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Zanamivir solid lipid nanosphere oral preparation and preparation method thereof

A kind of solid lipid nanometer and lipid material technology, applied in the field of new pharmaceutical dosage forms

Inactive Publication Date: 2011-04-27
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Before this patent was declared, there was no oral zanamivir preparation on the market or research on solid lipid nanoparticles at home and abroad

Method used

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  • Zanamivir solid lipid nanosphere oral preparation and preparation method thereof
  • Zanamivir solid lipid nanosphere oral preparation and preparation method thereof
  • Zanamivir solid lipid nanosphere oral preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Embodiment 1: Preparation of blank nanoparticles

[0021] Take 0.2ml of distilled water (inner water phase) and add it to 1ml of the oil phase. After being dispersed by a disperser, put it in an ultrasonic cell pulverizer for 200w and 60s to form W / O colostrum. Then add colostrum into 4ml of Proxamer 188 solution (1.6% w / v, external water phase), after being dispersed by a disperser, put it in an ultrasonic cell pulverizer at 200w, 30s and form W / O / W Double milk. The prepared double emulsion was placed on a magnetic stirrer at 25° C., 700 rpm, and stirred for 5 hours to evaporate the organic solvent to obtain a nanosuspension. For the oil phase, 120 mg of glyceryl monostearate and 40 mg of soybean lecithin were melted in 1 ml of dichloromethane, and mixed thoroughly to obtain a uniform oil phase. Add 5% mannitol to the nanosuspension as a freeze-drying protective agent, set the shelf temperature to -30°C, and vacuum degree to 0.1mbar. After pre-freezing in a -70°C ref...

Embodiment 2

[0022] Embodiment 2: Preparation of blank nanoparticles

[0023] Take 0.2ml of distilled water (inner water phase) and add it to 1ml of the oil phase. After being dispersed by a disperser, put it in an ultrasonic cell pulverizer for 200w and 60s to form W / O colostrum. Then add colostrum into 8ml of Proxamer 188 solution (1.6% w / v, external water phase), after being dispersed by a disperser, put it in an ultrasonic cell pulverizer at 200w and 30s to form W / O / W Double milk. The prepared double emulsion was placed on a magnetic stirrer at 25° C., 700 rpm, and stirred for 5 hours to evaporate the organic solvent to obtain a nanosuspension. For the oil phase, 120 mg of glyceryl monostearate and 40 mg of soybean lecithin were melted in 1 ml of dichloromethane, and mixed thoroughly to obtain a uniform oil phase.

Embodiment 3

[0024] Embodiment 3: Preparation of blank nanoparticles

[0025]Take 0.2ml of distilled water (inner water phase) and add it to 1ml of the oil phase. After being dispersed by a disperser, put it in an ultrasonic cell pulverizer for 200w and 60s to form W / O colostrum. Then add colostrum into 12ml of Proxamer 188 solution (1.6% w / v, external water phase), after being dispersed by a disperser, put it in an ultrasonic cell pulverizer at 200w, 30s and form W / O / W Double milk. The prepared double emulsion was placed on a magnetic stirrer at 25° C., 700 rpm, and stirred for 5 hours to evaporate the organic solvent to obtain a nanosuspension. For the oil phase, 120 mg of glyceryl monostearate and 40 mg of soybean lecithin were melted in 1 ml of dichloromethane, and mixed thoroughly to obtain a uniform oil phase.

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Abstract

The invention provides a zanamivir solid lipid nanosphere oral preparation and a preparation method thereof. In the method, medicinal solution with different concentrations is used as inner water phases, dichloromethane in which glycerin monostearate / granulesten mixture is melted serves as an oil phase, and poloxamer 188 solution is used as an outer water phase so as to prepare the solid lipid nanosphere suspension or a free-dried preparation by a water-in-oil-in-water (W / O / W) composite emulsion solvent volatilization method. Solid lipid nanospheres prepared by the method have round shapes, the particle diameter of between 150 and 500nm, the surface potential of between -45 and -55mV, the entrapment rate of over 30 percent and release rate of more than 80 percent. The method is reliable and is easy and convenient to operate, the prepared solid lipid nanospheres can promote oral absorption of medicaments, and improve bioavailability, and the compliance of patients.

Description

technical field [0001] The invention relates to the field of new drug dosage forms, in particular to a solid lipid nanoparticle of an influenza virus neuraminidase (NA) inhibitor-zanamivir and a preparation method thereof. Background technique [0002] Influenza (abbreviated as influenza) is an acute respiratory infectious disease caused by influenza virus, which seriously endangers human health and life. In the United States alone, there are 20,000 to 25,000,000 visits to a doctor due to influenza, 20,000 deaths, and an economic loss of 3 to 5 billion U.S. dollars each year. According to GlaxoWellcome, the annual cost of treating the flu is about $120 million. It can be seen that influenza, as a viral infectious disease, not only seriously threatens public health, but also brings a heavy economic burden to the country and society. The recent emergence of H1N1 new mutant type A influenza has made people realize the necessity and urgency of developing anti-influenza drugs. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/14A61K9/19A61K31/351A61P31/16
Inventor 曹青日崔京浩
Owner SUZHOU UNIV
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