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Rhein phospholipid complex as well as preparation method and application thereof, rhein phospholipid complex long-circulating liposome and preparation method of liposome

A technology of rhein phospholipids and complexes, which is applied in liposome delivery, drug combination, drug delivery, etc., can solve the problems of limiting the drug loading of phospholipid compounds, achieve good application prospects, easy large-scale production, and low production cost Effect

Pending Publication Date: 2020-05-08
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, the modification of chemical bonds also greatly limits the drug loading capacity of phospholipid compounds

Method used

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  • Rhein phospholipid complex as well as preparation method and application thereof, rhein phospholipid complex long-circulating liposome and preparation method of liposome
  • Rhein phospholipid complex as well as preparation method and application thereof, rhein phospholipid complex long-circulating liposome and preparation method of liposome
  • Rhein phospholipid complex as well as preparation method and application thereof, rhein phospholipid complex long-circulating liposome and preparation method of liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Take 0.3g of rhein and 0.6g of soybean lecithin, add 50ml of absolute ethanol, stir and react at 45°C for 24h to obtain a clear solution, remove the ethanol under reduced pressure at 50°C, collect the solids and dry them in vacuum for 12h, then pulverize them to obtain rhein phospholipids Complex.

[0036] Dissolve 0.9 g of the obtained rhein phospholipid complex in 50 mL of chloroform, stir and dissolve until transparent oily liquid, and obtain the rhein phospholipid complex solution; then add 1.8 g of soybean lecithin, 1.2 g of cholesterol, and 0.18 g of distearoyl Phosphatidylethanolamine-polyethylene glycol, stirred until dissolved to form a clear oily solution. At a temperature of 35°C, remove the solvent by rotary evaporation under reduced pressure to form a thin film, then add 10mL of deionized water, hydrate under the action of water bath ultrasonic (80w, 3min), and then probe ultrasonically (200w, 2min, set to work for 3s , an interval of 7s, and a total of 12...

Embodiment 2

[0038] Take 0.2g of rhein and 0.8g of egg yolk lecithin, add 40ml of dichloromethane, stir and reflux at 40°C for 10 hours to obtain a clear solution, remove the dichloromethane under reduced pressure at 50°C, collect the solids, dry them in vacuum for 12 hours, and crush them to obtain Rhein Phospholipid Complex.

[0039] Dissolve 1 g of the obtained rhein phospholipid complex in 50 mL of dichloromethane, stir and dissolve until transparent oily liquid, and obtain the rhein phospholipid complex solution; then add 1.2 g of lecithin, 1 g of cholesterol, and 0.5 g of distearoyl phospholipid Acetyl ethanolamine-polyethylene glycol, dissolves to form a clear, transparent oily solution. The solvent was removed by rotary evaporation under reduced pressure at 30°C to form a thin film, then deionized water was added to hydrate under the action of ultrasonic (80w, 3min) in a water bath, and then the ultrasonic probe (200w, 2min, set to work for 3s, intermittent for 7s, a total of 12 cy...

Embodiment 3

[0041] Take 0.5g of rhein and 2g of soybean lecithin, add 50ml of methanol, stir and react at 45°C for 24 hours to obtain a clear solution, remove the ethanol under reduced pressure at 50°C, collect the solids and dry them in vacuum for 12 hours, then crush them to obtain the rhein phospholipid complex.

[0042] Dissolve 1.0 g of the obtained rhein phospholipid complex in 50 mL of chloroform, stir and dissolve until it becomes a transparent oily liquid, and obtain a rhein phospholipid complex solution; then add 2.0 g of lecithin, 1.0 g of cholesterol, and 0.2 g of distearoyl phospholipid Acetyl ethanolamine-polyethylene glycol, dissolved to form a clear and transparent oily solution; remove the solvent by rotary evaporation under reduced pressure at 30°C to form a thin film, then add 5mL deionized water, hydrate under the action of ultrasonic (60w, 5min) in a water bath, and then probe Ultrasound (200w, 3min, set to work for 3s, intermittent for 7s, a total of 18 cycles), and f...

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Abstract

In view of difficulty in clinical administration of rhein, the invention firstly provides a rhein phospholipid complex as well as a preparation method and application thereof. The preparation method of the rhein phospholipid complex includes the following steps: (1) weighing rhein and a first phospholipid according to the weight ratio of the rhein to the first phospholipid of 2:1 to 1:20, and dispersing the weighed rhein and first phospholipid in an organic solvent to obtain a reaction solution; (2) performing a reaction on the reaction solution under stirring at 30-60 DEG C for 2-24 h; and (3) performing reduced-pressure concentration on the solution after the reaction, and collecting the obtained solid to obtain the rhein phospholipid complex; and preparing a long-circulating liposome by using the rhein phospholipid complex, a second phospholipid, cholesterol, and distearoyl phosphatidylethanolamine-polyethylene glycol. According to the preparation method provided by the invention,after the rhein is compounded with the phospholipid, the solubility is improved, the druggability is improved, preparation of preparations is facilitated, and the complex is used to further prepare the long-circulating liposome, so that the biological half-life period of the rhein is effectively prolonged while efficient drug loading capacity is ensured.

Description

technical field [0001] The invention belongs to the technical field of rhein preparations, and in particular relates to a preparation method of a rhein phospholipid complex, which is further prepared into a long circulation liposome. Background technique [0002] Rhein (Rhein) is one of the active ingredients of traditional Chinese medicine rhubarb. Dihydroxy-3-carboxy-anthraquinone), its structural formula is as follows: [0003] [0004] From a structural point of view, rhein contains a planar 1,8-dihydroxyanthraquinone structural unit, which has electrochemical redox properties, endowing rhein with a wide range of pharmacological effects such as anticancer, antibacterial, anti-inflammatory, immunosuppressive and antioxidative. Great clinical application value (Sun H, Luo G, Chen D, Xiang Z. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient. Frontiers in Pharmacology. 2016; 7:247.). It is worth m...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/192A61P35/00A61P29/00A61P31/12A61P39/06A61P9/10
CPCA61K47/6911A61K47/544A61K31/192A61P35/00A61P29/00A61P31/12A61P39/06A61P9/10
Inventor 张金洁李建波强弘张振中
Owner ZHENGZHOU UNIV
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