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Oral pharmaceutical dosage form comprising as active ingredients a proton pump inhibitor together with acetyl salicyclic acid

A proton pump inhibitor, acetylsalicylic acid technology, applied in the directions of organic active ingredients, salicylic acid active ingredients, medical preparations containing active ingredients, etc., can solve unsatisfactory, inconvenient to obtain optimal results, etc. question

Inactive Publication Date: 2008-12-03
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, administration of two or even more different tablets / capsules to the patient is inconvenient or unsatisfactory for optimal results

Method used

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  • Oral pharmaceutical dosage form comprising as active ingredients a proton pump inhibitor together with acetyl salicyclic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0161] Male or female Helicobacter pylori-negative patients 60 years of age or older, who have a moderate to high risk of gastroduodenal ulcers, are included in a randomized, double-blind, multi-center, placebo-controlled trial. The patients were randomized to receive esomeprazole 20mg (take esomeprazole magnesium, which is owned by AstraZeneca AB ) Or placebo, once a day for 26 weeks. The primary outcome variable is endoscopy for the presence of gastric and / or duodenal ulcers after 26 weeks.

[0162] A total of 991 patients were included in the population to be treated, all of whom received ASA at a dose between 75-325 mg / day (57.1% of men, average age 69.3 years, average acetylsalicylic acid (ASA) dose 124.0 mg / day) . The cumulative proportion of patients without gastric or duodenal ulcers in 26 weeks is: 98.2% of those taking esomeprazole, compared with 93.8% of those taking placebo (life table assessment, p=0.0007 ). The incidence of gastric ulcer was lower in patients taking...

Embodiment 2

[0164] Capsules containing 20 mg of esomeprazole and 325 mg of ASA particles.

[0165] Principle: An enteric-coated pellet containing esomeprazole magnesium trihydrate corresponding to 20 mg of esomeprazole is produced and mixed with magnesium stearate.

[0166] This mixture and ASA microparticles are filled into hard gelatin capsules.

[0167] Manufacturing of enteric-coated esomeprazole pellets

[0168] Core material

[0169] Sugar spherical seeds 0.25 to 0.35mm approximate diameter 300g

[0170] Active layer

[0171] Esomeprazole Magnesium Trihydrate 445g

[0172] Hydroxypropyl methylcellulose 67g

[0173] Polysorbate 80 9g

[0174] Purified water 2100g

[0175] Primer

[0176] Hydroxypropyl cellulose 90g

[0177] Talc 340g

[0178] Magnesium stearate 22g

[0179] Purified water 3100g

[0180] Enteric coating

[0181] Methacrylic acid copolymer type C, 30% dispersion 1270g

[0182] Triethyl citrate 38g

[0183] Glycerol mono and diglycerides 19g

[0184] Polysorb...

Embodiment 3

[0206] Capsules containing 20 mg of esomeprazole and 325 mg of ASA powder.

[0207] Principle: An enteric-coated pellet containing esomeprazole magnesium trihydrate corresponding to 20 mg of esomeprazole was produced and mixed with magnesium stearate, according to Example 2.

[0208] This mixture and ASA powder are filled into hard gelatin capsules.

[0209] Capsule filling

[0210] Per capsule

[0211] Mixture of enteric-coated esomeprazole pellets and magnesium stearate 86.2mg

[0212] (According to Example 2 above)

[0213] ASA powder 325mg

[0214] Hard capsule, size number 0 1

[0215] Place the capsule according to the above in a plastic (high-density polyethylene, also known as HDPE) bottle with a desiccant, and check the stability. The results obtained can be seen in the table below;

[0216] surroundings

[0217] NT = not tested

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Abstract

The present invention relates to an oral pharmaceutical preparation for use in the prevention and / or reduction of gastrointestinal complications associated with the use of acetyl salicylic acid. The present preparation comprises a fixed oral dosage form comprising a proton pump inhibitor in combination with acetyl salicylic acid. Furthermore, the present invention refers to a method for the manufacture thereof and the use thereof in medicine. The present invention also relates to a specific combination comprising esomeprazole, or an alkaline salt thereof or a hydrated form of any one of them, and acetyl salicylic acid for use as a medicament for the prevention of thromboembolic vascular events, such as myocardial infarction or stroke, and for the prevention and / or reduction of gastrointestinal complications associated with the use of acetyl salicylic acid.

Description

Invention field [0001] The present invention relates to oral pharmaceutical preparations for preventing and / or reducing gastrointestinal complications related to acetylsalicylic acid treatment. The preparation contains a fixed oral dosage form, which includes a combination of a proton pump inhibitor (hereinafter also referred to as PPI, namely proton pump inhibitor) and acetylsalicylic acid (hereinafter also referred to as ASA) or its derivatives. In addition, the present invention relates to the manufacturing method of the dosage form and its use in medicine. [0002] The present invention also relates to a specific combination containing esomeprazole or its alkali metal salt or any one of the hydrated forms and acetylsalicylic acid in an oral fixed combination dosage form, the dosage form including esomeprazole A group of individual physical units of azole or its alkali metal salt or a hydrated form of any one of them and other individual physical units containing one or more of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/60A61K9/20A61K9/48A61P1/04A61P9/10A61K31/4184A61K31/4439A61K31/444
Inventor D·约翰逊L·尼尔森L·－E·斯维德伯格
Owner ASTRAZENECA AB
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