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Injection-use recombinant human Endostatin porous sustained-release microsphere and preparation method thereof

A technology of vascular endothelium and slow-release microspheres, which is applied to medical preparations containing non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., to achieve the effects of reducing the number of administrations, facilitating adjustments, and improving compliance

Active Publication Date: 2009-09-23
JIANGSU SIMCERE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the large molecular weight of Endostar (21kD), polymers may be formed during the preparation of microspheres; after in vivo injection, it is difficult for the drug inside the microspheres to maintain release after burst release, because the degradation rate of the surface of the microspheres is lower than that of the internal materials. The speed of degradation can only be released completely when the material is severely degraded and disintegrated in the late release period, which is very unfavorable for maintaining a constant blood drug concentration in the body

Method used

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  • Injection-use recombinant human Endostatin porous sustained-release microsphere and preparation method thereof
  • Injection-use recombinant human Endostatin porous sustained-release microsphere and preparation method thereof
  • Injection-use recombinant human Endostatin porous sustained-release microsphere and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0039]

[0040] Recipe 1 and Recipe 2 use the same process: Precisely weigh Endostar and dissolve it in 80ml of pH 8.0 phosphate buffer to form an aqueous phase. PLGA and PEG 4000 were dissolved in 240 ml of dichloromethane to form the organic phase. Mix the above two phases, disperse at a high speed of 10,000rpm in a homogenizer for 5 minutes, and form a water-in-oil emulsion; then pour this colostrum into 3.2L containing 3% polyvinyl alcohol 1788 (the degree of polymerization is about 1700, and the degree of alcoholysis is 88%) ) in the outer aqueous phase, at 20 degrees Celsius, mechanically stirred at atmospheric pressure for 2 hours, filtered through a 0.8 μm microporous membrane to obtain microspheres, washed three times with pure water, and freeze-dried for 24 hours to obtain finished microspheres.

[0041] Accurately weigh 20 mg of two batches of finished microspheres, dissolve them in 1 ml of dichloromethane, then add 10 ml of phosphate buffered saline (PBS) with a...

Embodiment 2

[0045]

[0046] Accurately weighed Endostar and different porogens were dissolved in 100ml pH 3.0 glycine-hydrochloric acid buffer to obtain the aqueous phase. PLGA was dissolved in 158 ml of dichloromethane to form the organic phase. Mix the two phases, ultrasonicate with a 200W probe for 10 seconds to form a water-in-oil emulsion, then pour this colostrum into 1.032L of the external water phase containing 0.1% tween 80, and mechanically stir at 0°C for 24 hours at normal pressure to evaporate the solvent , using a 0.8 μm microporous membrane to filter to obtain microspheres, wash with pure water three times, and vacuum-dry for 5 days to obtain finished microspheres.

[0047] Precisely weigh 20 mg of the finished microsphere, measure the protein content in the microsphere according to the method in Example 1, and calculate the drug loading and encapsulation yield, wherein the drug loading of prescription 3 is 1.80%, and the encapsulation yield is 90.00%; The drug loading ...

Embodiment 3

[0050]

[0051] Accurately weigh Endostar and dissolve it in 100ml of tris buffer solution with pH 5.0 to obtain the aqueous phase. MCT and PLGA were dissolved in 1.9 L of mixed solvent (volume ratio dichloromethane:ethyl acetate=1:1) to form an organic phase. Mix the above two phases, and disperse at a high speed of 4000rpm in a homogenizer for 10 minutes to form a water-in-oil emulsion, and then pour this colostrum into a 20L container containing 1% PVA 0486 (the degree of polymerization is about 400, and the degree of alcoholysis is 86%). In the water phase, the temperature was raised from 0°C at a rate of 1°C / min, and finally kept at 30°C, mechanically stirred to evaporate the solvent for 6 hours, and the pressure was controlled at 20kpa during the whole process. The microspheres were obtained by filtering with a 0.8 μm microporous membrane, washed three times with pure water, and dried in vacuum for 2 hours to obtain the finished microspheres.

[0052] Precisely weigh...

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Abstract

The invention relates to a recombinant human Endostatin porous sustained-release microsphere for injection, and a preparation method thereof, in particular to an injection-use porous sustained-release microsphere which takes a biodegradable polymer of lactic acid and hydroxyacetic acid as a matrix and comprises recombinant human Endostatin and a pore-forming agent, and a preparation method thereof.

Description

technical field [0001] The invention relates to a porous slow-release microsphere of recombinant human endostatin for injection and a preparation method thereof, in particular to a biodegradable lactic acid-glycolic acid polymer as a matrix, including recombinant human endostatin and porogen Porous sustained-release microspheres for injection and preparation method thereof. Background technique [0002] Professor Folkman of Harvard Medical School in the United States put forward the theory that "tumor growth depends on angiogenesis" in the 1960s, that is, during the growth and metastasis of solid tumors, angiogenesis plays a vital role. At this time, tumor cells will emit some Cytokines (aFGF, bFGF, VEGF, etc.) that promote the proliferation of blood vessels to tumor tissue. Another study found that some endogenous angiogenesis inhibitors, such as Angiostatin and Endostatin, can hinder the growth of blood vessels in tumor tissues, and stagnate the growth and metastasis of t...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/17A61K47/34A61P35/00
Inventor 孟博宇李玲许向阳
Owner JIANGSU SIMCERE PHARMA
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