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Lipopeptide compositions and related methods

A technology for drugs and substances, applied in chemical instruments and methods, drug combinations, peptides, etc., can solve the problems of inability to stabilize daptomycin, inability to prevent daptomycin isomerization, and inability to prevent degradation of daptomycin

Active Publication Date: 2012-10-03
CUBIST PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Kirsch was unable to stabilize daptomycin and prevent the conversion of daptomycin to anhydro-daptomycin and its subsequent isomerization to the β-isomer
Kirsch also does not prevent the degradation of daptomycin to other degradation products unrelated to anhydro-daptomycin and the β-isomer

Method used

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  • Lipopeptide compositions and related methods
  • Lipopeptide compositions and related methods
  • Lipopeptide compositions and related methods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1A

[0096] Example 1A: Comparative Preparation Method A (lyophilized daptomycin without sugar or amino acid at pH 4.7)

[0097] Complexation of comparative daptomycin formulations without sugar or glycine was performed under refrigerated (2-10°C) conditions. Daptomycin active pharmaceutical ingredient (API) is supplied as a frozen liquid at pH 3.0 in the concentration range of 125-130 mg / mL. Complexation was initiated by obtaining liquid daptomycin API (eg, thawing frozen daptomycin API provided at a pH of about 3.0), followed by adjusting the pH to a target pH of about 4.7 using 3N NaOH. The bulk solution was further diluted with sWFI to a target concentration of 105 mg / mL and mixed to ensure a homogeneous solution (again at 2-10°C). The bulk product solution was 0.2 μm filtered and filled into 10 mL vials, followed by lyophilization according to the current lyophilization cycle set forth in Example 3. The drug product formulation was capped and sealed under nitrogen.

Embodiment 1B

[0098] Example 1B: Comparative Preparation Method B (lyophilized daptomycin without sugar or amino acid at pH 7.0)

[0099] Compounding of the overall formulation was performed under refrigerated (2-10°C) conditions. Daptomycin API is supplied as a frozen liquid at pH 3.0 in the concentration range of 125-130 mg / mL. The population was complexed by thawing the API and then adjusting the pH to a target pH of approximately 7.0 using 3N NaOH under frozen (2-10°C) conditions, followed by dilution with sWFI to a target concentration of 105 mg / mL and mixing to ensure a homogeneous solution. preparation. The formulated drug product was 0.2 μm filtered and filled into 10 mL vials, followed by lyophilization according to the modified lyophilization cycle set forth in Example 3. The drug product formulation was capped and sealed under nitrogen.

Embodiment 2A

[0100] Example 2A: Preparation Method A (lyophilized at pH 4.7)

[0101] Compounding of the improved daptomycin formulation was performed under refrigerated (2-10°C) conditions. Daptomycin active pharmaceutical ingredient (API) is supplied as a frozen liquid at pH 3.0 in the concentration range of 125-130 mg / mL. By obtaining liquid daptomycin API (e.g., thawing frozen daptomycin API provided at a pH of about 3.0), then adjusting the pH to a target pH of about 4.7 using 3N NaOH, followed by adding one or more sugars ( Such as sucrose) to start the complex. The bulk solution was further diluted with sWFI to a target concentration of 105 mg / mL and mixed to ensure a homogeneous solution (again at 2-10°C). The bulk product solution was 0.2 μm filtered and filled into 10 mL vials, followed by lyophilization according to the current lyophilization cycle set forth in Example 3. The drug product formulation was capped and sealed under nitrogen. The sugar is added as a powder or in ...

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Abstract

The present disclosure provides novel powder daptomycin formulations which have improved chemical stability and faster reconstitution times when in the solid state. Some examples of the compositions comprise daptomycin and sucrose.

Description

[0001] related application [0002] This application claims the benefit of US Provisional Patent Application 61 / 263,784, filed November 23, 2009, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates to improved lipopeptide compositions for reconstitution in liquid diluents to form pharmaceutical compositions for parenteral administration, and methods of preparing solid lipopeptide compositions. Preferred improved lipopeptide compositions include solid daptomycin formulations with increased reconstitution rates and / or increased daptomycin chemical stability in aqueous liquids. Background technique [0004] Daptomycin is a cyclic lipopeptide antibiotic indicated for the treatment of complicated skin and skin structure infections and bacteremia, including bacteremia with suspected or proven infective endocarditis. Daptomycin for injection can be administered intravenously to treat indicated infections caused by susce...

Claims

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Application Information

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IPC IPC(8): C07K7/64C07K7/06C07K7/08A61K38/12A61P31/04
CPCA61K38/12A61K9/08A61K47/26A61K38/00A61K9/19A61K9/00A61K38/10A61K9/0019C07K11/02A61P17/00A61P31/00A61P31/04A61K2121/00
Inventor S.孙G.纳伊克S.奥康纳
Owner CUBIST PHARMA INC
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