Icaritin liposome oral preparation, and preparation method thereof

An acridine fat and oral preparation technology, applied in nutritional preparations, pharmaceutical preparations, and food fields, can solve problems such as destruction and high oil intake, and achieve the effects of improving absorption, improving bioavailability, and good physical stability.

Inactive Publication Date: 2017-07-28
CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention discloses an oral preparation of alcradine liposome and a preparation method thereof. On the one hand, the dosage form overcomes the problem of high fat intake in the existing oil suspension preparation of alcladinine during ingestion, and on the other hand On the one hand, it also solves the problem that Alcoradine is directly destroyed by the gastric juice environment after it is directly orally taken into the digestive system. Application in Oral Preparations

Method used

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  • Icaritin liposome oral preparation, and preparation method thereof
  • Icaritin liposome oral preparation, and preparation method thereof
  • Icaritin liposome oral preparation, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035]Weigh 100mg of alcradine, 1g of soybean lecithin, 100mg of cholesterol, vortex and shake with 20mL ether and fully dissolve to form an organic phase; dissolve 200mg of Tween-80 in 100mL of phosphate buffer solution (0.01mol / L, pH 7.4) and fully dissolved to form a water phase; the organic phase was removed by rotary evaporation under reduced pressure to remove ether, and then the evaporated lipid film was hydrated with a water phase preheated to 50 ° C, and it was removed from the It was eluted in a round bottom flask to form a thick Alcoradine liposome suspension, and was emulsified in an ice bath with an ultrasonic homogenizer, with an ultrasonic power of 400W and an ultrasonic time of 10min, to obtain an oral preparation of Alcoradine liposome.

[0036] The entrapment rate of the oral liposome preparation of Alcoradine prepared in this example was 77.7%, the average particle size was 249.6±2.7nm, and the Zeta potential was -43.3±2.2mV.

[0037] figure 1 and figure ...

Embodiment 2

[0039] Weigh 1g of Alcradine, 5g of soybean lecithin, and 500mg of cholesterol, vortex and shake with 50mL of ether and fully dissolve to form an organic phase; dissolve 200mg of Tween-80 in 100mL of phosphate buffer solution (0.01mol / L, pH 7.4) and fully dissolved to form a water phase; the organic phase was removed by rotary evaporation under reduced pressure to remove ether, and then the evaporated lipid film was hydrated with a water phase preheated to 50 ° C, and it was removed from the circle with a water-bath ultrasonic cleaner. Elute in the bottom flask to form a thick Alcoradine liposome suspension, and emulsify in an ice bath with an ultrasonic homogenizer, with an ultrasonic power of 400W and an ultrasonic time of 10min, to obtain an oral preparation of Alcoradine liposome.

[0040] The entrapment rate of the oral liposome preparation of Alcoradine prepared in this example was 84.8%, the average particle size was 284.3±26.3nm, and the Zeta potential was -38.3±1.2mV. ...

Embodiment 3

[0043] Weigh 1.2g of Acradine, 12g of soybean lecithin, and 1.2g of cholesterol, vortex and shake with 30mL ether and fully dissolve to form an organic phase; dissolve 200mg of Tween-80 in 100mL of phosphate buffered saline , pH 7.4) and fully dissolved to form an aqueous phase; the organic phase was evaporated under reduced pressure to remove ether, and then the evaporated lipid film was hydrated with an aqueous phase preheated to 50 ° C, and it was washed with a water-bath ultrasonic cleaner. Elute from the round-bottomed flask to form a thick Alcoradine liposome suspension, and emulsify through a high-pressure homogenizer, the homogenization pressure is 50MPa, and circulate homogeneously for 2 times to obtain the Alcoradine liposome oral preparation .

[0044] The entrapment rate of the oral liposome preparation of Alcoradine prepared in this example was 85.2%, the average particle size was 249.1±2.1nm, and the Zeta potential was -46±2.4mV.

[0045] The oral preparation of...

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Abstract

The invention discloses an icaritin liposome oral preparation, and a preparation method thereof. According to the preparation method, the icaritin liposome oral preparation is prepared via thin film dispersion combined ice bath ultrasonic treatment or high pressure homogenization emulsification treatment. 100ml of the icaritin liposome oral preparation contains, 0.2 to 2.4% of icaritin, 0.4 to 12% of lecithin, 0.1 to 1.2% of a film structure conditioning agent, and 0.2% of a nonionic surfactant. The preparation method is capable of solving problems in the prior art via conventional liposome preparation technology that the dissolvability of icaritin in water phase systems is poor, and degradation is easily caused under influences of the external environment; and stability of icaritin in gastrointestinal digestion process is increased. The obtained icaritin liposome oral preparation is regular spherical vesicles; embedding rate is 70% or higher; particle size ranges from 100 to 300nm; particle size distribution is uniform; the preparation method is simple; liposome quality is increased greatly; and the preparation method is suitable for large-scale industrialized production.

Description

technical field [0001] The invention belongs to the technical fields of food, nutritional preparations and pharmaceutical preparations, and specifically provides a liposome oral preparation and a preparation method thereof, in particular relates to an alcradine liposome oral preparation and a preparation method thereof. Background technique [0002] Acradine, also known as icariin or icariin, is a derivative monomer obtained from icariin extracted from the dry leaves of the traditional Chinese medicine Epimedium Herba through enzymatic conversion. The specific structural formula is as follows: 1) as shown: [0003] [0004] In the Chinese patent applications with application numbers 201510127652.6 and 201510126477.9, the use of Alcradine in the preparation of drugs for the treatment of liver cancer related to GP130 and GP80 is mentioned. In the Chinese patent application with the application number 201410472236.5, the use of Alcladine in the preparation of drugs for inhi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/352A61K47/28A61K47/24A61P35/00
CPCA61K9/0053A61K9/127A61K31/352A61K47/24A61K47/28
Inventor 袁芳邰克东何晓叶高彦祥毛立科
Owner CHINA AGRI UNIV
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