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Renal cell carcinoma treatment medicine sunitinib-PLGA/Fe3O4 composite microsphere and preparation method thereof

A technology for sunitinib and therapeutic drugs, which is applied in the field of preparation of drug sustained-release dosage forms or drug sustained-release carriers, can solve the problems of slow degradation rate, poor hydrophilicity and high crystallinity of PLA, and achieves simple operation and high encapsulation. rate, good biocompatibility

Active Publication Date: 2016-03-30
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 PLGA in 7ml ethyl acetate, add 0.05g Span80 and 0.02g sodium bicarbonate in turn, stir and mix to obtain a PLGA solution; add 0.10g magnetic nano Fe 3 O 4 The particles are added to the PLGA solution, and after stirring and mixing, under the condition of ultrasonic power of 150w, ultrasonic treatment is carried out for 12min to obtain a composite solution;

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

[0028] (3) slowly dispersing 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 normal temperature, so that the ethyl acetate in it was completely volatilized, and the obtained solid was vacuum-dried at a...

Embodiment 2

[0031] (1) Dissolve 1g PLGA in 13ml acetone, add 0.09g glycerol monostearate and 0.18g toluene in turn, stir and mix to obtain a PLGA solution; add 0.25g magnetic nano Fe 3 O 4 The particles are added to the PLGA solution, and after stirring and mixing, under the condition of ultrasonic power of 200w, ultrasonic treatment is carried out for 10.5min to obtain a composite solution;

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

[0033] (3) slowly dispersing 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 normal temperature, so that the acetone in it was completely volatilized, and the obtained solid was vacuum-dried at ...

Embodiment 3

[0036] (1) Dissolve 1 g of PLGA in 19 ml of dichloromethane, add 0.13 g of hexadecyl hexadecanoate and 0.34 g of water in turn, stir and mix to obtain a PLGA solution; add 0.38 g of magnetic nano Fe 3 O 4 The particles were added to the PLGA solution, and after stirring and mixing, under the condition of ultrasonic power of 250w, ultrasonic treatment was carried out for 9.5min to obtain a composite solution;

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

[0038] (3) slowly dispersing 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 normal temperature, so that the dichloromethane in it was completely volatilized, and the obtained solid was vacuum-dried at a te...

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Abstract

The invention discloses a renal cell carcinoma treatment medicine sunitinib-PLGA / Fe3O4 composite microsphere and a preparation method thereof. The method comprises the following steps: dissolving PLGA in an organic solvent, adding a surfactant and a pore forming agent, uniformly stirring and mixing, and adding magnetic nano-Fe3O4 particles to prepare a compound solution; slowly adding sunitinib into 120-200ml of a sodium carboxymethyl cellulose aqueous solution having a concentration of 1.2 percent by mass, and uniformly stirring and mixing to prepare a solution 1; and slowly dispersing the compound solution into the solution 1, stirring to sufficiently volatize the organic solvent, and drying the solid at 25-30 DEG C in vacuum for 24-32 hours to prepare the sunitinib-PLGA / Fe3O4 composite microsphere. The sunitinib-PLGA / Fe3O4 composite microsphere has a regular pore diameter and relatively high entrapment efficiency, and has a clinical application prospect in the target cancer cell killing and cancer treatment aspects.

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 renal cell carcinoma therapeutic drug sunitinib-PLGA / Fe3O4 composite microsphere and its preparation. technical background [0002] Sunitinib, a novel oral inhibitor of multiple kinases, can block vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) pathways, 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 disease has deteriorated. Sunitinib is a small molecule indolinone compound whose 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, the molecular formula is C 22 H 27 FN 4 O 2 ·C 4 H 6 O 5 , the molecular weight ...

Claims

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Application Information

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Patent Type & Authority Applications(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
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