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Stably isoosmotic desmoteplase alpha1 or mutant preparation thereof

An aminoplase and mutant technology, applied in the field of biomedicine, can solve the problems of loss of activity, difficult recovery of activity, change of tertiary structure, etc., and achieve the effects of improving stability, easy acceptance, and easy storage.

Inactive Publication Date: 2010-07-28
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] (4) Formation of wrong disulfide bonds Exchange between disulfide bonds or between disulfide bonds and sulfhydryl groups can form wrong disulfide bonds, resulting in changes in tertiary structure and loss of activity
In the denatured state, peptides tend to be more prone to chemical reactions, and the activity is difficult to restore

Method used

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  • Stably isoosmotic desmoteplase alpha1 or mutant preparation thereof
  • Stably isoosmotic desmoteplase alpha1 or mutant preparation thereof
  • Stably isoosmotic desmoteplase alpha1 or mutant preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: Preparation of a stable isotonic DSPAα1 lyophilized preparation with 10 mM phosphate buffer at pH 5.8 as a buffer system

[0037] Detailed prescription

[0038]

[0039] Preparation:

[0040] Prepare the prescribed amount of 10mM phosphate buffer solution with pH 5.8, accurately weigh the excipients in the prescribed amount, add an appropriate amount of phosphate buffer solution to dissolve, adjust the pH value to 5.5-6.5, and set the volume to the total volume of the solution Difference from DSPAα1 stock solution. Add the prescribed amount of DSPAα1 stock solution into it, shake gently to mix, sterilize and filter with a microporous membrane with a pore size of 0.22 μm, subpackage, freeze-dry, stopper, and press the cap to obtain the product.

Embodiment 2

[0041] Embodiment 2: 20mM phosphate buffer with pH 6.0 is buffer system and prepares stable isotonic DSPA α1 mutant DSMa lyophilized preparation

[0042] prescription composition

[0043]

[0044] Preparation:

[0045] Prepare the prescribed amount of 20mM phosphate buffer solution with pH 6.0, accurately weigh the excipients in the prescribed amount, add an appropriate amount of phosphate buffer solution to dissolve, adjust the pH value to 5.5-6.5, and set the volume to the total volume of the solution Difference with DSMa stock solution. Add the prescribed amount of DSMa stock solution into it, shake gently to mix, sterilize and filter with a microporous filter membrane with a pore size of 0.22 μm, sub-package, freeze-dry, stopper, and cap, to obtain.

Embodiment 3

[0046] Example 3: Preparation of stable isotonic DSPA α1 mutant DSMb lyophilized preparation with 0.1M citrate buffer at pH 6.2 as buffer system

[0047] prescription composition

[0048]

[0049] Preparation:

[0050] Prepare the prescribed amount of 0.1M citrate buffer solution with pH 6.2, accurately weigh the excipients in the prescribed amount, add an appropriate amount of phosphate buffer solution to dissolve, adjust the pH value to 5.5-6.5, and dilute to the volume for the recipe. The difference between the total volume of the solution and the stock solution of DSMb. Add the prescribed amount of DSMb stock solution into it, shake gently to mix, sterilize and filter with a microporous filter membrane with a pore size of 0.22 μm, subpackage, freeze-dry, stopper, and press the cap to obtain the product.

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PUM

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Abstract

The invention discloses a stably isoosmotic freeze-drying preparation, which takes a recombinant desmoteplase alpha1vampire bat plasminogen activator or mutant thereof as an active ingredient. The stably isoosmotic freeze-drying preparation comprises the desmoteplase alpha1 or the mutant thereof and a freeze-drying protective agent. The freeze-drying preparation of the invention can be re-prepared into a solution preparation by using a proper diluent so as to be used in clinic.

Description

technical field [0001] The invention relates to a freeze-dried preparation with recombinant vampire bat plasminogen activator desmoteplase α1 or a mutant thereof as an active ingredient, belonging to the technical field of biomedicine. Background technique [0002] Desmoteplase (DSPA) is a plasminogen activator isolated from the saliva of a vampire bat in South America. It mainly includes four proteins: DSPAα1, DSPAα2, DSPAβ and DSPAγ. It was found that desmoteplase α1 has the best biochemical and pharmacological properties, so it was further studied. Studies have shown that: under the stimulation of fibrin, the activity of desmoteplase α1 increases by 10500 times, while that of tissue plasminogen activator (tPA) is only 550 times; in the presence of fibrin and fibrinogen, desmoteplase α1 The ratio of enzyme α1 activity is 12900 times, while tPA is only 72 times, desmoteplase α1 has higher fibrin selectivity. Pharmacological studies have shown that in the model of pulmonar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/49A61K9/19A61P7/02
Inventor 刘禄娟杨清敏马中珲张明会王晶翼
Owner QILU PHARMA
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