Breviscapine composition nano-particle and preparation method thereof

A breviscapine and nanoparticle technology, applied in the field of medicine, can solve the problems of reducing the effect of micronization, large surface free energy of the drug, neglecting the microstructure of the product, etc., and achieves high drug loading, in vivo bioavailability improvement, solvent remove full effect

Inactive Publication Date: 2014-04-02
NANJING DACHUANG BIOLOGICAL SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the surface free energy of the micronized drug is large, and there is a tendency to spontaneously coalesce, which will reduce the effect of micronization
At the same time, the preparation of solid dispersion by the traditional solvent method ignores the investigation of the microstructure of the product, and the viscosity of the remaining solvent increases with the evaporation under reduced pressure, which may lead to solvent residue and drug precipitation crystals

Method used

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  • Breviscapine composition nano-particle and preparation method thereof
  • Breviscapine composition nano-particle and preparation method thereof
  • Breviscapine composition nano-particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Mix breviscapine (33%), polyethylene glycol 40 hydrogenated castor oil (5%), copovidone (42%), polyacrylic acid resin (20%), stir in absolute ethanol for 2 hours at room temperature to dissolve , the mass volume fraction of the polymer is 6%, and when the solution is clear, it is transferred to the needle tube, the needle diameter is 0.5mm, the ambient temperature is 25°C, the humidity is controlled below 40%, and the pushing speed of the push pump is 4mL / h. The distance is 20cm, and 15kV high-voltage static electricity is applied between the needle and the steel plate for electrostatic spraying, and the obtained nanoparticles are collected on the steel plate. The obtained breviscapine composition nanoparticles were vacuum-dried for 1 h to completely remove the solvent.

Embodiment 2

[0032] Mix breviscapine (55%), vitamin E polyethylene glycol succinate (10%), copovidone (15%), and polyacrylic resin (20%), stir in absolute ethanol for 2 hours at room temperature to dissolve , the mass volume fraction of the polymer is 6%, when the solution is clear, transfer it to the needle tube, the needle diameter is 0.8mm, the ambient temperature is 25°C, the humidity is controlled below 40%, and the push speed of the push pump is 2mL / h. The distance is 20cm, and 15kV high-voltage static electricity is applied between the needle and the steel plate for electrostatic spraying, and the obtained nanoparticles are collected on the steel plate. The obtained breviscapine composition nanoparticles were vacuum-dried for 1 h to completely remove the solvent.

Embodiment 3

[0034] Breviscapine (40%), poloxamer 188 (8%), copovidone (40%), polyacrylic acid resin (12%) were mixed, and mixed solvents of absolute methanol and absolute ethanol (1 / 1. Stir at room temperature for 2 hours in V / V) to dissolve. The mass volume fraction of the polymer is 8%. When the solution is clear, transfer it to a needle tube with a needle diameter of 0.5mm. The ambient temperature is 25°C and the humidity is controlled at 40%. Next, the push speed of the push pump is 2mL / h, the receiving distance is 20cm, and 19kV high-voltage static electricity is applied between the needle and the steel plate for electrostatic spraying, and the obtained nanoparticles are collected on the steel plate. The obtained breviscapine composition nanoparticles were vacuum-dried for 1 h to completely remove the solvent.

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Abstract

The invention belongs to the field of pharmacy, and relates to a breviscapine composition nano-particle and a preparation method thereof. The provided novel breviscapine composition nano-particle is prepared by a solution containing the breviscapine, a polymer, a surfactant and a solvent with the adoption of an electrostatic spraying technology. The composition preparation device is simple, the parameters are controllable, the drug loading capacity is high, , the direct and continuous nano-particles with uniform particle size distribution can be obtained, the specific surface area is increased, and the dissolution in vitro and bioavailability of the breviscapine are improved remarkably.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to the preparation of a novel nanoparticle of scutellarin composition. The present invention particularly relates to the key step of preparing nano-particles of scutellarin composition by electrostatic spraying technology. Background technique [0002] Breviscapine is the extract of the dried whole herb of Asteraceae breviscapita, the main component is scutellarin, the structural formula is 4,5,6-trihydroxyflavone-7-gluconoside, which has the effect of improving cardiovascular and cerebrovascular blood Blood flow, anti-platelet aggregation, anti-oxidative free radicals, etc., are mainly used clinically to treat cerebral insufficiency, cerebral thrombosis, coronary heart disease and other diseases. Breviscapine belongs to Class II drugs of the Biopharmaceutics Classification System (BSC). The rate-limiting steps of this type of drug absorption in the body are the dissolution and disso...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/7048A61K47/32A61J3/02A61P9/10A61P7/02
Inventor 柯学
Owner NANJING DACHUANG BIOLOGICAL SCI & TECH CO LTD
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