US 2012/0058194 A1Published application

Pharmaceutical formulations comprising substituted benzimidazole derivatives

OwnerNavin Vaya, Mamta Mishra +10inventors

InventorsNavin Vaya, Mamta Mishra, Atul Shivaji Shinde, Harshal Prabhakar Bhagwatwar, Debashis Dash, Deepti Jain, Rahul Sudhakar Gawande, Vishal Lad, Sushant Dube, Venkateswarlu Vobalaboina, Srinivas Irukulla, Manikandan Ramalingam

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Abstract

Stabilized substituted benzimidazole modified release pharmaceutical formulations with at least two drug-containing fractions, wherein the release from a first fraction precedes the release from a second fraction, pharmaceutical excipients, processes for preparing the stable formulations, packaging therefor, and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.

Claims26

Dependent claims

A pharmaceutical formulation for oral administration, comprising:

(a) a first fraction, comprising:
(i) a core containing a substituted benzimidazole derivative or a pharmaceutically acceptable salt thereof, at least one stabilizer, and at least one pharmaceutically acceptable excipient;
and
(ii) a pH-dependently soluble release-controlled coating layer surrounding the core, wherein the pH-dependently soluble release-controlled coating layer dissolves in a pH range of about 5-6;
and
(b) a second fraction, comprising:
(i) a core containing a substituted benzimidazole derivative or a pharmaceutically acceptable salt thereof, at least one stabilizer, and at least one pharmaceutically acceptable excipient;
and
(ii) a release-controlled coating layer surrounding the core, wherein the release-controlled coating layer comprises one or more pH-independent polymers and one or more pH-dependently soluble release-controlled coating polymers.

6 more elements

A pharmaceutical formulation for oral administration, comprising:

(a) an inert core;
(b) a first layer containing a substituted benzimidazole derivative or a pharmaceutically acceptable salt thereof, at least one stabilizer, and at least one pharmaceutically acceptable excipient surrounding the core of (a);
(c) a first pH-dependently soluble release-controlled coating layer surrounding the layer of b), wherein the pH-dependently soluble release-controlled coating layer is soluble in a pH range of about 6-8;
(d) a layer containing a substituted benzimidazole derivative or a pharmaceutically acceptable salt thereof, at least one stabilizer, and at least one pharmaceutically acceptable excipient, coated over the pH-dependently soluble release-controlled coating layer of (c);
and
(e) a pH-dependently soluble release-controlled coating layer surrounding the layer of (d), wherein the pH-dependently soluble release-controlled coating layer is soluble in a pH range of about 4-6.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application: 13/217,901Filed 25 Aug 2011
Priority: IN 2475/CHE/201027 Aug 2010
Published: 8 Mar 2012
Term ends: Not estimatedThe source records don’t support an estimate.

Classification9 codes

A61K 31/4439
Containing further heterocyclic ring systems: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 9/5026
Organic macromolecular compounds: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, polyacrylates
A61K 9/5047
Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose: cellulose ethers containing no…
A61K 9/5078
Having two or more different coatings optionally including drug-containing subcoatings: with drug-free core