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Tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere and preparation method thereof

A technology of glycolic acid microspheres and glycolic acid, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of low bioavailability, affecting clinical efficacy, and low solubility, etc. problem, to achieve the effect of reducing microvessel density, inhibiting tumor growth, and high encapsulation efficiency

Inactive Publication Date: 2013-05-08
SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low solubility of tanshinone ⅡA in water, the bioavailability of common preparations containing tanshinone ⅡA (such as tablets, capsules, etc.) is not high, which directly affects the clinical efficacy

Method used

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  • Tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere and preparation method thereof
  • Tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere and preparation method thereof
  • Tanshinone IIA-polyactic acid/hydroxyacetic acid microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The oil phase (dispersed phase) is PLGA with a weight to volume ratio of 30% (g / ml) 75 / 25 - Dichloromethane solution, the water phase (continuous phase) is a PVA-water solution with a weight volume ratio of 0.5% (g / ml), and the oil phase / water phase ratio is 1:10 (volume ratio). The drug loading, that is, the content of tanshinone ⅡA is 3.5% by weight. Homogenize under the condition of 2900rpm×3min. After forming colostrum, pour it into 400ml of PVA-water solution with a weight-volume ratio of 0.5%. Stirring speed is 200rpm, Dichloromethane was volatilized at 35°C to solidify the microspheres. After sieving, the PVA attached to the surface was washed off with 400 ml of pure water, and dried under reduced pressure to obtain microsphere powder. Flowchart such as figure 1 shown.

[0053] Among them, Tanshinone Ⅱ A was purchased from Xi'an Guanyu Biotechnology Company, with a purity of ≥98%. PLGA: monomer ratio lactic acid / glycolic acid = 75 / 25, Mw 15kD, ester-capped, pu...

Embodiment 2

[0055] The oil phase (dispersed phase) is PLGA with a weight to volume ratio of 10% (g / ml) 70 / 30 -Dichloromethane solution, the water phase (continuous phase) is a PVA-water solution with a weight-to-volume ratio of 1% (g / ml), and the oil phase / water phase ratio is 1:10 (volume ratio). The drug loading, that is, the content of tanshinone ⅡA is 1% by weight, homogenized under the condition of 2900rpm×3min, and poured into 200ml of PVA-water solution with a weight-volume ratio of 1% after forming colostrum, at a stirring speed of 200rpm, Dichloromethane was volatilized at 35°C to solidify the microspheres. After sieving, the PVA attached to the surface was washed off with 400 ml of pure water, and dried under reduced pressure to obtain microsphere powder.

[0056] Among them, Tanshinone Ⅱ A was purchased from Xi'an Guanyu Biotechnology Company, with a purity of ≥98%. PLGA: monomer ratio lactic acid / glycolic acid=70 / 30, ester-terminated, purchased from Shandong Institute of Medi...

Embodiment 3

[0058] The oil phase (dispersed phase) is PLGA with a weight to volume ratio of 20% (g / ml) 85 / 15-Dichloromethane solution, the water phase (continuous phase) is PVA-water solution with a weight volume ratio of 0.6% (g / ml), and the oil phase / water phase ratio is 1:10 (volume ratio). The drug loading, that is, the content of tanshinone ⅡA is 6% by weight, homogenized under the condition of 2900rpm×3min, and poured into 300ml of PVA-water solution with a weight-volume ratio of 0.6% after forming colostrum, at a stirring speed of 200rpm, Dichloromethane was volatilized at 35°C to solidify the microspheres. After sieving, the PVA attached to the surface was washed off with 400 ml of pure water, and dried under reduced pressure to obtain microsphere powder.

[0059] Among them, Tanshinone Ⅱ A was purchased from Xi'an Guanyu Biotechnology Company, with a purity of ≥98%. PLGA: monomer ratio lactic acid / glycolic acid = 85 / 15, ester-terminated, purchased from Shandong Institute of Medi...

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Abstract

The invention discloses a tanshinone IIA-polyactic acid / hydroxyacetic acid microsphere and a preparation method thereof. The microsphere is prepared by drying oil-in-water type emulsion, wherein the oil phase is dichloromethane solution of a polyactic acid / hydroxyacetic acid copolymer and the water phase is the water solution of polyvinyl alcohol. The drug content of tanshinone IIA in the microsphere is 1-10% and the entrapment efficiency is 60-90%. The particle size range of the microsphere is 30-200mm. The tanshinone IIA-polyactic acid / hydroxyacetic acid microsphere provided by the invention is suitable for interventional therapy of liver cancers, has a good liver tumor peripheral vascular thrombosis function, has an effective thrombosis time of 7-60 days, can be distributed in tumor tissues in a targeted manner, slowly release drugs, increase the local concentrations of the drugs, prolong the drug metabolism time, obviously inhibit animal liver tumor growth and prolong the animal lifetime and can inhibit expressions of a human hypoxia inducible factor 1alpha and a vascular endothelial growth factor and reduce the tumor tissue microvessel density after thrombosis.

Description

technical field [0001] The invention relates to a drug-loaded microsphere and a preparation method thereof, in particular to a tanshinone IIA-polylactic acid / glycolic acid microsphere and a preparation method thereof. Background technique [0002] Primary liver cancer (PLC) is one of the common malignant tumors in my country with a high mortality rate. In the incidence of cancer in my country, liver cancer ranks second, accounting for 53% of the global liver cancer mortality rate, ranking first in the world. Liver cancer is a highly invasive and metastatic malignant tumor with hidden early symptoms. Only 29% to 47.9% of liver cancer patients can be diagnosed early, and most cases are diagnosed at an advanced stage, or with severe liver cirrhosis, and can undergo radical surgical resection Only 10% to 30% of cases. Transcatheter hepatic artery intervention is the preferred non-surgical treatment for patients with hepatocellular carcinoma who cannot be cured by surgery. In ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/58A61K47/34A61P35/00
Inventor 李琦王炎朱惠蓉殷佩浩陈红宇周利红秦建民孙珏范忠泽
Owner SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M
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