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Plagiochin nanocrystal preparation and preparation method thereof

A technology of nano-crystallization and patinol, which is applied in the direction of pharmaceutical formulations, antifungal agents, medical preparations of non-active ingredients, etc., to achieve the effects of increasing curative effect, improving in vitro solubility, and good biocompatibility

Inactive Publication Date: 2012-07-04
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the absence of relevant reports in the prior art, a pallassin nanoparticle with good curative effect, good biocompatibility, high bioavailability, stable system, suitable for large-scale industrial production, and low cost has been developed. Crystallization preparations and preparation methods are difficult, requiring creative work, a large number of tests and condition screening

Method used

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  • Plagiochin nanocrystal preparation and preparation method thereof
  • Plagiochin nanocrystal preparation and preparation method thereof
  • Plagiochin nanocrystal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1: Preparation of nano-crystal preparation of palladium

[0045] Weigh 0.5g papadone, 0.5g poloxamer, 0.1g PVP K 30 Dissolved in 80ml of water for injection, ultrasonicated for 40min, then passed through a high-pressure micro-jet nano-disperser, first homogenized twice under the pressure of 30*233psig and 50*233psig as pre-dispersion, and then homogenized under the pressure of 100*233psig for 10 times, you can get the palladium nanocrystal suspension.

[0046] Take the above suspension and add mannitol according to the ratio of 5% (w / v, g / ml), stir and dissolve, divide into vials according to 2mL / bottle, put it into the ultra-low temperature refrigerator quickly, and freeze it at -80°C for 24 hours , and then take it out and quickly put it on the shelf of the freeze dryer whose temperature has dropped to -50°C, cover with a vacuum cover, turn on the vacuum pump switch, and freeze-dry for 48 hours. After the freeze-drying is completed, take it out and pack i...

Embodiment 2

[0048] Embodiment 2: Preparation of nano-crystal preparation of palladium

[0049] Weigh 0.2g patinol, 0.2g poloxamer, 0.04g PVP K 30 Dissolved in 50ml of water for injection, ultrasonicated for 40min, and then passed through a high-pressure micro-jet nano-disperser, first homogenized twice under the pressure of 30*233psig and 50*233psig as pre-dispersion, and then homogenized under the pressure of 100*233psig for 10 times, you can get the palladium nanocrystal suspension.

[0050] Take the above suspension and add mannitol according to the ratio of 5% (w / v, g / ml), stir and dissolve, divide into vials according to 2mL / bottle, put it into the ultra-low temperature refrigerator quickly, and freeze it at -80°C for 24 hours , and then take it out and quickly put it on the shelf of the freeze dryer whose temperature has dropped to -50°C, cover with a vacuum cover, turn on the vacuum pump switch, and freeze-dry for 48 hours. After the freeze-drying is completed, take it out and pa...

Embodiment 3

[0051] Embodiment 3: Preparation of nano-crystal preparation of pabasporin

[0052] Weigh 1.0g papelin, 1.0g lecithin, 0.2g PVP K 30 Dissolved in 50ml of water for injection, ultrasonicated for 40min, and then passed through a high-pressure micro-jet nano-disperser, first homogenized twice under the pressure of 30*233psig and 50*233psig as pre-dispersion, and then homogenized under the pressure of 100*233psig for 10 times, you can get the palladium nanocrystal suspension.

[0053] Take the above suspension and add sucrose according to the ratio of 5% (w / v, g / ml), stir and dissolve, then pack into vials according to 2mL / bottle, put it into an ultra-low temperature refrigerator quickly, and freeze it at -80°C for 24 hours. Then take it out and quickly put it on the shelf of the lyophilizer whose temperature has dropped to -50°C, cover the vacuum cover, turn on the vacuum pump switch, and freeze-dry for 48 hours. After the freeze-drying is completed, take it out and pack it wit...

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Abstract

The invention discloses plagiochin nanocrystal preparation and a preparation method thereof, belonging to the field of pharmaceutic preparation. The plagiochin nanocrystal preparation consists of plagiochin and a stabilizing agent or a freeze-drying protective agent, wherein the stabilizing agent comprises a surface active agent and a suspending agent. All the ingredients are as follows: 0.01-2.0g of the plagiochin, 0.01-2.0g of the surface active agent, 0.002-0.5g of the suspending agent, and 0 or 1-10g of freeze-drying protective agent, when the plagiochin nanocrystal preparation is prepared, a micro jet flow high-pressure homogeneity method is adopted. The plagiochin nanocrystal preparation prepared by the invention can play a release role in a body, so that the dissolving degree of the plagiochin can be increased greatly, the particle size of the plagiochin is about 500mm, the curing effect can be improved greatly due to the increasing of the content of the plagiochin, the bioavailability of the plagiochin is improved, and the plagiochin nanocrystal preparation has the advantages that the biocompatibility is good, the degradation is easy, the bioavailability is high, the target transmission can be realized and the like.

Description

technical field [0001] The invention relates to a nano-crystal preparation of papadin and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] In recent years, the incidence of fungal infection has been increasing year by year. The main reasons include the abuse of broad-spectrum antibiotics, HIV infection, cancer chemotherapy and immunosuppression caused by organ transplantation. Especially in patients with persistent immunodeficiency, the rate of fungal infection is very high. Azole drugs, especially fluconazole (FCZ), are widely used clinically because of their exact course of treatment and good tolerance. However, with the high-dose and long-term use of fluconazole, the drug resistance rate of Candida albicans and non-Candida infections has increased significantly, and clinical treatment failures have increased day by day. Therefore, the research, development and application of new and effective antifungal d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/335A61K47/32A61K47/36A61K47/38A61P31/10
Inventor 娄红祥张典瑞刘光璞郑丹丹王莉宁
Owner SHANDONG UNIV
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