Glycyrrhetinic acid solid lipid nanoparticles and preparation method for same

A technology of solid lipid nanometer and glycyrrhetinic acid, which is applied in liposome delivery, pharmaceutical formula, oil/fat/wax non-effective ingredients, etc. It can solve the problems of large individual differences, low bioavailability, poor absorption, etc. , to achieve the effect of uniform particle size, good physiological compatibility and easy disinfection

Inactive Publication Date: 2012-06-27
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since glycyrrhetinic acid is a water-insoluble compound, it has poor absorption in the body after oral administration, low bioavailability, and large individual differences

Method used

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  • Glycyrrhetinic acid solid lipid nanoparticles and preparation method for same
  • Glycyrrhetinic acid solid lipid nanoparticles and preparation method for same
  • Glycyrrhetinic acid solid lipid nanoparticles and preparation method for same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Formula mass percentage (%)

[0036] Glycyrrhetinic acid 5

[0037] Yolk Lecithin 40

[0038] Stearic acid 30

[0039] mPEG-DSPE 25

[0040] Weigh glycyrrhetinic acid, egg yolk lecithin, stearic acid and mPEG-DSPE, dissolve them in 2ml of ethanol, and ultrasonically dissolve them to form a transparent solution, pour them into 50ml of distilled water at 50°C, keep stirring for 30 minutes, and place in a rotating Evaporate under reduced pressure on the evaporator to further volatilize the organic solvent, then circulate and homogenize for 3-5 times through a high-pressure homogenizer, let it cool at room temperature, and pass through a 0.45 μm filter membrane to obtain a colloidal solution of glycyrrhetinic acid solid lipid nanoparticles , the colloidal solution is translucent, blue opalescent. The drug content in the drug was determined by a reversed-phase high-performance liquid chromatography column. Column selection ODS C 18 Column (4.6*250mm, 5μm), the mobile p...

Embodiment 2

[0042] Formula mass percentage (%)

[0043] Glycyrrhetinic acid 1

[0044] Yolk Lecithin 80

[0045] Oleic acid 9

[0046] PEGCHS 10

[0047] Weigh glycyrrhetinic acid, egg yolk lecithin, oleic acid and mPEG-DSPE into a 50ml round-bottomed flask, add 2ml chloroform to dissolve them, place a 40°C water bath on a rotary evaporator to recover the organic solvent under reduced pressure, and form A layer of film was further placed in a desiccator under reduced pressure to completely remove the organic solvent. Inject pH 8 phosphate buffer solution for hydration for 1 hour, place it in a probe ultrasonic breaker and sonicate for 10-30 minutes, pass through a 0.45 μm filter membrane, dilute the resulting liposome solution to volume, add 10% (g / ml) sucrose, and pass through Freeze-dry to obtain glycyrrhetinic acid solid lipid nanoparticle freeze-dried powder. After reconstitution, take 0.2ml to pass through the agarose CL-4B gel column, use pH 7.4 phosphate buffer as the eluent, ...

Embodiment 3

[0049] Formula mass percentage (%)

[0050] Glycyrrhetinic acid 4

[0051] Soy Lecithin 46

[0052] Glyceryl Palmitate 5

[0053] Poloxamer 50

[0054] Weigh glycyrrhetinic acid, egg yolk lecithin, glyceryl palmitate, and poloxamer, melt and mix at 60°C, inject water at 60°C into the melt under stirring, continue stirring for 30 minutes, and circulate through a high-pressure homogenizer After massaging for 3-5 times, let cool at room temperature, pass through a 0.45 μm filter membrane, stabilize the volume of solid lipid nanoparticles obtained by ultrasound, add 5% (g / ml) mannitol, and freeze-dry to obtain glycyrrhetinic acid solid lipid nanoparticles. granules of freeze-dried powder. After adding distilled water to redissolve, take 0.2ml to pass through the agarose CL-4B gel column, use pH 7.4 phosphate buffer as the eluent, collect the effluent in an amount of 1ml per test tube, and calculate the encapsulation according to the elution curve The rate reached 98%. The pa...

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Abstract

The invention relates to glycyrrhetinic acid solid lipid nanoparticles and a preparation method for the same, belonging to the field of medicinal preparation. The main ingredients of the glycyrrhetinic acid solid lipid nanoparticles disclosed by the invention comprise active raw material glycyrrhetinic acid, medicinal phospholipid, a lipid material and a surfactant. The glycyrrhetinic acid solid lipid nanoparticle solution and the freeze-dried powder injection thereof prepared by the preparation method disclosed by the invention are small in particle diameter, high in entrapment efficiency, good in stability and capable of being used for a plurality of administration routes such as oral administration and injection administration. The glycyrrhetinic acid solid lipid nanoparticles disclosed by the invention can reduce dosage, enhance curative effect and reduce the toxic and side effects of medicine, as well as are suitable for treating a plurality of diseases such as hepatitis, liver cancer, lung cancer, ovarian cancer, gastritis, gastric cancer, leukaemia and aids.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to glycyrrhetinic acid solid lipid nanoparticles and a preparation method thereof. Background technique [0002] Glycyrrhetinic acid (Glycyrrhetinic acid, GA) is derived from the hydrolysis of glycyrrhizic acid, the main component of licorice, and is also an active metabolite of glycyrrhizic acid in the body. It is a pentacyclic triterpenoid compound. GA is also known as glycyrrhetinic acid, and its molecular formula is C 30 h 46 o 4 , white needle crystal, melting point 289~291℃. The structure is as follows: [0003] [0004] Modern studies have shown that glycyrrhetinic acid has anti-inflammatory, anti-ulcer, anti-allergic, anti-viral, blood lipid-lowering, cough-relieving, asthma-relieving, and pain-relieving effects, as well as anti-tumor hyperplasia [Liu Bin, Qi Yun. Advances in pharmacological research of glycyrrhizic acid and glycyrrhet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/56A61K47/24A61K47/28A61K47/34A61K47/44A61P1/16A61P31/14A61P31/18A61P31/20A61P35/00A61P35/02
Inventor 周小菊王炯胡先明
Owner WUHAN UNIV
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