Tigecycline composition and preparation method thereof

A technology of tigecycline and composition, applied in the field of tigecycline composition, tigecycline composition and its preparation, capable of solving problems such as tigecycline instability and increasing tigecycline, Achieve the effects of reducing the formation of epimers, enhancing resistance, and inhibiting oxidative degradation

Active Publication Date: 2014-06-25
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to increase the curative effect of tigecycline, expand the applicable population of the product, reduce the safety risk of clinical use, and overcome the shortcoming of tigecycline instability, the present invention provides a new tigecycline composition, thereby solving the problem of above question

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] (A) Place 50 mg of tigecycline in a 10 mL sample bottle, add 2 mL of water to dissolve; (B) Place 50 mg of tigecycline in a 10 mL sample bottle, add 2 mL of water to dissolve, and adjust the pH to 4.5; (C) 50mg of vitamin C was dissolved in 2mL of water, added with NaOH aqueous solution to adjust the pH to 3.5, added 50mg of tigecycline, stirred to dissolve, and adjusted to pH 3.5; (D) 50mg of vitamin C was dissolved in 2mL of water , Add NaOH aqueous solution to adjust the pH to 4.5, add 50mg tigecycline, stir to dissolve, adjust the pH to 4.5; (E) 50mg vitamin C dissolved in 2mL of water, adjust the pH to 6.0, add 50mg tigecycline, stir Dissolve, adjust the pH to 6.0; (F) Dissolve 100mg of threonine in 2mL of water, add hydrochloric acid to adjust the pH to 3.5, add 50mg of tigecycline, stir to dissolve, adjust the pH to 3.5; (G) 100mg of threonine The acid was dissolved in 2mL of water, hydrochloric acid was added to adjust the pH to 4.5, 50mg of tigecycline was added...

Embodiment 2

[0037] (A') 25mg of vitamin C was dissolved in 2mL of water, added NaOH aqueous solution to adjust the pH to 4.5, added 50mg of tigecycline, stirred to dissolve, adjusted to pH 4.5; (B') 50mg of vitamin C was dissolved in 2mL of In water, add NaOH aqueous solution to adjust the pH to 4.5, add 50mg of tigecycline, stir to dissolve, adjust the pH to 4.5; (C') 100mg of vitamin C is dissolved in 2mL of water, NaOH to adjust the pH to 4.5, add 50mg of substitute Gecycline, stir to dissolve, adjust the pH to 4.5; (D') 250mg of vitamin C dissolved in 2mL of water, NaOH to adjust the pH to 4.5, add 50mg of tigecycline, stir to dissolve, adjust the pH to 4.5; (E ') 25mg of threonine was dissolved in 2mL of water, adjusted to pH 4.5 with hydrochloric acid, 50mg of tigecycline was added, stirred to dissolve, and adjusted to pH 4.5; (F') 50mg of threonine was dissolved in 2mL of water, Adjust the pH to 4.5 with hydrochloric acid, add 50mg of tigecycline, stir to dissolve, adjust the pH to ...

Embodiment 3

[0043] (A") 50 mg of vitamin C was dissolved in 2 mL of water, added with NaOH aqueous solution to adjust the pH to 4.5, then 50 mg of tigecycline was added, stirred to dissolve, and adjusted to pH 4.5; (B") 100 mg of threonine was dissolved in Add hydrochloric acid aqueous solution to adjust the pH to 4.5 in 2 mL of water, add 50 mg of tigecycline, stir to dissolve, and adjust the pH to 4.5. The solutions prepared above were respectively filled through a 0.22 μm filter membrane, freeze-dried, and filled with nitrogen to press the plug.

[0044] The freeze-dried sample was placed under the condition of 40° C. / 75% RH for 90 days, and the sample was analyzed by HPLC. The detection method was the same as that in Example 1. The results are shown in Table 3. It can be seen that the addition of vitamin C or its pharmaceutically acceptable salt or amino acid can significantly increase the stability of tigecycline during storage.

[0045] table 3

[0046]

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PUM

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Abstract

The invention relates to a tigecycline composition belonging to the field of medicament preparations, in particular to a tigecycline composition suitable for injection and a preparation method thereof. The composition provided by the invention is prepared by adding one or more selected from Vitamin C or pharmaceutically acceptable salts thereof and amino acids. The tigecycline composition disclosed by the invention not only effectively restricts oxidative degradation, but also remarkably decreases the epimerization of tigecycline and improves the stability of the tigecycline.

Description

Technical field [0001] The invention relates to a tigecycline composition, which belongs to the field of pharmaceutical preparations, and specifically relates to a tigecycline composition suitable for injection and a preparation method thereof. Background technique [0002] Tigecycline (tigecycline) is the first glycylcycline antibiotic approved for clinical intravenous administration. Its structure is similar to tetracycline drugs. As shown in formula I, it was developed and marketed by Wyeth for the treatment of adults Complex skin and skin tissue [0003] Formula I [0004] Infections and complicated intra-abdominal infections in adults. Tigecycline is not stable enough in solution, and the main degradation pathways are oxidative degradation and epimerization, both of which exist simultaneously. Specifically, under weakly alkaline conditions, oxidative degradation is prone to occur; while under acidic conditions, especially when the pH is less than 6.0, epimerization becomes t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/65A61K47/22A61K47/18A61P31/04
Inventor 董平金金张喜全
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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