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Cardiac glycoside active compound lipidosome and preparation method thereof

A compound, cardiac glycoside technology, applied in the field of cardiac glycoside active compound liposome and its preparation, can solve problems such as cardiac toxicity and side effects, achieve the effects of reducing toxicity and side effects, expanding the scope of application, and increasing distribution

Inactive Publication Date: 2019-03-12
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the activity and side effects of the compound have been improved after structural modification, since the target of cardiac glycosides is Na + -K + -ATPase, which is also distributed in normal cells, especially cardiomyocytes, so high doses may cause cardiotoxic side effects

Method used

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  • Cardiac glycoside active compound lipidosome and preparation method thereof
  • Cardiac glycoside active compound lipidosome and preparation method thereof
  • Cardiac glycoside active compound lipidosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1II1E-01

[0052] Example 1 Preparation of II1E-01·HCl liposome (II1E-01·HCl@Lipo)

[0053] The hydrogenated soybean lecithin, cholesterol, and distearoylphosphatidylethanolamine-polyethylene glycol copolymer were mixed in a weight ratio of (56:20:24), dissolved in absolute ethanol, and placed on a rotary evaporator at 40 Rotary evaporation at -60℃ and pressure of 0.02-5.32kPa to remove the absolute ethanol and form a lipid film; then add 0.11M ammonium sulfate aqueous solution at the same temperature for hydration, and continue to rotate for 0.5h under normal pressure ; Use ultrasound (30% power, 10min) to uniform the particle size of the liposome suspension formed, and use column chromatography to replace the external phase with deionized water to form an ammonium sulfate gradient inside and outside the phospholipid membrane, which is a blank Liposomes. The II1E-01·HCl solution (according to the mass ratio of the drug to the membrane material is 8:100) and the blank liposome are respecti...

Embodiment 2C01

[0054] Example 2 Preparation of C01 liposome (C01@Lipo)

[0055] Mix the hydrogenated soybean lecithin, cholesterol and distearoyl phosphatidylethanolamine-polyethylene glycol copolymer in a mass ratio of (56:20:24), and add C01 (according to the mass percentage of the drug and the membrane material is 8:100) , Completely dissolved in anhydrous ethanol and heated at 50℃, slowly poured into PBS (pH 8.0) stirred at the same temperature, after the injection is completed, continue to open the heating and stirring to volatilize the anhydrous ethanol; finally mix the formed liposomes The suspension is ultrasonic (30% power, 10min) with uniform particle size and passed through a 0.22μm microporous filter membrane to remove the drugs not encapsulated in the liposomes, thereby obtaining C01@Lipo.

Embodiment 3

[0056] Example 3 Preparation of Bufalin Liposome (Bufalin@Lipo)

[0057] Bufalin was used to replace C01 in Example 2, and the remaining operations were the same as in Example 2.

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Abstract

The invention discloses a liposome preparation of a cardiac glycoside active compound. According to the liposome, hydrogenated soybean lecithin, polyethylene glycol phosphatide and cholesterol are used as lipid materials; firstly, a blank liposome is prepared, and then an ammonium sulfate gradient method is used to actively carry a drug. The prepared drug-carried liposome is good in biocompatibility and has a uniformly distributed particle size of 120 to 240 nm. The liposome can prolong the circulation time of the cardiac glycoside active compound in the body and reduce the number of administrations, and can increase the drug concentration in tumor tissues by using the high permeation and long-term retention effect of the tumor tissues, reduce toxic and side effects on other tissues and organs, especially the heart and improve the anti-tumor effect and the clinical adaptability of the cardiac glycoside active compound.

Description

Technical field [0001] The invention relates to pharmaceutical preparation technology, in particular to a cardiac glycoside active compound liposome and a preparation method thereof. Background technique [0002] Malignant tumors are one of the most serious diseases that threaten human health, and are on the rise. In 2017, the National Cancer Center released the latest status and trends of cancer in China. China accounted for about a quarter of new cancer cases in the world, which is equivalent to about 10,000 diagnoses in the country every day, and an average of 7 people are diagnosed with cancer every minute. [0003] Cardiac glycosides are mainly a steroid derivative extracted from Scrophulariaceae, Apocynaceae plants or toad skin gland secretions. They are currently the first-line drugs for the treatment of congestive heart failure. In the process of treating heart failure, researchers found that cardiac glycosides can effectively prevent and inhibit a variety of solid tumors,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K31/585A61P35/00
CPCA61K9/1277A61K31/585A61K47/24A61K47/28A61P35/00
Inventor 胡立宏胡刚乔宏志高丽娜
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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