Enterically coated cysteamine, cystamine and derivatives thereof
View Patent ↗The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.
1. A method of administering cystamine, or pharmaceutically acceptable salts thereof, to a patient in need thereof comprising administering to said patient a pharmaceutical composition comprising cystamine, or pharmaceutically acceptable salts thereof, wherein the composition increases delivery of cystamine, or pharmaceutically acceptable salts thereof, to the small intestine and wherein the frequency of administering is less than four times daily.
2. The method of claim 1 , wherein each dose of cystamine is about 0.5-1.0g/m 2 body surface area.
3. The method of claim 1 , wherein the total daily dose of cystamine is about 1.35 g/m 2 body surface area or less.
4. The method of claim 1 , wherein the composition comprises enterically coated cystamine or a salt thereof.
5. The method of claim 4 , wherein each dose of cystamine is about 0.5-1.0 g/m 2 body surface area.
6. The method of claim 4 , wherein the total daily dose of cystamine is about 1.35 g/m 2 body surface area or less.
7. The method of claim 4 , wherein the composition comprises a coating selected from the group consisting of polymerized gelatin, shellac, methacrylic acid copolymer type CNF, cellulose butyrate phthalate, cellulose hydrogen phthalate, cellulose proprionate phthalate, polyvinyl acetate phthalate (PVAP), cellulose acetate phthalate (CAP), cellulose acetate trimellitate (CAT), hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate, dioxypropyl methylcellulose succinate, carboxymethyl ethylcellulose (CMEC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), and acrylic acid polymers and copolymers formed from methyl acrylate, ethyl acrylate, methyl methacrylate and/or ethyl methacrylate with copolymers of acrylic and methacrylic acid esters.
8. The method of claim 1 , wherein the pharmaceutical composition comprises a capsule containing enterically coated cystamine granules, wherein the enteric coating allows dissolution during the approximate 3 hour transit time in the small intestine and begins dissolution in the duodenum and continues to dissolve through the mid-small intestine.
9. A method of administering cystamine or a pharmaceutically acceptable salt thereof to a patient with cystinosis, comprising administering to said patient a pharmaceutical composition comprising cystamine or a pharmaceutically acceptable salt thereof, twice per day, wherein the composition increases delivery of cystamine or the pharmaceutically acceptable salt thereof to the small intestine.
10. The method of claim 9 , wherein each dose of cystamine is about 0.5-1.0 g/m 2 body surface area.
11. The method of claim 9 , wherein the total daily dose of cystamine is about 1.35 g/m 2 body surface area or less.
12. The method of claim 9 , wherein the composition comprises enterically coated cystamine or a salt thereof.
13. The method of claim 12 , wherein each dose of cystamine is about 0.5-1.0 g/m 2 body surface area.
14. The method of claim 12 , wherein the total daily dose of cystamine is about 1.35 g/m 2 body surface area or less.
15. The method of claim 12 , wherein the composition comprises a coating selected from the group consisting of polymerized gelatin, shellac, methacrylic acid copolymer type CNF, cellulose butyrate phthalate, cellulose hydrogen phthalate, cellulose proprionate phthalate, polyvinyl acetate phthalate (PVAP), cellulose acetate phthalate (CAP), cellulose acetate trimellitate (CAT), hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate, dioxypropyl methylcellulose succinate, carboxymethyl ethylcellulose (CMEC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), and acrylic acid polymers and copolymers formed from methyl acrylate, ethyl acrylate, methyl methacrylate and/or ethyl methacrylate with copolymers of acrylic and methacrylic acid esters.
16. The method of claim 9 , wherein the pharmaceutical composition comprises a capsule containing enterically coated cystamine granules, wherein the enteric coating allows dissolution during the approximate 3 hour transit time in the small intestine and begins dissolution in the duodenum and continues to dissolve through the mid-small intestine.