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Spinosin solid lipid nanoparticles and its preparation method and application

A technology of solid lipid nano and lipid materials, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients. Restrict the development and application of problems, achieve the effect of low equipment requirements, improve oral bioavailability, and improve bioavailability

Inactive Publication Date: 2015-10-28
TIANJIN UNIV OF COMMERCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of spinosin is small, the dissolution rate is slow, and the absorption is low, thus greatly affecting its bioavailability (absolute bioavailability is only 2.2%), thus limiting its further clinical development and application

Method used

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  • Spinosin solid lipid nanoparticles and its preparation method and application
  • Spinosin solid lipid nanoparticles and its preparation method and application
  • Spinosin solid lipid nanoparticles and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Weigh the lipid material carrier and spinosin into a round-bottomed flask, add 25mL of dichloromethane for ultrasonic dissolution, and evaporate to dryness under reduced pressure at 40°C to form a uniform transparent film. Wherein, the lipid material carrier is glycerol monostearate and lecithin, and the mass ratio of spinosin to lipid material is 1:20. In the lipid material carrier, the mass ratio of glyceryl monostearate to lecithin is 1:1, and the total mass of glyceryl monostearate and lecithin is 900 mg.

[0029] (2) Add 20mL of poloxamer 188 aqueous solution with a concentration of 1.0% to the film, hydrate it, and disperse it ultrasonically at 45KHz for 20min to obtain a dispersion.

[0030] (3) Pass the dispersion liquid through a 0.22 μm microporous membrane to obtain spinosin solid lipid nanoparticles.

Embodiment 2

[0032] (1) Weigh the lipid material carrier and spinosin into a round-bottomed flask, add 25 mL of dichloromethane for ultrasonic dissolution, and evaporate to dryness under reduced pressure at 30°C to form a uniform transparent film. Wherein, the lipid material carrier is glyceryl monostearate and lecithin, the mass ratio of drug spinosin and lipid material is 1:25, the mass ratio of glyceryl monostearate and lecithin is 1:3, Wherein the total mass of glyceryl monostearate and lecithin is 900mg.

[0033] (2) Add 20mL of poloxamer 188 aqueous solution with a concentration of 1.60% to the film, hydrate it, and disperse it ultrasonically at 45KHz for 40min.

[0034] (3) Pass the dispersion liquid through a 0.22 μm microporous membrane to obtain spinosin solid lipid nanoparticles.

Embodiment 3

[0036] (1) Weigh the lipid material carrier and spinosin into a round-bottomed flask, add 25mL of dichloromethane for ultrasonic dissolution, and evaporate to dryness under reduced pressure at 40°C to form a uniform transparent film. Wherein, the lipid material carrier is glyceryl monostearate and lecithin, the mass ratio of spinosin and lipid material is 1:10, the mass ratio of glyceryl monostearate and lecithin is 1:2.5, and the single The total mass of glyceryl stearate and lecithin is 900mg.

[0037] (2) Add 20mL of poloxamer 188 aqueous solution with a concentration of 1.50% to the film, hydrate it, and disperse it ultrasonically at 45KHz for 20min.

[0038] (3) Pass the dispersion liquid through a 0.22 μm microporous membrane to obtain spinosin solid lipid nanoparticles.

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Abstract

The invention discloses spinosin solid lipid nanoparticles and a preparation method and application thereof. Spinosin is taken as a medicinal material, a lipid material is taken as a carrier, and the mass ratio of spinosin to the lipid material carrier is 1:(10-40); the lipid material carrier consists of glycerin monostearate and lecithin. The preparation method comprises the following steps: adding methylene dichloride into spinosin and the lipid material carrier, ultrasonically dissolving, and rotationally evaporating to dryness under reduced pressure to form a uniform and transparent film; adding a surfactant into the obtained film, and ultrasonically dispersing to obtain dispersion liquid; making the dispersion liquid pass through a micro-porous filter membrane of 0.22 micron to obtain spinosin solid lipid nanoparticles. Spinosin is prepared into spinosin solid lipid nanoparticles by taking the lipid material as the carrier, the bioavailability of spinosin can be enhanced greatly, the release of medicaments is better controlled, and medicament degradation is avoided, so that clinical application of spinosin becomes possible.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a spinosin solid lipid nanoparticle and its preparation method and application. Background technique [0002] Suanzaoren is the dry and mature seed of Ziziphus jujuba, a plant of Rhamnaceae, which has the effects of suppressing sweat, nourishing the liver, calming the mind and calming the nerves, especially the effect of calming the nerves. Modern studies have shown that Chinese jujube seed has sedative, hypnotic, analgesic, anticonvulsant and other effects, and is the first choice for nourishing the heart and calming the nerves. Among all kinds of traditional Chinese medicine preparations for the treatment of insomnia, the jujube seed is the most commonly used component. [0003] Suanzaoren flavonoids are the main active ingredients in the sedative and hypnotic effects of Suanzaoren. Numerous pharmacological studies have shown that Suanzaoren flavonoids can s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/7048A61K47/24A61K47/14A61P25/20
Inventor 张彦青解军波张婷马桂劼
Owner TIANJIN UNIV OF COMMERCE