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Novel acetylsalicylic acid formulations

A technology of acetylsalicylic acid and gastric acid inhibitors, applied in the field of novel acetylsalicylic acid preparations, which can solve the problems of harmful long-term use, large and long-lasting gastric mucosal damage, etc.

Inactive Publication Date: 2008-06-25
FLAMEL TECHNOLOGIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this method is that the damage to the gastric mucosa is very large and long-lasting, and high doses of proton pump inhibitors lead to a constant high pH, ​​which is harmful for long-term use

Method used

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  • Novel acetylsalicylic acid formulations

Examples

Experimental program
Comparison scheme
Effect test

other Embodiment approach

[0052] Other embodiments relate to methods for treating a disease or condition caused by chronic COX, reducing the risk of a thrombotic cardiovascular event in a human patient in need of such treatment and at risk of a thrombotic cardiovascular event, and / or treating a thrombotic disease . The method comprises administering an oral pharmaceutical formulation of the present specification to a patient. The method prevents and / or treats pathological conditions associated with excess thromboxane, in particular cardiovascular diseases and risks. The method consists of oral administration of the pharmaceutical formulation of the invention, preferably once or twice a day.

[0053] The inventors found that surprisingly, they could selectively inhibit COX-1 in the portal vein, allowing minimal aspirin to enter the systemic circulation. This significantly increases patient comfort and drug safety. Patients did not have to discontinue aspirin therapy or switch to another drug. This a...

Embodiment 1

[0112]Example 1: Preparation of aspirin-based microcapsules for controlled release

[0113] 66 g ethylcellulose (Ethocel 7 Premium / Dow), 7 g Plasdone K29 / 32(R) (Povidone / ISP), 8 g castor oil, 9 g magnesium stearate and 10 g tartaric acid were dispersed in 60% isopropanol and 40 % of the acetone composition of the 1200g mixture. This suspension was sprayed onto 900 g of acetylsalicylic acid (aspirin) crystals pre-screened to 200 to 500 μm.

[0114] At pH6.8 (KH 2 PO 4 0.05M / NaOH), these microcapsules were tested under stirring with a stirring blade at a speed of 100 rpm (USP II equipment) in a dissolution medium maintained at 37°C (see Figure 1).

Embodiment 2

[0115] Example 2: Preparation of microcapsules based on omeprazole for controlled release

[0116] Step 1: Disperse 700 g of omeprazole and 100 g of Klucel EF(R) (Hydroxypropylcellulose / Aqualon) in 3000 g of isopropanol. The suspension was sprayed onto 200 g of neutral microspheres (Asahi-Kasei) in a spray coater Glatt GPCG 1 .

[0117] Step 2: 50 g ethylcellulose (Ethocel 20 Premium / Dow), 20 g Plasdone K29 / 32(R) (povidone / ISP), 20 g Lutrol F-68 (poloxamer 188 / BASF) and 10 g castor oil were dispersed in a in a mixture of 60% isopropanol and 40% acetone. This solution was sprayed onto 900 g of omeprazole granules (from step 1).

[0118] The microparticles obtained are filled into size 3 gelatin capsules. In this trial, the dose of omeprazole per capsule was 80 mg, ie 127 mg of microcapsules. At pH6.8 (KH 2 PO 4 0.05M / NaOH), these microcapsules were tested under stirring with a stirring blade at a speed of 100 rpm (USP II equipment) in a dissolution medium maintained at 3...

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Abstract

The invention relates to pharmaceutical compositions of acetylsalicylic acid-based microcapsules to selectively inhibit the COX in the portal vein and / or in the liver to reduce the production of thromboxane. Further, the pharmaceutical composition minimizes COX inhibition in the systemic circulation to optimize the inhibition of platelet aggregation. Certain embodiments also address methods of prevention and / or treatment of these diseases, using these oral compositions such as enhancing the safety of antithrombotic treatments. Other embodiments contemplate oral pharmaceutical compositions that combine acetylsalicylic acid with anti-platelet aggregation drugs, without inducing gastric side effects.

Description

Background technique [0001] In patients with established cardiovascular disease, aspirin use has been shown to reduce the risk of primary myocardial infarction, stroke, and vascular death. Aspirin may also be used to prevent cardiovascular events in patients with established cardiovascular disease such as myocardial infarction, stroke or angina. Typically, aspirin use is recommended for these individuals based on a demonstrated reduction in future cardiovascular events and mortality. [0002] Aspirin, or acetylsalicylic acid, prevents platelet aggregation by irreversibly inhibiting cyclooxygenases (COX). There are many types of COX, including COX-I, COX-2, COX-3, and COX-derived proteins, collectively referred to as COX. COX converts arachidonic acid to thromboxane, a potent vasoconstrictor and activator of platelet aggregation. Aspirin inhibits COX by acetylating COX. Inhibition of COX activity by aspirin is generally irreversible. This is an important distinction for as...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K45/06
CPCA61K45/06A61K31/60A61K9/1652A61K9/5026A61K9/5084A61K9/5047A61K9/1676
Inventor 热拉尔・苏拉弗洛朗斯・甘贝尔托
Owner FLAMEL TECHNOLOGIES
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