Injectable polymer nanoparticle compositions of antithrombotic agents and methods thereof

A nanoparticle and composition technology, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as poor oral bioavailability

Active Publication Date: 2022-02-08
FORDOZ PHARMA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, many of these antithrombotic agents mentioned above are hydrophobic and have limited water solubility, resulting in poor oral bioavailability

Method used

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  • Injectable polymer nanoparticle compositions of antithrombotic agents and methods thereof
  • Injectable polymer nanoparticle compositions of antithrombotic agents and methods thereof
  • Injectable polymer nanoparticle compositions of antithrombotic agents and methods thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0087] Example 1. General preparation of mPEG-PLA polymer micelles containing apixaban The method used for the preparation of polymer micelles containing apixaban can refer to Int. 206 and J. Control. Release, 2001, 72, 191-202.

[0088] Briefly, apixaban (7.7 mg) and mPEG-PLA (770 mg, molecular weight = 3860-4200 Daltons) were dissolved in 5 mL of methanol / dichloromethane (3 / 7 v / v) mixed solvent. Then the organic solvent was removed under reduced pressure at 60°C to obtain a transparent gel matrix, which was dissolved by adding 25mM citrate buffer (pH 6.1) at 60°C to form a transparent apixaban-encapsulated micellar solution. The solution was sterilized by filtration through a 0.22 μm membrane and then lyophilized using a freeze dryer system.

[0089] An average micelle size of 19.8 nm was observed at a concentration of apixaban of 0.5 mg / mL. One or more lyoprotectants are dissolved in the apixaban solution. The resulting apixaban-lyoprotectant solution was then lyophilize...

Embodiment 2

[0090] Example 2. Apixaban-containing polymer micelle composition was prepared by the method described in Example 1 using the following ingredients:

[0091] mPEG-PLA (molecular weight = 3860-4200 Daltons), 100 mg.

[0092] Apixaban, 1mg

[0093] water, 2mL.

Embodiment 3

[0094] Example 3. Apixaban-containing polymer micelle composition was prepared by the method described in Example 1 using the following ingredients:

[0095] mPEG-PLA (molecular weight = 3860-4200 Daltons), 100mg

[0096] Apixaban, 1mg

[0097] 25mM citrate buffer (pH 6.1), 2mL.

[0098] Sucrose: 222mg.

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Abstract

Disclosed are injectable nanoparticle compositions comprising a micelle formulation of an antithrombotic agent and a water-soluble, biodegradable, and amphiphilic polymer that improves water solubility of the antithrombotic agent. A method of preparing the injectable nanoparticle compositions and methods for preventing or treating thrombotic diseases such as venous thromboembolisms and / or stroke using the compositions, as well as devices and kits suitable for such treatment, are also disclosed.

Description

[0001] Cross references to related applications: [0002] This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application No. 62 / 846,058, filed May 10, 2019; the disclosure of which is incorporated herein by reference in its entirety. [0003] field of invention [0004] The present disclosure relates to injectable nanoparticle compositions for the prevention or treatment of thrombotic disorders such as venous thromboembolism and / or stroke. [0005] Background of the invention [0006] The recent development of new drugs has resulted in more and more new drugs with poor water solubility and thus poor bioavailability. These poorly water-soluble drugs administered orally are often excreted from the gastrointestinal tract before being fully dissolved and absorbed into the circulatory system, which often results in low bioavailability of these compounds. Therefore, dose increases are required to achieve therapeutic drug concentrations in the circulation. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/107A61K47/10A61K47/24A61K47/34A61K45/00A61K31/4545A61K45/06A61P7/02
CPCA61K47/10A61K9/0019A61K9/08A61K31/4545A61K9/1075A61P7/02A61K45/06A61K2300/00
Inventor 辛启胜S·乌格J·贺
Owner FORDOZ PHARMA CORP
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