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Recombined human vascellum esoderma inhibin durative action preparation, preparation method and application thereof

A technology of vascular endothelium and inhibin, which is applied in the field of medicine, can solve the problems of patients' pain, achieve the effects of reducing pain, high encapsulation rate, and reducing burst release

Active Publication Date: 2012-03-28
SHANDONG SIMCERE BIO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such frequent injections, on the one hand, bring great pain to patients physically, and on the other hand, they also bring huge economic pressure to patients psychologically.

Method used

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  • Recombined human vascellum esoderma inhibin durative action preparation, preparation method and application thereof
  • Recombined human vascellum esoderma inhibin durative action preparation, preparation method and application thereof
  • Recombined human vascellum esoderma inhibin durative action preparation, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Dissolve 100mg PLGA (Mw=15000, 50:50) in 1ml 1-methyl-2-pyrrolidone (10% concentration), then add 0.1ml 100mg / ml Endostar aqueous solution (the weight ratio of PLGA to Endostar is 10:1 ), mixed with a shaker for 30 minutes, and the mixed solution was added to a dialysis bag with a molecular weight cut-off of 30,000 and a diameter of 1 cm with a syringe, and the two ends were tightened with clamps. Then place the dialysis bag in a beaker containing 10 ml of phosphate buffer (0.1 mol / L, pH 7.0), and keep stirring with a magnetic stirrer. The solvent is rapidly dialyzed into the beaker and the PLGA solidifies to form the implanted pump. Take 1ml of the buffer solution in the beaker every day, and replenish the same volume of fresh phosphate buffer solution at the same time. The content of Endostar in the samples was determined by HPLC. The cumulative release percentage of the drug was plotted against the release time. 18.8% was released on day 1, 55.5% was released on d...

Embodiment 2

[0047] Dissolve 100mg of PLGA (Mw=40500, 50:50) in 1ml of 1-methyl-2-pyrrolidone (concentration: 10%), then add 0.1ml of 200mg / ml Endostar aqueous solution (the weight ratio of PLGA to Endostar is 10: 2), all the other steps are with embodiment 1. The cumulative release percentage of the drug was plotted against the release time. 18.1% was released on day 1, 21.5% was released on day 7, 51.0% was released on day 14, and 89.1% was released on day 28.

Embodiment 3

[0049] Dissolve 100mg of PLGA (Mw=40500, 75:25) in 1ml of 1-methyl-2-pyrrolidone (concentration: 10%), then add 0.05ml of 100mg / ml Endostar aqueous solution (the weight ratio of PLGA to Endostar is 20: 1), all the other steps are with embodiment 1. The cumulative release percentage of the drug was plotted against the release time. 7.6% was released on day 1, 11.5% on day 7, 23.0% on day 14, and 54.1% on day 28.

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Abstract

The invention relates to the field of medical technology and discloses a long-acting preparation of lactic-glycolic acid copolymer (PLGA) for the recombination of endostatin of vein and the application to preparing a drug for treating tumor. The invention uses four methods of implanting a pump in vivo, implanting a microsphere in vivo, a W / O / W solvent volatilization method and a W / O / O solvent volatilization method to prepare the long-acting preparation. The sustained-release time of the long-acting preparation prepared is 7 to 28 days in accordance with the needs.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a slow-release long-acting preparation of recombinant human endostatin (rhEndostatin), a preparation method and application thereof. Background technique [0002] Angiogenesis plays an important role in the growth and metastasis of solid tumors. In order to stimulate angiogenesis, tumor cells will upregulate a series of angiogenic factors, such as: aFGF, bFGF and VEGF. At the same time, some angiogenesis inhibitors will also be produced. The opening and closing of the angiogenic phenotype in the tissue will depend on the dynamic balance between angiogenesis stimulators and inhibitors in the local area of ​​the tissue (Folkman, J.Nat.MED.1:27-31, 1995; Hanahan, D., et al. Cell. 86:353-364, 1996). Studies have found that endogenous angiogenesis inhibitors, such as: angiotensin (Angiostatin), vascular endostatin (Endostatin), etc., can inhibit the growth of tumors in mice (O'Relly...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K38/17A61K47/34A61P35/00
Inventor 胡一桥许向阳吴锦慧刘春晖陈英杰江征殷晓进
Owner SHANDONG SIMCERE BIO PHARMA CO LTD
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