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Sunitinib-plga/fe3o4 composite microspheres, a drug for treating renal cell carcinoma, and preparation method thereof

A technology of sunitinib and composite microspheres, which is applied in drug combination, drug delivery, and pharmaceutical formulations, can solve the problems of PLA high crystallinity, slow degradation speed, poor hydrophilicity, etc., and achieve good biocompatibility, Simple operation and high encapsulation efficiency

Active Publication Date: 2018-03-06
HUNAN ER KANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PLA has the disadvantages of high crystallinity and no reactive groups in the macromolecular chain, resulting in slow degradation and poor hydrophilicity.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Dissolve 1g of PLGA in 7ml of ethyl acetate, add 0.05g of Span80 and 0.02g of sodium bicarbonate in turn, stir and mix to obtain a PLGA solution; add 0.10g of magnetic nano-Fe 3 o 4 The particles were added to the PLGA solution, stirred and mixed, and then ultrasonically treated for 12 minutes under the condition of ultrasonic power of 150w to obtain a composite solution;

[0027] (2) Slowly add 0.12 g of sunitinib to 120 ml of an aqueous solution of sodium carboxymethylcellulose with a concentration of 1.2% by mass, stir and mix to obtain solution 1;

[0028] (3) Slowly disperse the composite solution into the solution 1 obtained in step (2) under stirring conditions, the stirring speed is 200r / min, and the stirring time is 18h, to obtain an oil-in-water emulsion;

[0029] (4) The emulsion obtained in step (3) was distilled under reduced pressure at room temperature to completely volatilize the ethyl acetate, and the obtained solid was vacuum-dried at 25°C for 32 ...

Embodiment 2

[0031] (1) Dissolve 1g of PLGA in 13ml of acetone, add 0.09g of glyceryl monostearate and 0.18g of toluene in turn, stir and mix to obtain a PLGA solution; add 0.25g of magnetic nano-Fe 3 o 4 The particles were added to the PLGA solution, stirred and mixed, and then ultrasonically treated for 10.5min under the condition of ultrasonic power of 200w to obtain a composite solution;

[0032] (2) Slowly add 0.16 g of sunitinib to 150 ml of an aqueous solution of sodium carboxymethylcellulose with a concentration of 1.2% by mass, stir and mix to obtain solution 1;

[0033] (3) Slowly disperse the composite solution into the solution 1 obtained in step (2) under stirring conditions, the stirring speed is 230r / min, and the stirring time is 15h, to obtain an oil-in-water emulsion;

[0034] (4) The emulsion obtained in step (3) was distilled under reduced pressure at room temperature to completely volatilize the acetone, and the obtained solid was vacuum-dried at 27°C for 29 hours to o...

Embodiment 3

[0036] (1) Dissolve 1g of PLGA in 19ml of dichloromethane, add 0.13g of cetyl cetyl ester and 0.34g of water in turn, stir and mix to obtain a PLGA solution; add 0.38g of magnetic nano-Fe 3 o 4 The particles were added to the PLGA solution, stirred and mixed, and then ultrasonically treated for 9.5 minutes under the condition of ultrasonic power of 250w to obtain a composite solution;

[0037] (2) Slowly add 0.20 g of sunitinib to 170 ml of an aqueous solution of sodium carboxymethyl cellulose with a concentration of 1.2% by mass;

[0038] (3) Slowly disperse the composite solution into the solution 1 obtained in step (2) under stirring conditions, the stirring speed is 265r / min, and the stirring time is 13h, to obtain an oil-in-water emulsion;

[0039] (4) The emulsion obtained in step (3) was distilled under reduced pressure at room temperature to completely volatilize the dichloromethane in it, and the obtained solid was vacuum-dried at 28°C for 26 hours to obtain sunitini...

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Abstract

The invention discloses sunitinib-PLGA / Fe3O4 composite microspheres, a drug for treating renal cell carcinoma, and a preparation method thereof. The method is to dissolve PLGA in an organic solvent, add a surfactant and a pore-forming agent, stir and mix, and then add magnetic nano-Fe3O4 particles to prepare a composite solution; slowly add sunitinib to 120-200ml mass percentage concentration of 1.2% sodium carboxymethyl cellulose aqueous solution, stirred and mixed to obtain solution 1; then the composite solution was slowly dispersed into solution 1, stirred to fully volatilize the organic solvent, and the solid was vacuum-dried at 25-30°C for 24~ After 32 hours, the sunitinib-PLGA / Fe3O4 composite microspheres were obtained. The sunitinib-PLGA / Fe3O4 composite microspheres prepared by the invention have regular apertures and high encapsulation efficiency, and have clinical application prospects in the aspects of targeted killing of cancer cells and cancer treatment.

Description

technical field [0001] The invention relates to a preparation technology of a drug sustained-release dosage form or a drug sustained-release carrier, in particular to a sunitinib-PLGA / Fe3O4 composite microsphere and its preparation for treating renal cell carcinoma. technical background [0002] Sunitinib is a new type of oral inhibitor for multiple kinases, which can block the pathways of vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF), and has a strong anti-angiogenic effect. It can inhibit the proliferation of tumor cells and is used for the treatment of gastrointestinal stromal cell tumors that are intolerant to imatinib mesylate or whose condition has deteriorated. Sunitinib is a small molecule indolinone compound, its chemical name is (Z)-N-[2-(diethylamino)ethyl-5-[(5-fluoro-2-oxo-1,2 -Dihydro-3H-indole-3-ylidene)methyl]-2,4-dimethyl-3-carbamoyl-1H-pyrrole malate, molecular formula C 22 h 27 FN 4 o 2 ·C 4 h 6 o 5 , the molec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/404A61K47/34A61K47/02A61P35/00
CPCA61K9/0009A61K9/501A61K9/5031A61K31/404
Inventor 帅放文王向峰章家伟
Owner HUNAN ER KANG PHARMA