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Plasmin carrier lipidosome for promoting absorption of intestine and preparation method thereof

A liposome and plasmin technology, which is applied in the directions of liposome delivery, medical preparations with inactive ingredients, and pharmaceutical formulations, can solve the problems of high price, hyperfibrinolysis in the whole body, and short half-life.

Inactive Publication Date: 2012-12-12
BEIJING TECHNOLOGY AND BUSINESS UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, clinically used thrombolytic agents, such as urokinase (Urokinase, UK), streptokinase (Streptokinase, SK), staphylokinase (Staphylokinase), snake venom antithrombotic enzyme, recombinant plasminogen activator (t-PA and scu-PA), etc., are mostly plasminogen activators, they mainly generate plasmin by activating plasminogen in the body to play a thrombolytic effect, there is a need for intravenous injection, the half-life in the body is short, the stability is poor, and there is no fiber Protein-specific, requires repeated large-dose injections, easily induces hyperfibrinolysis throughout the body, easily causes systemic bleeding and other toxic side effects, or is expensive

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0014] (1) With ω-NH 2 -PEG was used as the initiator, and PEG-Subtilisin FS33 modified protease was prepared by anionic ring-opening polymerization.

[0015] (2) Preparation of plasmin-loaded liposomes. Weigh an appropriate amount of cholesterol and egg yolk lecithin (cholesterol: lecithin = 1:2; W / W), fully dissolve and mix with absolute ethanol and absolute ether, evaporate under reduced pressure at 50°C and drain to form a lipid film, add Appropriate amount of O-carboxymethyl chitosan (chitosan or cholate or lectin, one or its mixture) and 0.5mol / l concentration (NH 4 ) 2 SO 4 The solution was fully hydrated, treated with an ultrasonic cell disruptor (450w) for 20 minutes in an ice bath, then filtered through a 0.22 μm microporous membrane, added modified PEG-Subtilisin FS33 enzyme, and incubated in a water bath at 50°C to obtain the loaded enzyme Liposomes.

[0016] (3) Preparation of plasmin-loaded liposomes for promoting intestinal absorption. The enzyme-carrying ...

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PUM

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Abstract

The invention relates to a plasmin carrier lipidosome for promoting absorption of intestine and a preparation method thereof, belonging to the technical field of food processing and medicine and being applied to the industries of functional foods, health-care products and medicines. BacillussubtilisDC12-33 is a strain of germ separated and selected from the traditional ferment food in China, wherein the germ can produce fibrinolytic enzyme (fibrinolyticsubtilisin) SubtilisinFS33 with strong fibrinolysis activity. The experimental study in vivo and in vitro proves that the SubtilisinFS33 has direct and indirect thrombolysis action. In the invention, a plasmin carrier lipidosome system for promoting absorption of intestine is prepared by adopting the integrated measures of using the modified fibrinolytic enzyme SubtilisinFS33 as the warped object, selecting cholesterol and phospholipid as medium materials, using PEG to modify zymoprotein, 0-carboxymethyl chitosan (or cholate, chitosan and agglutinin) for surface modification of the lipidosome, using the protease inhibitor to restrict the activity of the protease in the alimentary canal, intestine dissolving of acrylic resin (Eudragit) so as to form a system which has multi-layer barrier and is beneficial to enteric epithelium membrane transport and absorption, thereby improving the intestine absorption efficiency and bioavailability of the SubtilisinFS33. The plasmin carrier system can be applied to functional foods, health-care products and the like.

Description

technical field [0001] The invention relates to a plasminase-loaded liposome for promoting intestinal absorption and a preparation method thereof, which belongs to the technical fields of food processing and medicine and can be applied to functional food, health products and medicine industries. Background technique [0002] Cardiovascular and cerebrovascular diseases seriously endanger people's health and have become the first "killer" of human death. Statistics released by the World Health Organization (WHO) show that there are 15 million patients suffering from various thrombotic diseases all over the world, of which about 8 million patients die every year. According to statistics from the Ministry of Health, nearly 1.2 million people die of cardiovascular and cerebrovascular embolism diseases such as cardiovascular and cerebral thrombosis, cerebral apoplexy, cerebral infarction, and senile dementia in my country every year, and more people show sub-health. The preventio...

Claims

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Application Information

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IPC IPC(8): A61K9/127A23L33/10A61K47/60A61K47/69
Inventor 王成涛孙宝国王静曹雁平
Owner BEIJING TECHNOLOGY AND BUSINESS UNIVERSITY