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Storage-stable and bio-stable formulations of ACE inhibitors, and methods for preparation thereof

A storage stability and inhibitor technology, which can be used in medical preparations containing active ingredients, pharmaceutical formulations, active ingredients of heterocyclic compounds, etc., and can solve problems such as stability that are not discussed.

Inactive Publication Date: 2006-04-12
SIGMAPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Harris does not discuss stability under adverse temperature and humidity storage conditions

Method used

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  • Storage-stable and bio-stable formulations of ACE inhibitors, and methods for preparation thereof
  • Storage-stable and bio-stable formulations of ACE inhibitors, and methods for preparation thereof
  • Storage-stable and bio-stable formulations of ACE inhibitors, and methods for preparation thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0034] The invention provides a storage-stable and biologically stable ACE inhibitor, especially a preparation method of enalapril maleate and quinapril hydrochloride preparations. The method comprises the steps of: mixing an ACE inhibitor, such as enalapril maleate, with alcohol to form an alcohol dispersion of the ACE inhibitor, and then dissolving or dispersing the metal compound in water to form a metal compound solution or dispersion, The alcoholic dispersion of the ACE inhibitor and the aqueous solution or dispersion of the metal compound are mixed together to form a "final aqueous alcoholic solution or dispersion" of the ACE inhibitor and the metal compound. In another embodiment, the method comprises the steps of: mixing an ACE inhibitor, such as quinapril hydrochloride, with a mixture of alcohol and water (aqueous alcoholic system) to form an aqueous alcoholic dispersion of the ACE inhibitor, and The metal compound is added thereto under constant stirring to form a "f...

Embodiment 1

[0059] The amounts of ingredients provided in the formulations below are by equivalent weight (mg per unit dose (mg / ud)). The approximate batch size is about 6000 units.

[0060] Preparation of Formulation I

[0061] Enalapril maleate (20 mg / ud; Byron Chem. Co., Long Island City, NY) was suspended in SD3A denatured alcohol (50 mg / ud) with stirring at 500 rpm. In less than 10 seconds, enalapril maleate was completely dispersed in alcohol. In a separate container, sodium bicarbonate (11 mg / ud) and povidone (polyvinylpyrrolidone; Plasdone(R), ISP, Bound Brook, New Jersey) were dissolved in 100 mg / ud purified water (USP). The sodium bicarbonate / povidone solution was gradually added to the alcohol dispersion of the drug under constant stirring (200 rpm) until a transparent solution was obtained, resulting in Solution 1, for example, the solution was free of foam (bubbles).

[0062] Microcrystalline cellulose (225 mg / ud, Avicel® PH200; FMC Corporation, Philadelphia, PA), sodium s...

Embodiment 2

[0121] Comparison of stability profiles of different formulations of enalapril maleate.

[0122] Comparison of the stability profiles of different formulations of enalapril maleate. Formulation stability of stabilized enalapril maleate (Formulations I-IV, as described above) and a marketed formulation of enalapril maleate, known as "enalapril- Commodity" VASOTEC TM (Merck & Co.) for comparison. Formulations were stored at 60°C and 75% relative humidity to simulate long-term storage. Formulation stability was assessed by HPLC at 5, 10, and 15 days.

[0123] like figure 1 As shown, at the 5, 10, and 15 day time points, formulation I was more effective than VASOTEC TM Formulations and Formulations II-IV are more stable. At the 5 and 10 day time points, Formulation II exhibited greater TM Better stability of formulations. Formulation II was more effective than VASOTEC at the 5, 10, and 15 day time points TM Formulation and Formulation IV are more stable.

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Abstract

The present invention provides storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride, that can be manufactured in a time efficient and cost effective manner. Such formulations can be prepared simply and on a large industrial scale using conventional methods and equipment. The present invention also provides methods for the preparation of highly manufacturable, storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride. Methods for treatment of cardiovascular disorders using storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride, are also provided.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Patent Application (now unknown) filed December 4, 2003 and is a continuation-in-part of US Application Serial No. 10 / 364,970, filed February 12,2003. field of invention [0003] The present invention relates to storage stable and biologically stable ACE inhibitor preparations and similar drugs, especially enalapril maleate and quinapril hydrochloride. The invention also relates to the preparation and industrial scale production of storage stable and biologically stable formulations of ACE inhibitors which have acceptable production characteristics and which are time saving and cost effective. Background of the invention [0004] ACE inhibitors, ie angiotensin converting enzyme inhibitors, are drugs used in the treatment of cardiovascular disorders, especially hypertension. However, it has been widely noted that ACE inhibitors are susceptible to decomposition, especially due to h...

Claims

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Application Information

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IPC IPC(8): A61K38/55A61K31/44A61K31/40
Inventor 斯皮里东·斯皮雷亚斯
Owner SIGMAPHARM
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