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Surfactant-containing Lonidamine amorphous multielement solid dispersion and preparation method thereof

A technology of solid dispersion and surfactant, applied in the direction of organic active ingredients, medical preparations containing active ingredients, medical preparations of non-active ingredients, etc., can solve the problem of difficult dissolution of lonidamine and achieve thermodynamic stability Good properties, improved solubility, and easy operation

Inactive Publication Date: 2012-08-15
CHANGZHOU RUIMING PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide an amorphous multi-component solid dispersion of lonidamine and a preparation method thereof for the difficult dissolution of lonidamine

Method used

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  • Surfactant-containing Lonidamine amorphous multielement solid dispersion and preparation method thereof
  • Surfactant-containing Lonidamine amorphous multielement solid dispersion and preparation method thereof
  • Surfactant-containing Lonidamine amorphous multielement solid dispersion and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Put 0.5g of lonidamine into a round bottom flask, add 20ml of absolute ethanol and 20ml of dichloromethane, dissolve it by ultrasonic, then add 3.5g of poloxamer 188 and 0.4g of SLS for ultrasonic dissolution. Then the solvent was removed by rotary evaporation under reduced pressure at 35°C, placed in a constant temperature desiccator, and dried overnight at 40°C. Take it out the next day, crush it and sieve it.

Embodiment 2

[0037] Dissolve 1 g of lonidamine, 9 g of PEG60000 and 0.5 g of SLS in tetrahydrofuran, and then spray dry the solution with a spray dryer to obtain an amorphous solid dispersion of lonidamine. Finally the solid dispersion was dried at 40°C for about 3 hours.

Embodiment 3

[0039] Put 0.5g of lonidamine into a round bottom flask, add 40ml of absolute ethanol and 40ml of dichloromethane, dissolve it by ultrasonic, then add 4.5g of PEG6000 and 0.25g of Tween 80 for ultrasonic dissolution. Then, the solvent was removed by rotary evaporation under reduced pressure at 35°C, placed in a constant temperature desiccator, and dried overnight at 40°C. Take it out the next day, crush it and sieve it.

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Abstract

The invention relates to the fields of chemical pharmacy and pharmaceutic preparation, in particular relating to a compound Lonidamine amorphous multielement solid dispersion and a preparation method thereof. The solid dispersion in the invention is characterized by being prepared from Lonidamine, a surfactant and a solid dispersion carrier, wherein the Lonidamine is dispersed in the solid dispersion carrier in an amorphous mode. The Lonidamine amorphous multielement solid dispersion in the invention has the advantages of non-toxic auxiliary materials, no pollution and simple and convenient operation, and greatly improves the solubility of the Lonidamine, thus enhancing the bioavailability and ensuring good thermodynamic stability of preparations.

Description

technical field [0001] The invention belongs to the fields of chemical pharmacy and pharmaceutical preparations, and specifically relates to an amorphous multi-component solid dispersion of compound lonidamine and a preparation method thereof. technical background [0002] The chemical name of lonidamine (English name: Lonidamine) is 1-(2,4-dichlorophenyl) H-indazole-3-carboxylic acid. Molecular formula C 15 h 10 Cl 2 N 2 o 2 , molecular weight: 321.16, has the following chemical structure: [0003] [0004] Lonidamine is a dichlorobenzene derivative of indazole acid, which has an antibiotic effect, and was later found to have anticancer activity against Lewis lung cancer and S-180 in mice. Lonidamine can change the strong mitochondrial structure of tumor cells, inhibit the aerobic metabolism of sugar, reduce oxygen consumption, and affect the energy metabolism of tumor cells. [0005] According to the patent of Hangzhou Minsheng Pharmaceutical Industry (applicatio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/416A61K47/34A61P35/00A61K47/10A61K47/26A61K47/38
Inventor 史为民操锋陈祎楠陈曦
Owner CHANGZHOU RUIMING PHARMA
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