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Waterless reverse micelles nanoparticles of water-soluble drug, and preparation method of suspension aerosol thereof

A technology for suspension-type aerosols and water-soluble drugs, applied in the field of biomedicine, can solve the problems of consuming a large amount of energy, destroying and degrading the molecular structure of drugs, and reducing the effect of reducing drug loss, facilitating storage and reducing energy consumption.

Active Publication Date: 2013-09-04
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, there are also some defects in nanotechnology at present: as using high-energy grinding to disperse or high-speed shear homogenization to reduce the particle size of the drug, it may cause damage to the molecular structure of the drug; for example, the preparation method of Nyambura et al. uses methanol, dichloromethane Or chloroform and other toxic solvents with low freezing point, the process of freeze-drying to remove the solvent will consume a lot of energy

Method used

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  • Waterless reverse micelles nanoparticles of water-soluble drug, and preparation method of suspension aerosol thereof
  • Waterless reverse micelles nanoparticles of water-soluble drug, and preparation method of suspension aerosol thereof
  • Waterless reverse micelles nanoparticles of water-soluble drug, and preparation method of suspension aerosol thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of blank lipid vesicles

[0039] The preparation method of blank lipid vesicles comprises the following steps:

[0040] Use ultrapure water as the water phase, and dissolve the amphiphilic substance soybean lecithin in tert-butanol, and the resulting solution with a concentration of 5% (w / v) is used as the oil phase. Add dropwise into ultrapure water, the volume ratio of the water phase to the oil phase is 8:1, pass through a 220nm organic filter membrane to segregate and remove bacteria at the same time to obtain a blank lipid vesicle suspension. From the above, it can be seen that by using this method, a lipid vesicle structure with a uniform particle size can be prepared in one step.

[0041] Adopt the Malvem Zetasizer Nano ZS90 of British Malvern Company to measure the particle size and distribution of the obtained blank lipid vesicles by dynamic light scattering method, the results are as follows Figure 1-A : As can be seen from this figure,...

Embodiment 2

[0042] Example 2 Preparation of salbutamol sulfate lipid vesicles

[0043] The preparation method of salbutamol sulfate lipid vesicle, comprises the steps:

[0044] Dissolve 8 mg of the water-soluble drug salbutamol sulfate in ultrapure water as the water phase, and dissolve the amphiphilic substance egg yolk phospholipid in tert-butanol, and the resulting solution with a concentration of 20% (w / v) is used as the oil phase, and put it in a water bath at 40°C , under the condition of magnetic stirring 1000rpm, add the oil phase into the water phase drop by drop, the volume ratio of the water phase and the oil phase is 4:1, pass through a 220nm organic filter membrane to granulate and remove bacteria at the same time, to obtain salbutamol sulfate lipid vesicle suspension liquid.

[0045] Adopt the Malvem Zetasizer Nano ZS90 of British Malvern Company to carry out the measurement of particle size and distribution to the obtained salbutamol sulfate lipid vesicles by dynamic light...

Embodiment 3

[0046] Example 3 Preparation of lysozyme lipid vesicles

[0047] A method for preparing lysozyme lipid vesicles, comprising the steps of:

[0048](1) Dissolve 4 mg of water-soluble drug lysozyme and 2 mg of lyoprotectant lactose in ultrapure water as the water phase, and dissolve the amphiphilic substance phosphatidylcholine in tert-butanol to obtain a concentration of 10% (w / The solution of v) is used as the oil phase. Under the condition of a water bath at 35°C and magnetic stirring at 1200rpm, the oil phase is dropped into the water phase. The volume ratio of the water phase to the oil phase is 5:1. The lysozyme lipid vesicle suspension was obtained.

[0049] The particle size and distribution of the obtained lysozyme lipid vesicles were measured using a Malvem Zetasizer Nano ZS90 from Malvern, UK, using the dynamic light scattering method. The average particle size was 166.0±9.0 nm, and the polydispersity coefficient PI was 0.14±0.06. Comparing Example 1 and Example 3, ...

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Abstract

The invention discloses waterless reverse micelles nanoparticles of a water-soluble drug, and a preparation method of a suspension aerosol thereof. The preparation method comprises the following steps: dissolving the water-soluble drug and a freeze-drying protectant into water as an aqueous phase; dissolving amphiphilic substances into tert-butyl alcohol as an oil phase, stirring uniformly in a water bath at a constant temperature, adding dropwise the oil phase into the aqueous, getting a nano suspension with a bilayer vesicles structure; freezing the nano suspension rapidly and solidifying, getting a freeze-drying product; adding an organic phase into the freeze-drying product, and getting the waterless reverse micelles nanoparticles; filling a spray bottle with the nanoparticles and nitrogen, sealing, pressing a propellent into the spray bottle, and getting the suspension aerosol. The preparation method of the invention helps to prepared the nanoparticles with a lipid vesicle structure in uniform particle size by one step, and the drug molecules are not easy to damage; and by taking tert-butyl alcohol / water as a solvent, energy consumption in the freeze-drying process is reduced, solvent sublimation is accelerated, and freeze-drying time is shortened. The nanoparticle suspension aerosol is high in sedimentation rate in vitro of pulmonary delivery, and helps to improve drug absorption.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a method for preparing a water-soluble drug anhydrous reverse micellar nanoparticle and a suspension aerosol thereof. Background technique [0002] At present, water-soluble drugs are usually dissolved in water. However, for some water-sensitive water-soluble drugs, the presence of water molecules will lead to the instability of their physical or chemical properties. For example, biomolecules such as proteins, polypeptides, nucleic acids, and vaccines are often inactivated by hydrolysis. In order to eliminate the destabilizing effects of water, Roger R.C. New et al took the lead in using amphiphilic molecules to coat the protein surface to form an anhydrous reversed-phase micellar system, solubilize the protein in the oil phase, and obtain a protein oral oil solution , the method is Macrosol technology. [0003] Due to the oral absorption and degradation of protein and poly...

Claims

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Application Information

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IPC IPC(8): A61K47/10A61K9/51A61K9/12A61K9/16
Inventor 吴传斌吴涵潘昕
Owner SUN YAT SEN UNIV
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