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Nuciferine microsphere and preparation method thereof

A technology of nuciferine and microspheres, applied in the field of traditional Chinese medicine, can solve the problems of low bioavailability, low oral absorption, poor water solubility, etc., and achieve the effects of good dispersion, less adhesion, and low cost

Active Publication Date: 2014-01-22
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But nuciferine is a kind of lipophilic organic compound with poor water solubility and high oil-water partition coefficient, poor stability, less oral absorption and low bioavailability, which greatly limits its application

Method used

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  • Nuciferine microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Take 0.4g of gelatin, add 4mL of double-distilled aqueous solution (to make a gelatin solution with a weight volume concentration of 10%), swell completely in a warm water bath at 55°C, and then add 0.2g of nuciferine, mix and dissolve (nuciferine in the water phase The weight-volume concentration is 5%); then drop into a beaker filled with 0.6mL Span 80 and 30mL liquid paraffin, stir evenly in a warm water bath at 40°C with a stirring speed of 1000r / min, and turn to milky white after stirring for 20min; Cool quickly in an ice-water bath to below 5°C and continue to stir for 10 minutes, add 3 mL of glutaraldehyde in a trickle and continue to stir for 30 minutes to cross-link and solidify, dehydrate with 30 mL of isopropanol and stir for 15 minutes, then filter with suction; then wash with a little isopropanol to Glutaraldehyde was washed with petroleum ether to remove the liquid paraffin on the surface of the microspheres, and dried in vacuum overnight to obtain microsph...

Embodiment 2

[0034] Take 0.4g of gelatin, add 4mL of 0.9mol / L pH5.0 phosphate buffer solution (to make a gelatin solution with a weight volume concentration of 10%), completely swell in a warm water bath at 55°C, then add 0.2g of nuciferine and mix well Dissolve (the weight-volume concentration of nuciferine in the water phase is 5%); then add it dropwise into a beaker containing 0.6mL Span 80 and 30mL liquid paraffin, stir evenly in a warm water bath at 55°C, and the stirring speed is 1000r / min, stirring for 20min until milky white; rapidly cooled in an ice-water bath to below 5°C and continuing to stir for 10min, adding 3mL of glutaraldehyde in a trickle and continuing to stir for cross-linking and solidification for 30min, dehydrating with 30mL of anhydrous acetone and stirring for 15min, then suction filtration; Wash with a little anhydrous acetone to wash away the glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with ether, and dry in vacuum overnight to...

Embodiment 3

[0037] Take 0.4g of gelatin, add 4mL of double-distilled aqueous solution (to make a gelatin solution with a weight volume concentration of 10%), completely swell in a warm water bath at 55°C, and then add 0.5g of nuciferine, mix and dissolve (nuciferine in the water phase The weight volume concentration is 5%); then drop into a beaker containing 20mL Span 80 and 30mL liquid paraffin, stir evenly in a warm water bath at 80°C, and stir at a speed of 1000r / min, until milky white after stirring for 20min; ice Rapidly cool in a water bath to below 5°C and continue stirring for 10 minutes, add 3 mL of glutaraldehyde in a trickle and continue stirring for 30 minutes to cross-link and solidify, dehydrate with 30 mL of isopropanol and stir for 15 minutes, then filter with suction; dialdehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum overnight to obtain microsphere powder.

[0038] The nuciferine gelatin microspheres in thi...

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Abstract

The invention discloses a nuciferine microsphere and a preparation method thereof, and belongs to the technical field of traditional Chinese pharmacology. The nuciferine microsphere achieves the drug loading capacity at 5-50 percent by weight, has good roundness and good dispersity in a water solution and achieves the particle size distribution within the range of 10-50 micrometers. The preparation method comprises the following steps of: dissolving a carrier material and nuciferine into water or a phosphate buffer solution to obtain a water phase; uniformly mixing span 80 or span 60 and liquid paraffin to obtain an oil phase; dropping the water phase to the oil phase, uniformly stirring to be milk white, and then continuing emulsifying under ice bath; adding glutaric dialdehyde for cross-linking curing, then dewatering through isopropanol, stirring, and carrying out suction filtration; washing away glutaric dialdehyde and the liquid paraffin, and drying to obtain the nuciferine microsphere. The preparation process disclosed by the invention is easy to operate and low in cost. The nuciferine microsphere prepared through the method has the advantages of roundness in shape, less adhesion, good dispersity in the water solution, uniformity in particle size distribution, high stability and hydrophilicity and high practicability.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine, and in particular relates to a nuciferine microsphere and a preparation method thereof. Background technique [0002] The lotus leaf is the dry leaf of the water lily plant lotus (Nelumbo nucifera Gaertn.), which is cultivated in both north and south of my country. Ancient medical literature records that the leaves have the effects of clearing heat and dampness, promoting hair growth, clearing yang, and stopping bleeding. Lotus leaves are rich in alkaloids, flavonoids, organic acids and tannins, among which Nuciferine is the main active ingredient in lotus leaves, and its chemical structure is shown in formula Ⅰ. [0003] [0004] A large number of experiments have proved that Nuciferine has significant lipid-lowering and weight-loss effects, especially has an inhibitory effect on acute hyperlipidemia; Nuciferine extract has a strong antibacterial effect on bacteria, yeas...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/473A61K47/48A61K47/36A61K47/38A61P3/06A61P3/04A61P31/04A61P31/12A61P31/10
Inventor 宋杨一嫣宋金春彭燕杨小青
Owner WUHAN UNIV
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