IP Library Granted Patent US 12708618
Granted Patent B2
US 12708618 · App. 18/004,317 · Granted Aug 18, 2026

Pharmaceutical composite formulation comprising proton pump inhibitor and antacid, and method for preparing same

Inventors: Hyuk Jun Cho (Uiwang-si, KR); Bo Sik Kim (Seoul, KR); Ho Taek Im (Paju-si, KR); Yong Il Kim (Gwacheon-si, KR)
Assignee: HANMI PHARM. CO., LTD.
A61K31/4439A61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/209A61K33/08
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Quick Facts
Patent No.
US 12708618
App. No.
18/004,317
Granted
Aug 18, 2026
Kind
B2
Abstract

Provided are a pharmaceutical composite formulation and a method of preparing the same, the pharmaceutical composite formulation including: a first layer containing, as an active ingredient, a proton pump inhibitor or a pharmaceutically acceptable salt thereof and a lubricant, and a second layer containing, as an active ingredient, an antacid selected from magnesium hydroxide, magnesium oxide, and a mixture thereof.

Claims (23)

1 . A pharmaceutical composite formulation comprising:

a first layer comprising, as an active ingredient, a proton pump inhibitor or a pharmaceutically acceptable salt thereof, a lubricant, and a binder; and

a second layer comprising, as an active ingredient, an antacid that is magnesium hydroxide,

wherein the proton pump inhibitor or a pharmaceutically acceptable salt thereof is esomeprazole or a pharmaceutically acceptable salt thereof,

wherein the lubricant in the first layer is sodium stearyl fumarate, wherein the lubricant is comprised in an amount of 3.7 percent by weight (wt %) to 5.5 wt % based on the total weight of the first layer,

wherein the binder is hydroxypropyl cellulose, wherein the binder is comprised in an amount of 1 wt % to 20 wt % based on the total weight of the first layer,

wherein the first layer comprising the proton pump inhibitor or a pharmaceutically acceptable salt thereof, the lubricant, and the binder is in a form of granules, and

wherein when a total weight of the first layer is 1 part by weight, a total weight of the second layer is 1.58 to 3.2 parts by weight.

2 . The pharmaceutical composite formulation of claim 1 , wherein the composite formulation is a tablet or a capsule.

3 . The pharmaceutical composite formulation of claim 1 , wherein the composite formulation is a double-layer tablet having a length ratio of major axis:minor axis of 1:1 to 2.3:1.

4 . The pharmaceutical composite formulation of claim 1 , wherein the first layer further comprises any one selected from the group consisting of a diluent, a disintegrant, and any mixture thereof.

5 . The pharmaceutical composite formulation of claim 1 , wherein the second layer further comprises any one selected from the group consisting of a diluent, a disintegrant, a fluidizing agent, a lubricant, and any mixture thereof.

6 . The pharmaceutical composite formulation of claim 1 , wherein when a mixed solution of 150 mL of 0.1 N HCl and 450 mL of purified water is tested under conditions of 75 rpm and 37±0.5° C. according to the second paddle method of the US Pharmacopoeia (USP) dissolution test item, a dissolution rate of the proton pump inhibitor for 60 minutes is 55% or higher.

7 . A method of preparing the pharmaceutical composite formulation of claim 1 , the method comprising:

preparing a first layer mixed part comprising, as an active ingredient, a proton pump inhibitor or a pharmaceutically acceptable salt thereof, a lubricant, and a binder; and

preparing a second layer mixed part comprising, as an active ingredient, an antacid that is magnesium hydroxide; and

tableting the first layer mixed part and the second layer mixed part,

wherein the preparing of the first layer mixed part comprises a granulation process,

wherein the proton pump inhibitor or a pharmaceutically acceptable salt thereof is esomeprazole or a pharmaceutically acceptable salt thereof,

wherein the lubricant in the first layer is sodium stearyl fumarate, wherein the lubricant is comprised in an amount of 3.7 percent by weight (wt %) to 5.5 wt % based on the total weight of the first layer,

wherein the binder is hydroxypropyl cellulose, wherein the binder is comprised in an amount of 1 wt % to 20 wt % based on the total weight of the first layer,

wherein the first layer comprising the proton pump inhibitor or a pharmaceutically acceptable salt thereof, the lubricant, and the binder is in a form of granules, and

wherein when a total weight of the first layer is 1 part by weight, a total weight of the second layer is 1.58 to 3.2 parts by weight.