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Apigenin polylactic acid sustained release microsphere and preparation method thereof

A technology of slow-release microspheres and plain polylactic acid, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problems of poor water solubility, poor oral absorption, and poor fat solubility of apigenin and other problems, to achieve the effect of long release time, short cycle and high encapsulation efficiency

Active Publication Date: 2014-02-19
TAIYUAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the shortcomings of apigenin, such as poor water solubility, poor fat solubility, poor oral absorption and low encapsulation efficiency, based on the characteristics of good biocompatibility and biodegradability of polylactic acid, it is used as a matrix material to prepare apigenin polylactic acid buffer release microspheres, and add soybean lecithin with good water and fat solubility to polylactic acid, so that the preparation of microspheres can overcome its inherent disadvantages of poor solubility and poor oral absorption, greatly reduce the frequency of administration, and improve its bioavailability rate, realize a kind of apigenin polylactic acid sustained-release microspheres and preparation method thereof that the present invention will provide

Method used

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  • Apigenin polylactic acid sustained release microsphere and preparation method thereof
  • Apigenin polylactic acid sustained release microsphere and preparation method thereof
  • Apigenin polylactic acid sustained release microsphere and preparation method thereof

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Experimental program
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Embodiment 1

[0022] Implement a kind of preparation method of apigenin polylactic acid slow-release microsphere, this preparation method is carried out according to the following steps:

[0023] (1) Preparation of apigenin polylactic acid sustained-release microspheres

[0024] Dissolve 0.2 g of OH-PDLLA-OH with a molecular weight of 20000 and 0.3 g of soybean lecithin in 10 mL of dichloromethane to prepare a mixed solution with a concentration of 0.02 g / mL OH-PDLLA-OH and 0.03 g / mL of soybean lecithin; Add 0.07g of apigenin to the polylactic acid dichloromethane mixed solution, mix and ultrasonically disperse at room temperature for 5min, the mass ratio of apigenin to polylactic acid is 1:3. At a high-shear stirring speed of 800 rpm, the above suspension was slowly added dropwise into 30 mL of Pluronic with a concentration of 0.25 g / mL F-68 In aqueous solution, mixed to make O / W type emulsion. Then, at a stirring speed of 400 rpm, the emulsion was stirred for 10 min, and then transferre...

Embodiment 2

[0039] Dissolve 0.6 g of OH-PDLLA-OH with a molecular weight of 70000 and 0.9 g of soybean lecithin in 10 mL of ethyl acetate to form a mixed solution of 0.06 g / mL OH-PDLLA-OH and 0.09 g / mL of soybean lecithin; Add g apigenin to the above mixed solution of polylactic acid ethyl acetate, mix and ultrasonically disperse at room temperature for 3 minutes, the mass ratio of apigenin and polylactic acid is 1:6. At a high-shear stirring speed of 1500rpm, slowly drop the above suspension into 50mL of 0.30g / mL Pluronic F-68 In aqueous solution, mixed to make O / W type emulsion. After stirring for 10 min at a stirring speed of 400 rpm, the solvent was evaporated on a rotary evaporator under reduced pressure, and concentrated to a volume of 15 mL to obtain an emulsion dispersed with microspheres. The solution was centrifuged at 12000rpm in a high-speed centrifuge for 30 minutes. After centrifugation, the upper layer of the mixture was liquid and the lower layer was solid microspheres. T...

Embodiment 3

[0041] Dissolve 0.8 g of OH-PDLLA-OH with a molecular weight of 100,000 and 1.3 g of soybean lecithin in 10 mL of acetone to form a mixed solution of 0.08 g / mL OH-PDLLA-OH and 1.3 g / mL of soybean lecithin; 0.1 g of celery Apigenin was added to the above polylactic acid-acetone mixed solution, and after mixing, it was ultrasonically dispersed at room temperature for 2 minutes. The mass ratio of apigenin to polylactic acid was 1:8. At a high-shear stirring speed of 2000rpm, the above suspension was slowly added dropwise into 20mL of 0.35g / mL Pluronic F-68 In aqueous solution, mixed to make O / W type emulsion. Then, after stirring at a stirring speed of 400 rpm for 10 min, the emulsion was transferred to a rotary evaporator to remove the solvent under reduced pressure, and concentrated to a volume of 20 mL to obtain an emulsion dispersed with microspheres. Centrifuge the solution at 12000 rpm for 40 minutes in a high-speed centrifuge. After centrifugation, the upper layer of the ...

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Abstract

The invention discloses an apigenin polylactic acid sustained release microsphere and a preparation method of the apigenin polylactic acid sustained release microsphere. The preparation method comprises the following steps: dissolving hydroxyl-terminated racemic polylactic acid and soybean lecithin in an organic solvent; stirring the liquid, and slowly adding the apigenin mixed liquid subjected to ultrasonic treatment in an emulsifier aqueous solution to be emulsified; reducing the pressure, removing the solvent with steam, concentrating the volume; centrifuging at high speed, washing and drying the obtained mixed liquid to prepare the polylactic acid entrapped apigenin acid sustained release microsphere, wherein the microsphere particle size is 1-5 microns, the drug loading ratio is larger than 25%, the encapsulation efficiency is larger than 79%, and the sustained release time is more than 550 hours. According to the polylactic acid with good biocompatibility and biodegradability is taken as a clad material to prepare the apigenin polylactic acid sustained release microsphere, so that the microsphere is uniform in shape, smooth and adhesion-free on the surface, uniformly distributed in the particle size, and good in slow-release effect, can keep continuous release time in vitro 550 h above, conquers the defects that the drug is poor in water solubility and fat solubility, improves the oral administration availability, prolongs the drug action time and improves the drug therapeutic effect.

Description

technical field [0001] The invention relates to a medicine slow-release preparation and a preparation method thereof, in particular to an apigenin polylactic acid slow-release microsphere composed of polylactic acid-loaded apigenin and a preparation method thereof. Background technique [0002] Apigenin is a flavonoid compound widely present in a variety of fruits and vegetables, beans and tea, which has biological activities of scavenging free radicals, anti-inflammatory and anti-cancer. It mainly controls the gene expression of cancer cells, affects its protein activity to induce apoptosis, and then inhibits the growth and promotes apoptosis of various cancer cells. At the same time, it can be used as an antiviral drug for the treatment of HIV and other viral infections, an inhibitor of MAP kinase, an antioxidant, a sedative, and an antihypertensive drug. Compared with other flavonoids, such as quercetin and kaempferone, it has the characteristics of low toxicity and no m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/352A61K47/34A61K47/24A61P35/00A61P31/18A61P31/12A61P9/00A61P25/16
Inventor 王慧芳牛宝龙晏泓高向华张志强郭睿劼魏丽乔许并社
Owner TAIYUAN UNIV OF TECH
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