Enterically coated cysteamine, cystamine and derivatives thereof

Patent metadata

Field	Value
Publication number	US-2016331691-A1
Application number	US-201615224414-A
Country	US
Kind code	A1
Filing date	Jul 29, 2016
Priority date	Jan 27, 2006
Publication date	Nov 17, 2016
Grant date	—

Abstract

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.

First claim

What is claimed is:

1 . A composition comprising:
delayed and extended release enterically coated cysteamine bitartrate formulation comprising:
a core tablet comprising cysteamine bitartrate and a binder; and
an enteric coating surrounding the core tablet,
wherein the enteric coating releases the cysteamine bitartrate at a pH of 4.5 or greater and provides a C max of between 2-4 hours after administration.

2 . The composition of claim 1 , wherein the enteric coating is selected from the group consisting of polymerized gelatin, shellac, methacrylic acid copolymer type C NF, 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, typically formed from methyl acrylate, ethyl acrylate, methyl methacrylate and/or ethyl methacrylate with copolymers of acrylic and methacrylic acid esters.

3 . The composition of claim 1 , wherein the composition is formulated for oral administration.

4 . The composition of claim 1 , wherein the composition comprises a dose of cysteamine bitartrate of about 0.5-1.0 g/m 2 body surface area.

5 . The composition of claim 1 , wherein the composition comprises a dose of cysteamine bitartrate of about 0.7-0.8 g/m 2 body surface area.

6 . The composition of claim 1 , wherein the enteric coating begins dissolution in the small intestine.

7 . The composition of claim 1 , wherein the cysteamine bitartrate is released during transit in the small intestine.

8 . The composition of claim 1 , wherein the composition further comprises a stabilizer.

9 . A method of treating a subject with cystinosis comprising administering a composition of claim 1 less than 4 times per day, wherein the total daily dose of cysteamine bitartrate is about 1.35 g/m 2 body surface area or less.

10 . A method of treating a subject with cystinosis comprising administering a composition of claim 1 at a dose of cysteamine bitartrate of about 0.5-1.0 g/m 2 body surface area.

11 . A method of treating a subject with cystinosis comprising administering a composition of claim 1 less than 4 times per day in an amount to provide white blood cell cystine suppression with a 12 hour level below 1 nm/½ cystine/mg protein.

12 . A method of treating a subject with cystinosis comprising administering a composition of claim 1 twice per day in an amount to provide white blood cell cystine suppression with a 12 hour level below 1 nm/½ cystine/mg protein.

13 . A method of treating a subject with Huntington's Disease comprising administering the composition of claim 1 comprising a dose of about 100 mg to 1000 mg of cysteamine bitartrate.

Assignees

• Univ California

Inventors

• Dohil Ranjan
• Schneider Jerry

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P39/06

  Free radical scavengers or antioxidants · CPC title

• A61P25/00

  Drugs for disorders of the nervous system · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title

• A61P25/16

  Anti-Parkinson drugs · CPC title