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Myricetin nanosuspension and preparation method thereof

A nano-suspension, myricetin technology, applied in the direction of anti-toxic agents, anti-viral agents, pharmaceutical formulations, etc., can solve problems such as retention, no nanotechnology application, no preparation technology, myricetin oral absorption, etc., to improve Properties, not easy to store, and the effect of simple composition

Inactive Publication Date: 2013-05-08
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The research on myricetin drug delivery system is still mainly in some traditional oral dosage forms and preparation intermediates. There is no preparation technology used to improve the oral absorption of myricetin. Other routes of administration and forms of administration have not yet been touched, and There is no research report on the application of nanotechnology in myricetin drug delivery system

Method used

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  • Myricetin nanosuspension and preparation method thereof
  • Myricetin nanosuspension and preparation method thereof
  • Myricetin nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Screening of Stabilizers

[0033] Weigh Tween-801g, CremophorEL1g, TPGS1g, PVP1g, Tylosamer 1g, CremophorEL0.8g + Tylosamer 0.2g, add 200mL water to dissolve it respectively, weigh 2400mg of myricetin raw material and dissolve it in 120mL ethanol, Under the condition of 16000rpm high-shear homogenization, take 20mL of liquid medicine and add them to different water phases, continue shearing for 20min, recover the organic solvent, put the obtained suspension in a high-pressure homogenizer, and circulate it 5 times at 200bar. 5 cycles at 500 bar and 15 cycles at 800 bar.

[0034] The particle size, PdI, Zeta potential and sedimentation ratio of myricetin nanosuspensions with different stabilizers after 15 days of storage are shown in Table 1. The results showed that the particle size, PdI and stability of myricetin nanosuspensions obtained by using different stabilizers were somewhat different. The particle size of the nanosuspension prepared with PVP, Tylosamer, and Ty...

Embodiment 2

[0038] Investigation on the Ratio of Myricetin and Stabilizer

[0039]Weigh Tween-800g, Tween-800.05g, Tween-800.1g, Tween-800.2g, Tween-800.3g, Tween-800.5g, Tween-801g, add 200mL water to dissolve them respectively, Weigh 1000 mg of myricetin raw material and dissolve it in 50 mL of ethanol. Under the condition of 16000 rpm high-shear milk homogeneity, take 10 mL of liquid medicine and add it to different water phases, continue shearing for 20 min, recover the organic solvent, and place the obtained suspension in In the high-pressure homogenizer, there are 5 cycles at 200bar, 5 cycles at 500bar, and 15 cycles at 800bar.

[0040] The particle size, PdI, Zeta potential and sedimentation ratio of myricetin nanosuspensions with different ratios of stabilizers after 15 days of storage are shown in Table 2.

[0041] The results showed that when the mass ratio of myricetin to Tween-80 was 1:0 and 1:5, the particle size of the sample was too large and the stability was poor, so it ...

Embodiment 3

[0045] Weigh 0.5g of Cremophor EL, add 200mL of water to dissolve it, weigh 200mg of myricetin raw material and dissolve it in 20mL of methanol, add the drug solution into the water phase under the condition of 12000rpm high-shear milk, continue shearing for 20min, and recover the organic The solvent is obtained by placing the obtained suspension in a high-pressure homogenizer, circulating 5 times at 200 bar, 5 times at 500 bar, and 15 times at 800 bar.

[0046] The particle size of the myricetin nanosuspension prepared by this process is 296.7nm, the PdI is 0.153, the Zeta potential is -19.6mV, and the sedimentation ratio is 80.44% after being placed for 10 days.

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Abstract

The invention belongs to the technical field of medicines and relates to a myricetin nanosuspension and a preparation method thereof. The myricetin nanosuspension is prepared by adopting a settling method and a high-pressure homogenization method, and the formula comprises myricetin and a stabilizer according to the weight ratio of 1: 0.25-1: 2.5. According to the preparation method provided by the invention, the formula is optimized, Tween-80, Cremophor EL and D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) are screened as the stabilizer, the prepared myricetin nanosuspension has stable nature and simple composition of the formula, the preparation process is simple, convenient and feasible, and the particle size range is 100nm-300nm; and by reducing the particle size of a medicament, the solubility and the dissolution of the myricetin are obviously improved, and the oral bioavailability and the in-vivo tissue distribution of the myricetin are further improved. In addition, the myricetin nanosuspension can be freeze-dried, and proper excipients are added into the obtained freeze-dried powder for further preparing oral liquid, tablets, granules, capsules and other different oral preparations so as to facilitate clinical applications.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to myricetin nano-suspension and its preparation method and application. Background technique [0002] Myricetin (3,5,7,3′,4′,5′,-hexahydroxyflavone), as a natural flavonoid chemical component, is the main substance in the bark and leaves of Myricaceae and red wine. Flavonol components, and widely exist in onions, berries, tea and other natural plants. Myricetin is a yellow needle-like crystalline powder with molecular formula C 15 h 10 o 8 , relative molecular weight 318, soluble in methanol, ethanol, acetone, slightly soluble in ethyl acetate, insoluble in water, petroleum ether (60 ~ 90 ℃), chloroform, toluene, n-hexane. In vivo and in vitro studies have shown that myricetin has strong pharmacological activity, and has various effects such as antibacterial, antiviral, antioxidative, neuroprotective, hypoglycemic, anti-liver damage, uric acid reduction, and preventio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/352A61K47/34A61K47/44A61K47/26A61P31/04A61P31/12A61P39/06A61P25/00A61P3/10A61P1/16A61P19/06A61P19/10A61P9/00
Inventor 谢燕林国钡姚雅淑洪超骆慧琳李国文孟厚君段景泽党阳
Owner SHANGHAI UNIV OF T C M
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