Ligustrazine nanoparticle, preparation method and pharmaceutical application thereof

A technology of ligustrazine and nanoparticles, applied in the field of medicine, can solve problems such as uncertainty in surgical techniques, poor effect of mechanical isolation, inconvenient continuous administration, etc., to prevent postoperative adhesive intestinal obstruction, prevent and treat intestinal adhesions, Effect without toxic side effects

Active Publication Date: 2012-05-23
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] For the prevention of adhesive intestinal obstruction, at present, the improvement of surgical techniques, the use of barrier substances and the combination of drugs are mainly used to reduce fibrin deposition, promote fibrinolysis, and reduce excessive adhesions. However, due to the uncertainty of surgical techniques and the current There are disadvantages such as unstable efficacy of therapeutic drugs, inconvenient continuous administration, and poor effect of simple mechanical isolation.
Therefore, this common pathological abdominal adhesion, which has no effective prevention and treatment measures so far, has always been an important topic in the anti-tissue fibrosis proposition.

Method used

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  • Ligustrazine nanoparticle, preparation method and pharmaceutical application thereof
  • Ligustrazine nanoparticle, preparation method and pharmaceutical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Weigh 125mg of polylactic acid and dissolve it in 7mL of acetone to form a polylactic acid acetone solution, then dissolve 25mg of ligustrazine in the polylactic acid acetone solution to form an oil phase, quickly add the oil phase to 20mL of 0.3% poloxa that has been kept at a temperature of 30°C in an aqueous solution. After the two phases were mixed, the mixture was magnetically stirred at 30°C for 80 minutes to volatilize the acetone to obtain the ligustrazine nanoparticle solution.

[0019] The encapsulation efficiency of nanoparticles can reach more than 30%.

Embodiment 2

[0021] Weigh 100mg of polylactic acid and dissolve it in 5mL of acetone to form a polylactic acid acetone solution, then dissolve 20mg of ligustrazine in the polylactic acid acetone solution to form an oil phase, and quickly add the oil phase to a solution with a concentration of 0.25% poise at a constant temperature of 40°C Loxamer in 20mL aqueous phase solution. After the two phases were mixed, the mixture was magnetically stirred at 40°C for 70 minutes to volatilize the acetone to obtain the ligustrazine nanoparticle solution.

[0022] The encapsulation efficiency of nanoparticles can reach more than 30%.

Embodiment 3

[0024] Weigh 100 mg of polylactic acid and dissolve it in 5 mL of acetone to form a polylactic acid acetone solution, then dissolve 30 mg of ligustrazine in the polylactic acid acetone solution to form an oil phase, and quickly add the oil phase to a solution with a concentration of 0.2% poise at a constant temperature of 35°C Loxamer in 20mL aqueous phase solution. After the two phases were mixed, the mixture was magnetically stirred at 35°C for 70 minutes to volatilize the acetone to obtain the ligustrazine nanoparticle solution.

[0025] The encapsulation efficiency of nanoparticles can reach more than 30%.

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Abstract

The invention relates to a ligustrazine nanoparticle, a preparation method and pharmaceutical application thereof. The preparation method comprises the following steps of: dissolving polylactic acid in acetone to form a polylactic acid acetone solution; then dissolving ligustrazine in the polylactic acid acetone solution to form an oil phase; adding the oil phase to a surface active agent-contained aqueous phase solution which is at the constant temperature of 20-50 DEG C; after the two phases are mixed, stirring for 50-90min at the temperature of 20-50 DEG C to make acetone volatilize to obtain a ligustrazine nanoparticle solution. The invention has simple process, mild reaction condition, even manufactured particle size and narrow distribution. Moreover, adopted auxiliary materials are biodegradable and have good biocompatibility, no toxic or side effects and sufficient market raw materials. Wrapped in the nanoparticle, ligustrazine can stably and slowly release, can effectively prevent and treat postoperative adhesion intestine and prevent postoperative adhesive intestinal obstruction.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a ligustrazine nanoparticle, a preparation method thereof, and an application in the field of pharmacy. 2. Background technology [0002] Abdominal adhesion is an inevitable process of postoperative peritoneal repair. After abdominal surgery, fibrinogen colloid will ooze from the local wound, which will quickly transform into fibrin coagulation, covering the wounded peritoneal surface, and repairing and protecting the wound. There is no repair without adhesions, but when the body's repair is disordered or the fiber degradation is incomplete so that it develops into punctate, angled or cord-like adhesions, it may lead to mechanical intestinal obstruction in patients. Adhesive ileus has been reported in more than 40% of patients after abdominal surgery. [0003] For the prevention of adhesive intestinal obstruction, at present, the improvement of surgical technique...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/4965A61K47/34A61P41/00A61K47/10
Inventor 曾莉毛春芹陆兔林李林李争艳王晓雯毕蕾卞尧尧陆敏
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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