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Process for producing recombinant human vascular endothelial inhibitor composition sustained-release microsphere

A slow-release microsphere preparation and vascular endothelial technology, which is applied in drug combinations, microcapsules, and pharmaceutical formulations, can solve the problems of easy drug leakage, limited drug loading, and reduced yield of preparation encapsulation, so as to reduce drug administration The effect of increasing the number of times, improving compliance, and facilitating adjustment

Active Publication Date: 2011-09-14
SHANDONG SIMCERE BIO PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The volume of the inner aqueous phase limits the drug loading capacity of the microsphere preparation. At the same time, during the migration process from the inner aqueous phase to the outer phase, the drug is easily leaked, and the encapsulation yield of the preparation is reduced. At the same time, the drug is also easy to distribute on the surface of the preparation. larger burst

Method used

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  • Process for producing recombinant human vascular endothelial inhibitor composition sustained-release microsphere
  • Process for producing recombinant human vascular endothelial inhibitor composition sustained-release microsphere
  • Process for producing recombinant human vascular endothelial inhibitor composition sustained-release microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Accurately weigh 10 mg Endostar and 300 mg glucose and dissolve in 1 ml PBS buffer solution of pH 7.0, freeze-dry the solution to obtain composition powder. 4 g of PLGA (Mw=50000, lactic acid:glycolic acid=50:50) was dissolved in 20 ml of ethyl acetate to form an organic phase. Suspend the powder of the above composition in the organic phase, disperse at a high speed of 10000rpm for 20s, to form an S / O two-phase dispersion system, then pour this colostrum into 1L containing 3% polyvinyl alcohol 1788 (the degree of polymerization is about 1700, alcohol In the outer aqueous phase with a solution degree of 88%), at 20 degrees Celsius, the solvent was evaporated under normal pressure by mechanical stirring for 6 hours, and the microspheres were obtained by filtering with a 0.8 μm microporous membrane, washed three times with pure water, and dried to obtain the finished microspheres.

[0041] Accurately weigh 20 mg of the finished microsphere, dissolve it in 1 ml of dichloro...

Embodiment 2

[0044] Accurately weigh 300 mg Endostar and 10 mg mannitol and dissolve in 1 ml pH 3.0 glycine-hydrochloric acid buffer, freeze-dry the solution to obtain composition powder. 3 g of PLGA (Mw=20000, lactic acid:glycolic acid=75:25) was dissolved in 20 ml of dichloromethane to form an organic phase. Suspend the powder of the above composition in the organic phase, ultrasonicate with a 200W probe for 40 seconds to form an S / O two-phase dispersion system, and then pour the colostrum into 150ml of the external aqueous phase containing 0.02% Tween 80, at 0°C , mechanically stirred at normal pressure to evaporate the solvent for 24 hours, filtered through a 0.8 μm microporous membrane to obtain microspheres, washed three times with pure water, and dried to obtain finished microspheres.

[0045] Precisely weigh 20 mg of the finished microsphere, dissolve it in 1 ml of dichloromethane, then add 10 ml of phosphate buffered saline (PBS) with pH=7.4 to extract the drug, and use the BCA me...

Embodiment 3

[0048] Accurately weigh 200mg Endostar and 200mg PEG 4000 and dissolve in 1ml Tris buffer solution with pH 8.0, freeze-dry the solution to obtain composition powder. 600 mg of PLGA (Mw=7000, lactic acid:glycolic acid=50:50) was dissolved in 20 ml of dichloromethane to form an organic phase. Suspend the powder of the above composition in the organic phase, disperse at a high speed of 4000rpm for 60 seconds to form an S / O two-phase dispersion system, then pour this colostrum into 1L containing 1% PVA 0486 (the degree of polymerization is about 400, the degree of alcoholysis 86%) in the external water phase, start from 0°C and heat up at a rate of 1°C / min, and finally keep it at 30°C, mechanically stir and volatilize the solvent for 2 hours, and control the pressure at 20kpa throughout the process. The microspheres were obtained by filtering with a 0.8 μm microporous membrane, washed three times with pure water, and dried to obtain the finished microspheres.

[0049] Precisely w...

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Abstract

The invention relates a method for preparing a recombinant human vascular endothelial inhibin composition slow-release microsphere, which belongs to the technical field of pharmaceuticals. The constituents of the slow-release microsphere include recombinant human vascular endothelial inhibin which accounts for 1-30% in terms of weight percentage, hydrophilic substances 1-30% and lactic acid-glycolic acid polymers 69-98%. The preparation comprises the following steps: (a), adding the hydrophilic substance into a recombinant human vascular endothelial inhibin solution for free drying so as to obtain composition powder from the recombinant human vascular endothelial inhibin and the hydrophilic substance; (b), then suspending the power obtained in an organic solvent containing the lactic acid-glycolic acid polymers, which allows the power to disperse therein; (c), after dispersion, adding the solvent into a water phase containing emulsifier, stirring the solvent in a normal pressure or decompression environment to enable the solvent to be volatile and to change into microspheres, and keeping the temperature unchanged at a proper temperature as the solvent becomes volatile; and (d), subjecting the obtained microspheres to cleaning and drying so as to obtain slow-release microsphere preparations in the form of finished products. The preparation method provided by the invention can ensure that the recombinant human vascular endothelial inhibin can take a relatively stable form which effectively allows the recombinant human vascular endothelial inhibin to be encapsulated in the microspheres, thereby reducing the risk of possible degradation of the recombinant human vascular endothelial inhibin during the preparation process.

Description

technical field [0001] A preparation method for slow-release microspheres of recombinant human endostatin composition, comprising directly dispersing the composition containing hydrophilic recombinant human endostatin in an organic solvent containing lactic acid-glycolic acid polymer, volatilizing Organic solvents yield sustained-release microsphere formulations. Background technique [0002] Studies have found that during the growth and metastasis of solid tumors, angiogenesis is needed to provide nutrition. At this time, tumor cells will send some signals to promote the proliferation of blood vessels to tumor tissues. Some endogenous angiogenesis inhibitors such as Angiostatin and Endostatin can hinder The growth of blood vessels in tumor tissue makes tumor growth and metastasis stagnate (O'Relly, M.S., et al. Cell.79:315-328, 1994; O'Relly, M.S., et al. Cell.88:277 -285, 1997), Professor Folkman of Harvard Medical School in the United States proposed the theory of "starv...

Claims

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Application Information

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IPC IPC(8): A61K38/39A61K38/17A61K9/16A61K9/50A61K47/10A61K47/26A61K47/32A61K47/34A61K47/36A61P35/00
Inventor 孟博宇李玲刘春晖许向阳殷晓进
Owner SHANDONG SIMCERE BIO PHARMA CO LTD
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