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Amoitone B nano crystallization preparation and preparation method thereof

A nano-crystal and derivative technology, applied in the field of doxorubicin derivative Amoitone B nano-crystalline preparation and preparation thereof, and the field of doxorubicin-derivative nano-crystalline preparation and preparation thereof, can solve the problem of insolubility and poor absorption, and cannot be directly injected Or oral administration, etc., to achieve the effect of improving solubility and dissolution rate, controllable particle size and good dispersibility

Inactive Publication Date: 2013-05-08
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to overcome the insoluble and poor absorption of Amoitone B, can not direct injection or oral administration etc., and provide a kind of Adriamycin derivative nanocrystal preparation and preparation method thereof, this preparation can significantly improve the Amoitone B Solubility and dissolution rate, improve bioavailability, high efficiency, low toxicity, good stability

Method used

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  • Amoitone B nano crystallization preparation and preparation method thereof
  • Amoitone B nano crystallization preparation and preparation method thereof
  • Amoitone B nano crystallization preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Weigh 0.2g Amoitone B, 0.2g poloxamer, and 0.2g lecithin and dissolve them in 80ml of water for injection (water for injection is the double distilled water specified in the Pharmacopoeia). After ultrasonication for 15min, coarsely disperse under the action of a high-speed shearing machine at 20000rpm for 3 ~5min, disperse 3 times, and then go through a high-pressure micro-jet homogenizer, first homogenize 3 times under 500bar and 1000bar pressure as pre-dispersion, and then homogenize 15 times under 1800bar pressure to get Amoitone B nano crystal mixture Suspension.

[0045] Take the above suspension and add mannitol at a ratio of 5% (w / v, g / ml), stir and dissolve, then pack into vials according to 2-4mL / bottle, freeze at -80°C for 24 hours in an ultra-low temperature refrigerator, and take it out quickly Vacuum freeze-dry at -50°C for 48h. After the freeze-drying is completed, take out the package with the pressurized aluminum cover to obtain the Amoitone B nano-crys...

Embodiment 2

[0049] Weigh 0.2g of Amoitone B, 0.1g of lecithin, and 0.1g of HPMC and dissolve them in 80ml of water for injection. After ultrasonication for 15 minutes, coarsely disperse for 3 to 5 minutes under the action of a high-speed shearing machine at 20,000 rpm, disperse for 3 times, and then pass through a high-pressure micro-jet homogenizer , first homogenized 3 times under the pressure of 500bar and 1000bar as pre-dispersion, and then homogenized 15 times under the pressure of 1800bar to obtain the Amoitone B nano crystal suspension.

[0050] Take the above suspension and add mannitol at a ratio of 5% (w / v, g / ml), stir and dissolve, then pack into vials according to 2-4mL / bottle, freeze at -80°C for 24 hours in an ultra-low temperature refrigerator, and take it out quickly Vacuum freeze-dry at -50°C for 48h. After the freeze-drying is completed, take out the package with the pressurized aluminum cover to obtain the Amoitone B nano-crystal preparation.

Embodiment 3

[0052] Weigh 0.2g of Amoitone B, 0.2g of poloxamer, and 0.1g of HPMC and dissolve them in 80ml of water for injection. After ultrasonication for 15 minutes, coarsely disperse them under the action of a high-speed shear at 20,000rpm for 3 to 5 minutes. Jet homogenizer, first homogenize 3 times under 500bar and 1000bar pressure as pre-dispersion, and then homogenize 15 times under 1800bar pressure to get Amoitone B nano crystal suspension.

[0053] Take the above suspension and add mannitol at a ratio of 5% (w / v, g / ml), stir and dissolve, then pack into vials according to 2-4mL / bottle, freeze at -80°C for 24 hours in an ultra-low temperature refrigerator, and take it out quickly Vacuum freeze-dry at -50°C for 48h. After the freeze-drying is completed, take out the package with the pressurized aluminum cover to obtain the Amoitone B nano-crystal preparation.

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Abstract

The invention relates to an Amoitone B nano crystallization preparation and a preparation method thereof. The adriamycinone derivative nano crystallization preparation comprises raw material drug Amoitone B, stabilizers and a cryoprotectant. The stabilizers include a surfactant and a high polymer suspending agent. The preparation method is a high pressure micro jet method. The Amoitone B nano crystallization preparation provided by the invention can be used for obviously improving the solubility and the dissolution rate of the Amoitone B and implementing uniform controllability of the particle size in the range of 200 to 1,000 nm by controlling the prescription ratio and micro jet homogeneous parameters and has the advantages of good biocompatibility, easiness in degrading, high stability, high efficiency and low toxicity, passive targeted transmission and the like. A carrier and an organic solvent are not contained in the prescription of the Amoitone B nano crystallization preparation, so that the Amoitone B nano crystallization preparation has high administration safety when being used for intravenous injection and can be developed into an oral preparation to improve the bioavailability. The high pressure micro jet method is simple in preparation process, good in reproducibility and stable and is convenient to industrial mass production.

Description

technical field [0001] The invention relates to a doxorubicinone derivative nanocrystal preparation and a preparation method thereof, in particular to a doxorubicinone derivative Amoitone B nanocrystal preparation and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] There is a kind of nuclear receptor (nuclear receptor) with gene regulation function in the nucleus of human cells. Since its physiological ligand has not been found for a long time, it is called orphan receptor (orphan receptor). Nuclear receptor acts as a ligand to activate transcription factors. , regulate the expression of target genes, and affect many physiological functions of the body. Nur77 (NR4A1, also known as TR3, NGFI-B), as a member of the orphan nuclear receptor subfamily NR4A, is a product of an immediate early gene, which can be detected by serum, epidermal growth factor, nerve growth factor, platelet growth factor, etc. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/216A61K47/32A61K47/34A61K47/36A61K47/38A61P35/00
Inventor 张典瑞郝蕾蕾张连茹徐庆妍胡志钰王飞虎李彩云郭和坚
Owner SHANDONG UNIV
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