Modified release composition of orlistat and acarbose for the treatment of obesity and related metabolic disorders

A modified-release oral composition comprising orlistat and acarbose, comprising as individually distinct parts with different release patterns:

• (a) a first part (G1) comprising acarbose and one or more of a hydrophobic polymer, a lipid and a wax, wherein G1 comprises from about 5 to about 70% w/w of the total dose of acarbose present in the composition;
• (b) a second part (G2) comprising acarbose, orlistat, an enteric polymer and a surfactant, wherein G2 comprises from about 30 to about 95% w/w of the total dose of acarbose present in the composition, and from about 10 to about 90% w/w of the total dose of orlistat present in the composition;
• and
• (c) a third part (G3) comprising orlistat and one or more of a surfactant and a water-soluble polymer, wherein G3 comprises from about 10 to about 80% w/w of the total dose of orlistat present in the composition.

A method for treating or reducing the risks of a condition selected from one or more of being overweight, obesity, type 2 diabetes, elevated blood glucose levels, impaired glucose tolerance, polycystic ovarian syndrome, disorders of lipoprotein metabolism, lipidemia, hyperglyceridemia;

• nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis;
• and metabolic syndrome, comprising administering to a subject in need thereof:
• (i) a modified-release oral composition comprising acarbose, comprising as individually distinct parts with different release patterns (a) a first part comprising acarbose and one or more of a hydrophobic polymer, a lipid and a wax, wherein the first part comprises from about 5 to about 70% w/w of the total dose of acarbose present in the composition;
• and (b) a second part comprising acarbose, an enteric polymer and a surfactant, wherein the second part comprises from about 30 to about 95% w/w of the total dose of acarbose present in the composition;
• and
• (ii) a modified-release oral composition comprising orlistat, comprising as individually distinct parts with different release patterns (a) a first part comprising orlistat, an enteric polymer and a surfactant, wherein the first part comprises from about 10 to about 90% w/w of the total dose of orlistat present in the composition, and does not include acarbose;
• and (b) a second part comprising orlistat and one or more of a surfactant and a water-soluble polymer, wherein the second part comprises from about 10 to about 80% w/w of the total dose of orlistat present in the composition.