Tanshinone IIA polylactic acid nano particles and preparation method thereof

A technology of tanshinone and polylactic acid, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem that the treatment of patients is difficult to continue, the quality of life of cancer patients is decreased, and the mortality rate is increased. problems, to achieve the effect of increasing liver targeting, improving bioavailability, and changing in vivo processes

Inactive Publication Date: 2008-11-26
SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reason is that the distribution of these drugs in the body is not selective. In addition to killing cancerous cells, they also have an impact on the metabolism of normal cells. It is difficult to continue, leading to a decline in the quality of life of cancer patients and an increase in mortality

Method used

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  • Tanshinone IIA polylactic acid nano particles and preparation method thereof
  • Tanshinone IIA polylactic acid nano particles and preparation method thereof
  • Tanshinone IIA polylactic acid nano particles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 1.42mg of tanshinone IIA, 36.9mg of PLA, 80mg of lecithin and dissolve in a mixture of 4.5ml of dichloromethane and 0.5ml of acetone to form an organic phase, add to 30ml of F68 aqueous phase solution with a concentration of 1.0%, and add the organic phase to Put it into the water phase, sonicate the probe for 5 minutes in an ice bath to form an O / W emulsion, and then evaporate the organic solvent with magnetic stirring at room temperature to obtain a suspension of tanshinone IIA polylactic acid drug-loaded nanoparticles, which is filtered through a 0.65 μm microporous membrane to remove aggregation The body and the unwrapped drug are added with scaffold agent glucose and freeze-dried to obtain freeze-dried nanoparticles.

[0034] Detection: the average particle diameter of tanshinone II A polylactic acid drug-loaded nanoparticles is 210nm, and the encapsulation efficiency is 68%.

Embodiment 2

[0036] Take by weighing 2.58mg tanshinone IIA, 36.9mgPLA, 80mg lecithin and be dissolved in the mixed solution of 4.5ml dichloromethane and 0.5ml acetone, constitute the organic phase, add 30ml concentration and be the PVA aqueous phase solution of 2.0%, the organic phase is added to In the water phase, the probe was sonicated for 5 minutes in an ice bath to form an O / W emulsion, and then the organic solvent was evaporated by magnetic stirring at room temperature to obtain a suspension of tanshinone IIA polylactic acid drug-loaded nanoparticles, which was filtered through a 0.65 μm microporous membrane to remove aggregates And the uncoated medicine, adding scaffold agent lactose, freeze-drying to obtain freeze-dried nanoparticles.

[0037] Detection: the average particle diameter of tanshinone IIA polylactic acid drug-loaded nanoparticles is 230nm, and the encapsulation efficiency is 78%.

Embodiment 3

[0039] Weigh 1.5mg of tanshinone IIA, 100mg of PLA, 80mg of lecithin and dissolve in a mixture of 8ml of dichloromethane and 1ml of acetone to form an organic phase, add 30ml of F68 aqueous phase solution with a concentration of 1.5%, and add the organic phase to the aqueous phase , the probe was ultrasonicated for 5 minutes in an ice bath to form an O / W emulsion, and then the organic solvent was volatilized by magnetic stirring at room temperature to obtain a suspension of tanshinone II A polylactic acid drug-loaded nanoparticles, which was filtered through a 0.65 μm microporous membrane to remove aggregates and untreated particles. The encapsulated medicine is added with scaffolding agent mannitol, and freeze-dried to obtain freeze-dried nanoparticles.

[0040] Detection: the average particle diameter of tanshinone II A polylactic acid drug-loaded nanoparticles is 195nm, and the encapsulation efficiency is 82%.

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Abstract

The invention pertains to pharmaceutical field and relates to a tanshinone IIA polylactic acid drug-loaded nanoparticle preparation and a preparation method of the preparation. The active component of the carrier drug nanoparticles of the invention is tanshinone IIA, the carrier drug nano-material is polylactic acid, the range of the particle size of the nanoparticle size is 50nm to 300nm, the carrier drug amount of the nanoparticles is 1 percent to 30 percent, and the encapsulation rate of the nanoparticles is 70 percent to 90 percent. The carrier drug nanoparticles can be prepared into a freeze-dried powder injection. The preparation of the invention can improve the dispersion degree of the drug in carrier material, enhance the dissolution of the drug, improve the bioavailability, change the process in vivo of the drug, increase the liver target and have great significance on the injection drug delivery of tanshinone. The problem of easy drug leakage of liposomes, microemulsion and other preparations can be simultaneously better solved.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a tanshinone IIA polylactic acid drug-loaded nanoparticle preparation and a preparation method of the preparation. Background technique [0002] Tanshinone II A (Tashinones, TS) is a fat-soluble active ingredient extracted from the traditional Chinese medicine Salvia miltiorrhiza Bunge. The cells have cytotoxic effect and can inhibit the invasion and metastasis of tumor cells. It is used in the treatment of leukemia, primary liver cancer, gastric cancer and other malignant tumors, which can improve the condition, shrink the tumor and prolong the survival period. It has been reported in the literature that 0.25-1.0 μg / ml tanshinone IIA has proliferation inhibitory and cytotoxic effects on a variety of tumor cells. It has a synergistic effect on the antitumor activity of cyclophosphamide, camptothecin and other drugs, has a killing effect on ascites cancer cells, and can inhibit the DNA synt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61K9/19A61K47/34A61P35/00
Inventor 李琦冯年平范忠泽孙珏王炎南艺蕾李先茜李绪林殷佩浩梅映昊刘宁宁刘昭林
Owner SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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