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Sunitinib malate liposome and preparation method thereof

A technology of sunitinib malate lipid and liposome preparation, which is applied in the field of medicine to achieve the effect of no significant change

Inactive Publication Date: 2012-06-06
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

That is, the ethanol added in the preparation process will affect the liposome membrane structure. Too much ethanol will easily cause the aggregation of liposomes, the fusion of bilayers and the leakage of drugs, thereby affecting the encapsulation efficiency of liposomes. , particle size and stability

Method used

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  • Sunitinib malate liposome and preparation method thereof
  • Sunitinib malate liposome and preparation method thereof
  • Sunitinib malate liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Hydrogenated soybean lecithin (HSPC) 3g

[0012] Cholesterol (CH) 1g

[0013] mPEG 2000 -DSPE 0.75g

[0014] Weigh each lipid compound in the prescription, stir and dissolve with an appropriate amount of absolute ethanol in a 65°C water bath, evaporate the ethanol, and add a certain concentration of ammonium sulfate ((NH 4 ) 2 SO 4 ) solution, stirred in a water bath at 65°C for 20 min to obtain the primary blank liposome. Sonicate the primary product probe for 8 min (200 w×2 min, 400 w×6 min), and pass through 0.8, 0.45, 0.22 μm microporous membranes in turn to obtain a blank liposome suspension, and the final phospholipid mass concentration 50 mg·mL -1 .

[0015] 2 General scheme 2

[0016] Blank liposome prescription

[0017] Hydrogenated soybean lecithin (HSPC) 3g

[0018] Cholesterol (CH) 1g

[0019] mPEG 2000 -DSPE 0.75g

[0020] Weigh each lipid compound in the prescription, stir and dissolve with an appropriate amount of absolute ethanol in a 70°C w...

Embodiment 2

[0031] Take an appropriate amount of gradient liposome and SU solution (5.0 mg·mL -1 ) and incubate at a certain temperature for a certain period of time to obtain SU-L.

[0032] Determination of SU-L Encapsulation Efficiency

[0033] The encapsulation efficiency of SU-L was determined by the cation exchange resin method, and the specific operation was as follows: Precisely pipette 0.1 mL of SU-L into a 10.0 mL volumetric flask, add 1.6 mL of distilled water, and make a volume fraction of 90% isopropanol solution (containing 0.75 mol·L -1 HCl) demulsification and constant volume, shake well, measure absorbance A at 430 nm wavelength 0 (total drug absorption). Another precision pipette 0.1 mL SU-L, placed in the center of the top surface of the cation exchange resin column, 2000 r min -1 Centrifuge for 4 min, then add 400 μL of distilled water to the top of the column, 2000 r min -1 Centrifuge for 4 min, repeat 4 times, and combine eluents. The eluate was transferred to a...

Embodiment 3

[0062] Cholesterol (CH) 1g

[0063] Macrogol 1000 Cholesterol Hemisuccinate (mPEG1000-CHEMS) 0.5g

[0064] Weigh the prescription quantities of DSPC, CH, mPEG1000-CHEMS, and use 2.5%, 5.0%, 10%, 15%, 20%, 25%, 30% and 40% (volume ratio of ethanol to hydration medium) of absolute ethanol respectively Dissolve the membrane material, add 150 mmol·L -1 of (NH 4 ) 2 SO 4 solution, stirred in a water bath at 65°C for 20 min to obtain the primary blank liposome, and the final phospholipid mass concentration was 50 mg·mL -1 . Sonicate the primary product probe for 8 min (200 w×2 min, 400 w×6 min), then pass through the microporous membranes of 0.8, 0.45, and 0.22 μm in sequence to obtain a blank liposome suspension, which was measured by laser particle size The particle size of each liposome was measured by an instrument, and the results showed that when the residual ethanol content did not exceed 10% (v / v), the liposome particle size did not change significantly between 108.2 a...

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Abstract

The invention discloses sunitinib malate liposome and a preparation method thereof, belonging to the technical field of medicines. A prescription for the sunitinib malate liposome in the invention is as follows: drugs and lipid substances used for constructing a bilayer membrane of the liposome are prepared by using an improved ethanol injection method. In the invention, influence of the content of ethanol in the preparation prescription on an entrapment rate, particle size distribution, stability and an antineoplastic effect of the liposome is also investigated. According to results of investigation, liposome which is obtained through drug loaded preparation by using a gradient method has an entrapment rate greater than 90%; when the content of ethanol is controlled to be no more than 10%, related parameters of the liposome hardly change, thereby providing reference for control of the content of ethanol in preparation and industrial production of the sunitinib liposome.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to sunitinib malate liposomes and a preparation method thereof, in particular to the control of ethanol content in the liposome preparation process, ensuring that the residual ethanol in the preparation process has no significant effect on liposome properties Influence. Background technique: [0002] Sunitinib and its malate (Sunitinib malate, Sutent, SU11248, SU) are novel multi-target tyrosine kinase receptor inhibitors, which have inhibitory effects on various receptor tyrosine kinases (TKIs). It mainly includes platelet-derived growth factor receptor β (PDGFRβ), vascular endothelial growth factor receptor 1, 2, 3 (VEGFR1, 2, 3) and stem cell factor receptor (c-Kit). This drug has obvious anti-tumor activity on a variety of solid tumors. and / or) Good results have been achieved in clinical trials. In 2006, Sutent, a product of Pfizer, which was approved by the FDA for t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/404A61K47/24A61K47/28A61K47/34A61P35/00
Inventor 邓意辉张艳晶
Owner SHENYANG PHARMA UNIVERSITY
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