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Preparation method for hypericin albumin nanometer particles

A technology of hypericin and nanoparticles, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, freeze-dried transportation, etc., and can solve the problem of low content of active ingredients of hypericin and failure to meet the requirements of terminal product development , Hypericin is unstable to light and heat, and achieves the effects of improving bioavailability, high drug loading and encapsulation efficiency, and rounded surface

Active Publication Date: 2013-07-17
GUANGDONG HINAPHARM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the instability of hypericin to light and heat, the content of active ingredients of hypericin on the market is extremely low, which is far from meeting the requirements of terminal product development

Method used

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  • Preparation method for hypericin albumin nanometer particles
  • Preparation method for hypericin albumin nanometer particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Accurately weigh 2.0 g of albumin and dissolve it in 98 ml of distilled water to make a carrier solution, weigh 4.0 g of HY and dissolve it in 96 ml of absolute ethanol to make an oil phase. rpm / min~1000 rpm / min), add 5 ml of oil phase dropwise to 50 ml carrier solution, fully emulsify and adjust PH=9, continue to add 20 ml of absolute ethanol dropwise at 0.5 ml / min, stir well for 2 h, solidified with glutaraldehyde for 24 h, centrifuged at 15,000 rpm / min for 15 min at high speed, washed 3 times, freeze-dried, and collected to obtain milky white hypericin albumin nanoparticles with an average particle size of 120 nm and a drug loading capacity of 4.12% , encapsulation efficiency 71.43%. The prepared hypericin albumin and ordinary hypericin were placed under fluorescent lamps, and their contents were measured on the 0th day, the 3rd day, the 5th day, and the 7th day respectively. It was found that the ordinary hypericin content The 3rd day decreased by 25.43%, the 5th d...

Embodiment 2

[0027] Accurately weigh 2.0 g of albumin and dissolve it in 98 ml of distilled water to make a carrier solution, weigh 4.0 g of HY and dissolve it in 96 ml of absolute ethanol to make an oil phase. rpm / min~1000 rpm / min), add 5 ml of the oil phase dropwise to 50 ml carrier solution, fully emulsify and adjust the PH=9, continue to add 20 ml of absolute ethanol dropwise at 1.0 ml / min, stir well for 2 h, solidified with glutaraldehyde for 24 h, centrifuged at 15,000 rpm / min for 15 min at high speed, washed 3 times, freeze-dried, and collected to obtain milky white hypericin albumin nanoparticles with an average particle size of 60 nm and a drug loading capacity of 4.54% , encapsulation efficiency 74.78%. The prepared hypericin albumin and ordinary hypericin were placed under fluorescent lamps, and their contents were measured on the 0th day, the 3rd day, the 5th day, and the 7th day respectively. It was found that the ordinary hypericin content The third day decreased by 26.17%, ...

Embodiment 3

[0029] Accurately weigh 2.0 g of albumin and dissolve it in 98 ml of distilled water to make a carrier solution, weigh 4.0 g of HY and dissolve it in 96 ml of absolute ethanol to make an oil phase. rpm / min~1000 rpm / min), add 5 ml of the oil phase dropwise to 50 ml carrier solution, fully emulsify and adjust PH=9, continue to add 20 ml of absolute ethanol dropwise at 2.0 ml / min, stir well for 2 h, solidified with glutaraldehyde for 24 h, centrifuged at 15,000 rpm / min for 15 min at high speed, washed 3 times, freeze-dried, and collected to obtain milky white hypericin albumin nanoparticles with an average particle size of 100 nm and a drug loading capacity of 4.23% , encapsulation efficiency 72.39%. The prepared hypericin albumin and ordinary hypericin were placed under fluorescent lamps, and their contents were measured on the 0th day, the 3rd day, the 5th day, and the 7th day respectively. It was found that the ordinary hypericin content The 3rd day decreased by 26.43%, the 5...

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Abstract

The invention discloses a preparation method for hypericin albumin nanometer particles, which comprises (1) using bovine serum albumin as a carrier material to be dissolved in distilled water to manufacture carrier solution with the mass concentration of 10% to 40%; (2) dissolving hypericin in ethanol with the concentration more than 95% to produce oil phase with the mass concentration of 20% to 40%; (3) adding the oil phase having been fully stirred into the carrier solution, adjusting potential of hydrogen (PH) to 9, dropwise adding emulsifier to fully emulsify, then dropping glutaraldehyde to cure for more than 24 hours, and obtaining curing nanometer particle solution; (4) centrifuging at high speed of 15,000 rpm / min to 20,000 rpm / min, removing supernate, adding distilled water to perform ultrasonic dispersion, centrifuging again at high speed, removing supernate, washing with water and collecting, and drying in vacuum or freezing mode to achieve hypericin albumin nanometer particles. The hypericin albumin nanometer particles prepared with the method are good in stability on light and heat, and effective content of hypericin is improved.

Description

technical field [0001] The invention relates to an antiviral natural medicine, in particular to a preparation method of hypericin albumin nanoparticles. Background technique [0002] Hypericin (Hypericin, HY) is a naphthalene dianthrone compound extracted from Hypericum perforatum Linn., a plant of the Clusiaceae family, and is considered to be the most biologically active substance in the extract of Hypericum perforatum , has photosensitizing activity and photoaction, and can be applied to the photochemical diagnosis and treatment of tumors. In addition to antidepressant and antitumor activities, hypericin also has antiviral and immune enhancing effects. However, due to the instability of hypericin to light and heat, the content of active ingredients of hypericin in the market is extremely low, which is far from meeting the requirements of terminal product development. [0003] Nano-drugs refer to the drugs made of nano-scale polymer nanoparticles (nanoparticles, NP), nan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/19A61K47/42A61K31/122A61P31/12
Inventor 梁剑平胡小艳陶蕾王学红刘宇尚若峰赫宝成华兰英
Owner GUANGDONG HINAPHARM PHARMA CO LTD
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