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Breviscapine-panax notoginseng saponins double-pharmaceutical nano-composite particle and preparation method and application thereof

A technology of nanocomposite particles and Panax notoginseng saponins, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., to achieve the effects of low toxicity, improved solubility, and high bioavailability

Active Publication Date: 2016-10-12
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, there is currently no report on the use of nanotechnology to realize the synergistic drug loading of breviscapine and Panax notoginseng saponins to improve the solubility and bioavailability of breviscapine

Method used

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  • Breviscapine-panax notoginseng saponins double-pharmaceutical nano-composite particle and preparation method and application thereof
  • Breviscapine-panax notoginseng saponins double-pharmaceutical nano-composite particle and preparation method and application thereof
  • Breviscapine-panax notoginseng saponins double-pharmaceutical nano-composite particle and preparation method and application thereof

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Experimental program
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Embodiment 1

[0031] The embodiments of the present invention will be described in detail below in conjunction with specific examples, which are only used to illustrate the present invention, and should not be regarded as limiting the scope of rights of the present invention. For those not marked with specific conditions in the implementation plan, follow the conventional conditions or the conditions suggested by the manufacturer. The reagents or instruments used were not marked with manufacturers, and they were all conventional products that could be purchased from the market. Example 1: Preparation of breviscapine-notoginseng saponins nanocrystal suspension in different average particle size ranges (100nm, 200nm, 500nm, 800nm, 900nm)

[0032] Weigh 0.05g of Panax notoginseng saponins and add 100ml of water to dissolve to obtain a stabilizer solution; then, 0.5g of scutellarin is dispersed in the stabilizer solution, and sheared by high-speed shear emulsification, the rotating speed is: 13...

Embodiment 2

[0038] Example 2: Determination of Saturation Solubility of Breviscapine Nanocrystal Suspensions with Different Particle Sizes

[0039] Dissolution was determined by the paddle method, using 900 mL of pH 7.4 phosphate buffer solution as the dissolution medium, and the speed was 100 r min -1 , the temperature of the water bath is 37 ° C, and the average particle diameter prepared in the above example 1 is 10ml each of 500nm, 600nm, 700nm, 800nm, and 900nm, and the suspension is placed in the dissolution cup for 0.5min and 1min. After 1.5min, 4min, 6min, 10min, 20min, and 30min, 1 mL of sample was taken, filtered through a 0.22 μm microporous membrane, and determined by HPLC. According to the scutellarin standard curve, A=0.0504C+0.0903(R 2 =0.9994), the linear range is 0.36~20 μg / ml, and its dissolution rate is calculated, and its content is shown in Table 1.

[0040] Table 1 Comparison of the dissolution rate of breviscapine nanocrystal suspensions in different particle size ...

Embodiment 3

[0043] Example 3: Preparation of breviscapine-total notoginseng saponins nanocomposite particles

[0044] Experimental method: take the average particle diameter obtained according to the experimental method of Example 1 as 200nm

[0045] Add 1.0g of lactose (protective agent) to disperse and dissolve the sample of the nanocrystal suspension, and then use spray drying and rapid curing technology. The spray drying hot air temperature is 120°C, the air outlet temperature is 60°C, and the peristaltic speed of the pump is 5ml / min. After drying and curing, nanocomposite particle powder of scutellarin and Panax notoginseng saponins can be obtained.

[0046] Add breviscapine and panax notoginseng saponins to redissolve and disperse in an appropriate amount of water, put a drop on a copper grid covered with a carbon film, and dry at room temperature. The morphology of scutellarin nanoparticles was observed by transmission electron microscope, and the results are shown in the attached...

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Abstract

The invention discloses a breviscapine-panax notoginseng saponins double-pharmaceutical nano-composite particle and a preparation method and application thereof, and belongs to the field of pharmaceutical preparations. The nano-composite particle is of a nano-composite particle stable structure which takes a breviscapine nanocrystal as a nucleus and takes panax notoginseng saponins with the pharmacological effect and the natural surface activity attribute as a shell. The preparation method of the nano-composite particle mainly comprises the steps of pharmaceutical mixing, dispersing, high-pressure homogenizing, drying and the like. The nano-composite particle has the advantages that the solubility, the dissolving-out speed and the bioavailability of breviscapine can be significantly increased, collaborative dosing of breviscapine and panax notoginseng saponins is achieved, the pharmaceutical compatibility treatment effect is achieved, the nano-composite particle is conveniently further processed into a preparation form containing the composite particle intermediate, and clinical application is convenient. According to the breviscapine-panax notoginseng saponins double-pharmaceutical nano-composite particle and the preparation method and application thereof, no toxic solvent or synthetic surfactant or macromolecular material is used, the safety is high, the preparation process is simple, industrialization is easy to achieve, and the very good application prospect is achieved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a double-drug nanocomposite particle of breviscapine and panax notoginseng saponins, a preparation method and application thereof. Background technique [0002] Breviscapine is a brass-like active component extracted from the Compositae plant Erigeron breviscapine, and scutellarin accounts for more than 90% of the breviscapine content. Breviscapine has the effects of improving cardio-cerebral blood circulation, increasing cerebral blood flow, reducing vascular resistance and anti-platelet aggregation. Breviscapine is widely used clinically, mainly for cardiovascular and cerebrovascular diseases, such as sequelae caused by occlusive cerebrovascular, paralysis, coronary heart disease, angina pectoris, etc. The clinical preparations of breviscapine are mainly injections, but there are risks of adverse reactions, and cardiovascular and cerebrovascular diseases re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/258A61K9/16A61K47/46A61P9/00A61P9/10A61P7/02A61K31/7048
Inventor 岳鹏飞杨明谢元彪郑琴伍振峰胡鹏翼王雅琪
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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