
10. The composition as described in claim 7 , wherein said composition is for preventing irritation of upper gastric organs.
11. The composition as described in claim 7 , wherein said composition is for improving pharmacological effect of the bicyclic compound to a living body.