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Sodium alginate targeted sustained release microsphere vascular occlusive agent containing Sorafenib as well as preparation and application thereof

A vascular embolizing agent and sodium alginate technology are applied in the field of sodium alginate targeted slow-release microsphere vascular embolizing agent to achieve the effects of reducing the systemic circulation process, being highly targeted, and reducing normal cell damage.

Active Publication Date: 2009-09-23
BEIJING SHENGYIYAO SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] At present, sorafenib and sodium alginate have not been made into microspheres for local target vascular embolization in the treatment of liver cancer, kidney cancer, non-small cell lung cancer, gastric cancer, ovarian cancer, prostate cancer, head and neck tumors, and melanin. solid tumors

Method used

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  • Sodium alginate targeted sustained release microsphere vascular occlusive agent containing Sorafenib as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] 1. Preparations before packing:

[0055] Treatment of glassware: dry the cleaned glassware, put it in a high-temperature oven and bake at 260 degrees Celsius for 3 hours (sterilize and remove heat source);

[0056] 2. Preparation of various reagents:

[0057] ①Preparation of the antineoplastic drug Sorafenib liquid:

[0058] Weigh 10 mg of commercially available sorafenib, place it in the above-mentioned glass vessel, add an appropriate amount of polyvinylglycerol 400 dropwise until it is completely dissolved, and obtain 20 ml of sorafenib solution.

[0059] ② Preparation of sodium alginate solution:

[0060] Configure sodium alginate solution at a concentration of 2% by weight (while stirring, add physiological saline), until sodium alginate is completely dissolved to obtain 3 liters of sodium alginate solution;

[0061] ③Consolidation solution preparation:

[0062] Calcium chloride is weighed, dissolved with physiological saline, and prepared into a calcium chlori...

Embodiment 2

[0077] 1. Preparations before packing:

[0078] Treatment of glassware: dry the cleaned glassware, put it in a high-temperature oven and bake at 260 degrees Celsius for 3 hours (sterilize and remove heat source);

[0079] 2. Preparation of various reagents:

[0080] ①Preparation of the antineoplastic drug Sorafenib liquid:

[0081] Weigh 0.62 g of commercially available Sorafenib, place it in the above-mentioned glass vessel, add an appropriate amount of dimethyl sulfoxide (DMSO solution) dropwise until it is completely dissolved, and obtain 500 ml of Sorafenib solution.

[0082] ② Preparation of sodium alginate solution:

[0083] Configure the sodium alginate solution at a concentration of 1% by weight (while stirring, adding physiological saline), until the sodium alginate is completely dissolved to obtain 45 liters of sodium alginate solution;

[0084] ③Consolidation solution preparation:

[0085] Calcium lactate was weighed, dissolved with physiological saline, and pre...

Embodiment 3

[0100] 1. Preparations before packing:

[0101] Treatment of glassware: dry the cleaned glassware, put it in a high-temperature oven and bake at 260 degrees Celsius for 3 hours (sterilize and remove heat source);

[0102] 2. Preparation of various reagents:

[0103] ①Preparation of the antineoplastic drug Sorafenib liquid:

[0104] Weigh 6.9 mg of commercially available sorafenib, place it in the above-mentioned glass vessel, add an appropriate amount of dimethyl sulfoxide (DMSO solution) dropwise until it is completely dissolved, and obtain 30 ml of sorafenib solution.

[0105] ② Preparation of sodium alginate solution:

[0106] Configure the sodium alginate solution at a concentration of 7% by weight (while stirring, add physiological saline), until the sodium alginate is completely dissolved to obtain 2000 milliliters of the sodium alginate solution;

[0107] ③Consolidation solution preparation:

[0108] The calcium lactate is weighed, dissolved in water for injection, ...

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Abstract

The invention discloses a sodium alginate targeted sustained release microsphere vascular occlusive agent containing Sorafenib as well as a preparation and application thereof. The invention is characterized by comprising carrier sodium alginate and antitumor targeted drug Sorafenib; the sodium alginate wraps the Sorafenib; the Sorafenib is 1 portion by weight and the sodium alginate is 1 to 30 portions by weight. The vascular occlusive agent leads the oral targeted drug to achieve the purpose of interventional embolotherapy by an interventional embolotherapy method for changing preparation formulation and changing the drug administration way, simultaneously leads Sorafenib of the antitumor drug to be directly located to cancer tissues in a fast and long-acting manner from local target areas, has strong pointedness and obvious effect, does not damage normal tissues while cutting blood supply of tumor and inhibiting growth of the tumor cells, has high drug concentration in local target areas and little drug amount for the whole body, better and effectively protects the self immune system of patients and reduces toxic and side effects and the like.

Description

technical field [0001] The invention relates to a microsphere vascular embolization agent containing antineoplastic drugs and its preparation and application, in particular to a Sorafenib-containing sodium alginate targeted slow-release microsphere vascular embolization agent and its preparation and application. Background technique [0002] Sorafenib is a novel diaryl urea with the chemical name 4-{4-[3-(4-chloro-3-trifluoro-phenyl)-ureide]-phenoxy} - Methylamine pyridine-2-carboxylate, molecular weight 464.8 g / mol. The clinical use is the tosylate salt of sorafenib. Molecular formula of sorafenib tosylate salt: C 21 h 16 C 1 f 3 N 4 o 3 ·C 7 h 8 o 3 S, the molecular weight is 637.0 g / mol. The molecular structural formula is as follows: [0003] [0004] Sorafenib tosylate has a melting point of 225-235°C and is an odorless, white to brown solid. Good thermal stability, non-absorbent. Low solubility in aqueous solution, slightly increased solubility in stro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/36A61K31/44A61P35/00A61J3/00A61L31/14
CPCA61K9/0019A61K9/5089A61K9/1652A61K31/44A61K9/5036A61P35/00A61P43/00
Inventor 李新建洪宏鲁格
Owner BEIJING SHENGYIYAO SCI & TECH DEV
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