Sustained releasing microspheric preparation of glucokinase mutant and its making method

A sustained-release microsphere preparation and technology of sustained-release microspheres, which are applied in the field of biopharmaceuticals, can solve the problems that there is no research report on staphylokinase mutant sustained-release microspheres, and achieve uniform appearance, good biocompatibility, and encapsulation. high rate effect

Inactive Publication Date: 2005-10-12
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After reviewing the literature, there is no report on staphylokinase mutant sustained-release microspheres and related research

Method used

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  • Sustained releasing microspheric preparation of glucokinase mutant and its making method
  • Sustained releasing microspheric preparation of glucokinase mutant and its making method
  • Sustained releasing microspheric preparation of glucokinase mutant and its making method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]Emulsify 0.2ml of 10mg / ml DGR solution (0.02M phosphate buffer, pH 7.4) into 2.5ml of PLGA in dichloromethane solution, and ultrasonically emulsify for 30s at a power of 80W to obtain a W / O emulsion . Inject the emulsion into 75ml of 0.02M phosphate buffer (pH7.4) containing 2% PVA with a micro sampler, stir at a speed of 600rpm for 1min to prepare a W / O / W emulsion, and pour the emulsion into 225ml of 0.02M phosphate buffer solution, stirred at room temperature at 300rpm for 6h, evaporated the organic solvent, centrifuged to collect the microspheres after solidification, washed three times with double distilled water, freeze-dried, and stored at low temperature.

[0038] The obtained microspheres have an average particle diameter of 95.1 μm, an encapsulation efficiency of 7.09%, and a drug loading capacity of 0.068%.

Embodiment 2

[0040] Emulsify 0.2ml of 10mg / ml DGR solution (0.02M phosphate buffer, pH 7.4) into 2.5ml of PLGA in dichloromethane solution, and ultrasonically emulsify for 30s at a power of 80W to obtain a W / O emulsion . Inject the emulsion into 75ml of 0.02M phosphate buffer (pH7.4) containing 2% PVA and 2.5% sodium chloride with a micro sampler, stir at a speed of 600rpm for 1min to prepare a W / O / W emulsion , Pour the emulsion into 225ml 0.02M phosphate buffer, stir at 300rpm at room temperature for 6h, evaporate the organic solvent, collect the microspheres by centrifugation after solidification, wash three times with double distilled water, freeze-dry, and store at low temperature.

[0041] The obtained microspheres have an average particle diameter of 93.7 μm, an encapsulation efficiency of 45.4%, and a drug loading capacity of 0.0.46%. The active DGR in the microspheres accounted for 75.0%, and the insoluble aggregates accounted for 25%.

Embodiment 3

[0043] 0.2ml of 10mg / ml DGR solution (0.02M phosphate buffer containing 2% PVA, pH 7.4) was emulsified in 2.5ml of PLGA in dichloromethane solution, and ultrasonically emulsified for 30s at a power of 80W. A W / O emulsion is obtained. Inject the emulsion into 75ml of 0.02M phosphate buffer (pH7.4) containing 2% PVA with a micro sampler, stir at a speed of 600rpm for 1min to prepare a W / O / W emulsion, and pour the emulsion into 225ml of 0.02M phosphate buffer solution, stirred at room temperature at 300rpm for 6h, evaporated the organic solvent, centrifuged to collect the microspheres after solidification, washed three times with double distilled water, freeze-dried, and stored at low temperature.

[0044] The obtained microspheres have an average particle diameter of 104.3 μm, an encapsulation efficiency of 12.5%, and a drug loading capacity of 0.119%.

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Abstract

A slow-releasing microsphere suitable for non-venous application is prepared from lactic acid-hydroxyacetic acid block copolymer (PLGA) as biodegradable high-molecular carrier and glucokinase mutant through ultrasonic or high-speed stirring for emulsifying and low-speed stirring for volatilizing solvent. Its advantages are high encapsulating rate and long release time (30 days).

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and relates to a preventive sustained-release microsphere preparation for non-intravenous administration, in particular to a sustained-release lactic acid-glycolic acid block copolymer (PLGA) containing a staphylokinase variant (staphylokinase variant) Microsphere formulations and methods for their preparation. Background technique [0002] Natural staphylokinase (staphylokinase, Sak) is a protein secreted by Staphylococcus aureus, consisting of 136 amino acids. Sak itself is not an enzyme, but forms a 1:1 complex with plasminogen (Plg) in human plasma, which is activated by trace amounts of plasmin (Plm) on the surface of blood clots to form Sak·Plm, Sak·Plm The substrate specificity of Plm in the medium changes, forming a highly efficient plasminogen activator, which activates the rest of Plg to form Plm. Plm catalyzes the degradation of fibrin, the main matrix of thrombus, thereby dissolvin...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/47A61K47/34A61P7/02
Inventor 贺进田宋后燕
Owner FUDAN UNIV
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