TH-302 preparation, preparation method and application thereof

A technology of TH-302 and preparation, applied in the fields of application, medical formula, surgical adhesive, etc., can solve the problem of high toxicity and side effects, and achieve the effect of enhancing the anti-tumor effect

Inactive Publication Date: 2018-06-05
GENERAL HOSPITAL OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral medication belongs to systemic medication, and only a part of the drug reaches cancer cells, so its toxic and side effects are very serious

Method used

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  • TH-302 preparation, preparation method and application thereof
  • TH-302 preparation, preparation method and application thereof
  • TH-302 preparation, preparation method and application thereof

Examples

Experimental program
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preparation example Construction

[0025] The present invention also relates to a preparation method of TH-302 hepatic artery embolization microspheres, which is prepared by a single emulsification-solvent evaporation method, and dissolves active drugs and biodegradable medicinal polymer materials in one or more organic solvents An oil phase is formed in the medium, and the organic solvent is selected from dichloromethane, ethyl acetate, acetone, ethanol, methanol, benzyl alcohol or more than one mixed organic solvent. In addition, the continuous water phase is prepared, and the non-ionic surfactant is dissolved in water, and their weight percentage in the water is 2%-5%. The nonionic surfactant is selected from polyvinyl alcohol, polyvinylpyrrolidone, sodium carboxymethylcellulose, sodium polymethacrylate, polypropylene, gelatin and tragacanth. The steps for preparing microspheres by the single emulsification-solvent evaporation method are as follows: add polymer excipients and active drug TH-302 into dichloro...

example 1

[0032] The influence of example 1 ester-terminated PLGA on microsphere encapsulation efficiency

[0033] Weigh 0.6 g of ester-capped PLGA and dissolve it in an organic solvent to form an oil phase. The organic solvent is dichloromethane or a mixture of dichloromethane and methanol. Precisely weigh a certain amount of TH-302 active drug and dissolve it in the above oil phase, and mix evenly by ultrasonic to obtain the drug-containing organic phase. Weigh an appropriate amount of PVA into a certain volume of distilled water, heat and dissolve the PVA repeatedly in a microwave oven to make up for the weight loss, and obtain an aqueous solution with a concentration of 3%. Inject the above oil phase into 15ml, 3% PVA solution with a syringe pump at a certain speed, stir at 350rpm for 7min, transfer the above emulsion to 250ml, 2%PVA solution, stir at 250rpm, 4°C for 4-5h, The organic solvent was volatilized, centrifuged, washed, and dried to obtain ester-capped PLGA microspheres, ...

example 2

[0034] The influence of example 2 carboxy-terminal PLGA on microsphere encapsulation efficiency

[0035] Weigh 0.6 g of carboxy-terminal PLGA and dissolve it in an organic solvent to form an oil phase. The organic solvent is dichloromethane or a mixture of dichloromethane and methanol. Precisely weigh a certain amount of TH-302 active drug and dissolve it in the above oil phase, and mix evenly by ultrasonic to obtain the drug-containing organic phase. Weigh an appropriate amount of PVA into a certain volume of distilled water, heat and dissolve the PVA repeatedly in a microwave oven to make up for the weight loss, and obtain an aqueous solution with a concentration of 3%. Inject the above oil phase into 15ml, 3% PVA solution with a syringe pump at a certain speed, stir at 350rpm for 7min, transfer the above emulsion to 250ml, 2%PVA solution, stir at 250rpm, 4°C for 4-5h, The organic solvent was volatilized, centrifuged, washed, and dried to obtain carboxy-terminal PLGA micros...

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Abstract

The invention relates to a TH-302 microsphere preparation as well as a preparation method and application thereof. A carrier material polylactic acid or polylactic acid / hydroxyacetic acid copolymer with a degradation product being lactic acid or hydroxyacetic acid is used for entrapping TH-302 or pharmaceutical salt thereof, so that an embolism microsphere is prepared, on one hand, a physical barrier of the microsphere can be utilized for blocking blood supply of tumor tissues; and on the other hand, a TH302 active product can be slowly released under the action of acid produced during degradation of the carrier material, so that the antitumor effect is further enhanced.

Description

technical field [0001] The present invention relates to a pharmaceutical preparation for treating liver cancer, in particular to a TH-301 preparation, preparation method and use for treating advanced liver cancer patients who cannot be treated with surgery. Background technique [0002] Hepatocellular carcinoma (Hepatocellular carcinoma HCC) is one of the malignant tumors worldwide. It has an insidious onset, rapid progression, and short survival period, which seriously endangers human health. More than 500,000 patients are diagnosed each year, and it is the third leading cause of cancer-related death worldwide. The incidence rate in Europe is 3.6 / 100,000 to 10.6 / 100,000, and the global incidence is 16.0 / 100,000. At present, the main treatment method for liver cancer patients is surgery, but the effect is only good for early-stage liver cancer. For most liver cancer patients, they are already in the middle and late stages when they are diagnosed, and there is no opportunity...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34A61K31/675A61P35/00A61L24/04A61L24/00
CPCA61K9/5031A61K31/675A61L24/001A61L24/0015A61L24/046A61L2300/204A61L2300/416A61L2300/604A61L2300/622C08L67/04
Inventor 王志军李志平唐雪梅
Owner GENERAL HOSPITAL OF PLA
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