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Cucurbitacin B nanometer liposome and preparation thereof

A nano-liposome and cucurbitacin technology, which is applied in the direction of liposome delivery, medical preparations containing active ingredients, organic active ingredients, etc., to achieve the effects of prolonging drug action time, improving selection, and prolonging residence time

Inactive Publication Date: 2016-11-23
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problems existing in the existing cucurbitacin B preparations, the present invention provides a cucurbitacin B nanoliposome drug for the treatment of various types of liver cancer

Method used

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  • Cucurbitacin B nanometer liposome and preparation thereof
  • Cucurbitacin B nanometer liposome and preparation thereof
  • Cucurbitacin B nanometer liposome and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The formula of the present invention is made up of following components:

[0049] Cucurbitacin B 0.5 parts

[0050] Hydrogenated soybean lecithin for injection 40 parts

[0051] Vitamin E 0.1 parts

[0052] Cholesterol 5 servings

[0053] Macrogol 2000-Distearoyl Phosphatidylethanolamine 0.5 parts

[0054] 0.5 parts of 2,6-di-tert-butyl-p-cresol

[0055] Poloxamer F-68 0.5 parts

[0056] 1) Dissolve cucurbitacin B, hydrogenated soybean lecithin for injection, vitamin E, cholesterol, polyethylene glycol 2000-distearyl phosphatidylethanolamine in a mixed solution of ether and ethanol at a volume ratio of 2-10:1, Ether and ethanol were removed under reduced pressure in a rotary evaporator, and a liposome film was formed on the bottle wall.

[0057] 2) Dissolve 2,6-di-tert-butyl-p-cresol and poloxamer F-68 in phosphate buffer in sequence, steam sterilize, cool to room temperature and adjust the pH value to 6.0-7.0.

[0058] 3) Dissolve the liposome membrane prepared ...

Embodiment 2

[0060] The formula of the present invention is made up of following components:

[0061] Cucurbitacin B 30 parts

[0062] Hydrogenated soybean lecithin for injection 90 parts

[0063] Vitamin E 10 parts

[0064] Cholesterol 50 servings

[0065] Macrogol 2000-Distearoyl Phosphatidylethanolamine 30 parts

[0066]2,6-di-tert-butyl-p-cresol 30 parts

[0067] Poloxamer F-68 50 parts

[0068] 1) Dissolve cucurbitacin B, hydrogenated soybean lecithin for injection, vitamin E, cholesterol, polyethylene glycol 2000-distearyl phosphatidylethanolamine in a mixed solution of ether and ethanol at a volume ratio of 2-10:1, Ether and ethanol were removed under reduced pressure in a rotary evaporator, and a liposome film was formed on the bottle wall.

[0069] 2) Dissolve 2,6-di-tert-butyl-p-cresol and poloxamer F-68 in phosphate buffer in sequence, steam sterilize, cool to room temperature and adjust the pH value to 6.0-7.0.

[0070] 3) Dissolve the liposome membrane prepared in step ...

Embodiment 3

[0072] The formula of the present invention is made up of following components:

[0073] Cucurbitacin B 15 parts

[0074] Hydrogenated soybean lecithin for injection 65 parts

[0075] Vitamin E 5 parts

[0076] Cholesterol 10 servings

[0077] Macrogol 2000-Distearoyl Phosphatidylethanolamine 15 parts

[0078] 15 parts of 2,6-di-tert-butyl-p-cresol

[0079] Poloxamer F-68 15 parts

[0080] 1) Dissolve cucurbitacin B, hydrogenated soybean lecithin for injection, vitamin E, cholesterol, polyethylene glycol 2000-distearyl phosphatidylethanolamine in a mixed solution of ether and ethanol at a volume ratio of 2-10:1, Ether and ethanol were removed under reduced pressure in a rotary evaporator, and a liposome film was formed on the bottle wall.

[0081] 2) Dissolve 2,6-di-tert-butyl-p-cresol and poloxamer F-68 in phosphate buffer in sequence, steam sterilize, cool to room temperature and adjust the pH value to 6.0-7.0.

[0082] 3) Dissolve the liposome membrane prepared in st...

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Abstract

The present invention relates to a cucurbitacin B liposome drug and preparation thereof. The invention provides a cucurbitacin B nanometer liposome drug and a preparation method thereof. According to the present invention, a passive drug delivery way is used, and a substance polyethylene glycol containing polyhydroxy groups is linked to the phospholipid phosphoric acid group to modify so as to prepare the long-circulating nanometer liposome, wherein the structural modification effect is to protect the liposome from being identified and uptaken by opsonin in blood so as to reduce the liposome clearance rate and prolong the residence time in the blood, such that the action time of the drug is prolonged, the liposome can effectively reach the lesion, and the selectivity on the targeted tissue can be improved; the preparation prepared by the preparation method has characteristics of good physical stability, good chemical stability, long residence time in the body, small distribution volume in the body, and high blood drug concentration in the body; the drug of the present invention can be used for treatment of various types and various stages of liver cancers; and the cucurbitacin B liposome drug has characteristics of scientific formula, convenient use, good stability and low toxicity, and the preparation method is suitable for large-scale production.

Description

Technical field: [0001] The invention relates to cucurbitacin B nano liposome and its preparation. technical background: [0002] (1) Cucurbitacin B (CuB for short) is a bitter aglycone component extracted from various plants of Cucurbitaceae and other families and genera. It is a highly oxidized tetracyclic triterpenoid compound. The most abundant member with a wide range of pharmacological activities. Modern studies have shown that cucurbitacin B has various biological activities such as liver protection, anti-inflammatory and anti-tumor. Cucurbitacin B has inhibitory effects on human liver cancer cell lines both in vivo and in vitro. Its inhibitory effect is caused by cell cycle arrest and induction of apoptosis. In recent years, scholars at home and abroad have systematically studied the antitumor effect of cucurbitacin B, which is a potential antitumor drug. [0003] (2) Systemic chemotherapy is one of the important means to treat tumors. However, most chemotherape...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/575A61K47/22A61K47/10A61K47/34A61P35/00
Inventor 白雪刘素香刘毅
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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