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ENTERIC COATED LANSOPRAZOLE FORMULATION

IP.com Disclosure Number: IPCOM000177493D
Publication Date: 2008-Dec-15
Document File: 5 page(s) / 71K

Publishing Venue

The IP.com Prior Art Database

Abstract

An enteric coated lansoprazole formulation comprising: a) a core comprising lansoprazole, and one or more pharmaceutically acceptable excipients; b) an intermediate layer surrounding the core and c) an enteric layer surrounding the core, wherein the enteric layer comprises polyethylene glycol 400 has been developed.

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ENTERIC COATED LANSOPRAZOLE FORMULATION

Abstract

An enteric coated lansoprazole formulation comprising: a) a core comprising lansoprazole, and one or more pharmaceutically acceptable excipients; b) an intermediate layer surrounding the core and c) an enteric layer surrounding the core, wherein the enteric layer comprises polyethylene glycol 400 has been developed.

U.S.

Patent Nos. 4,255,431; 4,628,098; and 4,758,579 disclose substituted pyridylsulfinyl benzimidazoles as potent inhibitors of gastric acid secretion.  This class of compounds inhibit gastric acid secretion by inhibiting H+-K+ ATPase (proton-pump) activity. Lansoprazole is a substituted benzimidazole, 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl] methyl] sulfinyl] benzimidazole, a compound that inhibits gastric acid secretion.  Lansoprazole is highly unstable in acidic enviornment.  

The choice of the plasticizer was found to be critical to the manufacturing process of the formulation as well as to the release characteristics and hence the bioavailability of the formulation after oral administration.  It was observed that polyethylene glycol 400 has an advantage of making better films compared to prior art plasticizers such as PEG 300 that makes too soft films.  It has also been found that choice of appropriate plasticizer in the enteric layer is critical to the in vivo bioavailability of the formulation.  Polyethylene glycol 400, as plasticizer, in enteric coating pellet compositions is capable of giving a formulation that is bioequivalent to Prevacid® capsules, commercially available in the

U.S.

from Takeda Pharmaceuticals.

An enteric coated lansoprazole formulation has been developed, wherein the formulation comprises,: a) a core comprising lansoprazole and one or more pharmaceutically acceptable excipients; b) an intermediate layer surrounding the core; and c) an enteric layer surrounding the intermediate layer, wherein the enteric layer comprises polyethylene glycol 400.

The formulation described above can be prepared by a process comprising the steps of: a) preparing a core by coating an inert carrier with an aqueous dispersion of lansoprazole, and one or more pharmaceutically acceptable excipients; b) coating the core with an intermediate layer; and c) covering the intermediate layer with an enteric layer comprising polyethylene glycol 400.

The term “lansoprazole” includes lansoprazole free base, pharmaceutically acceptable salts, solvates and mixtures thereof.  

The term “core”, as used herein, refers to pharmaceutically acceptable inert carrier coated with a mixture of lansoprazole and pharmaceutically acceptable excipients.

The pharmaceutically acceptable “inert carrier” may include starch, microcrystalline cellulose or sugar sphere, such as nonpareil sugar seeds.

The “pharmaceutically acceptable excipients”...