Pharmaceutical compositions for gastrointestinal drug delivery

Patent metadata

Field	Value
Publication number	US-8974825-B2
Application number	US-14489408-A
Country	US
Kind code	B2
Filing date	Jun 24, 2008
Priority date	Jul 6, 2007
Publication date	Mar 10, 2015
Grant date	Mar 10, 2015

Abstract

A novel pharmaceutical composition, which comprises a therapeutically effective amount of active principle(s) or a pharmaceutically acceptable salt or enantiomer or polymorph thereof, optionally one or more release controlling agent(s) and pharmaceutical acceptable excipient(s) thereof, wherein the composition is formulated to increase the residence time of the said pharmaceutical composition and/or active principle(s) in the gastrointestinal tract. A novel pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is controlled release. A pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is bioadhesive. A pharmaceutical composition comprising: at least two entities wherein one entity is controlled release and the other is bioadhesive All the three compositions are formulated to increase the residence time of active principle(s) in the gastrointestinal tract. A multilayered composition with active in a layer which provides immediate release or controlled release of active principles and layer providing increased residence time in the GI tract.

First claim

The invention claimed is:

1. An oral multilayer tablet comprising:
a first layer comprising a pharmaceutical composition comprising rifaximin or a pharmaceutically acceptable salt thereof and that is configured for immediate or fast release of the rifaximin or salt thereof; and
a second layer comprising the rifaximin or salt thereof and a polymer having affinity for gastrointestinal mucosa,
wherein the polymer adheres to the gastrointestinal mucosa and provides increased residence time of the tablet in the gastrointestinal tract by bioadhesion which is independent of food effect,
wherein the composition has an adhesive strength, measured as a force of detachment, of at least 1000 mN in 30 minutes, and
wherein bioadhesion is provided for a period greater than 0.5 hour.

2. The multilayer tablet of claim 1 , comprising at least one active principle in addition to rifaximin.

Assignees

• Jahagirdar Harshal Anil
• Kulkarni Rajesh
• Kulkarni Shirishkumar
• Lupin Ltd

Inventors

• Jahagirdar Harshal Anil
• Kulkarni Rajesh
• Kulkarni Shirishkumar

Classifications

• A61K9/1641

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers · CPC title

• A61K9/0095 Primary

  Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006) · CPC title

• A61K9/0065 Primary

  Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus · CPC title

• A61K9/2031

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers · CPC title

• A61K9/2086

  Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28) · CPC title