Stable nobiletin liquid preparation and preparing method thereof

A technology of nobiletin and liquid preparations, which is applied in the field of nobiletin liquid preparations and its preparation, can solve the problems of poor stability and low bioavailability of nobiletin, achieve excellent anti-oxidation, simple preparation process, and prevent precipitation Effect

Active Publication Date: 2018-05-08
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a liquid preparation of the hydrophobic drug nobiletin and a preparation method thereof, aiming at overcoming the defects of poor stability and low bioavailability of nobiletin in the liquid at present

Method used

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  • Stable nobiletin liquid preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve nobiletin in absolute ethanol to make a concentration of 7 mg / ml nobiletin ethanol solution; take persimmon tannin, tannic acid, epigallocatechin gallate, tea polyphenols, gallic acid, and coke respectively Catechol was dissolved in ultrapure water to make a polyphenol aqueous solution with a concentration of 40 mg / ml; under the condition of magnetic stirring, 500 μl of nobietin ethanol solution was quickly poured into the pH=7.7 solution by pipetting dropwise. 100 μl of polyphenol aqueous solution was added to 10 ml of phosphate buffer solution, placed in an air shaker at 25° C., and shaken for 48 hours to achieve equilibrium.

[0028] Detection: (1) the obtained solution is detected by a dynamic light scattering instrument to detect the average particle diameter, the smaller the particle diameter, the better the solubility, and the medicine is less likely to be separated out; (2) the dynamic light scattering instrument is used to measure the polymer dispersion...

Embodiment 2

[0033] Dissolve nobiletin in absolute ethanol to make a concentration of 7mg / ml nobiletin ethanol solution; get tannic acid and dissolve it with ultrapure water to make a polyphenol aqueous solution with a concentration of 40mg / ml; under the condition of magnetic stirring Next, 500 μl of nobietin ethanol solution was quickly poured into 10ml of phosphate buffer solution with pH=7.7 by means of pipetting, and then 50, 100, 150, 200, 250, 300 μl of polyphenol aqueous solution were added respectively. Make the volume ratio of nobietin ethanol solution and polyphenol aqueous solution to 10:1, 10:2, 10:3, 10:4, 10:5, 10:6 respectively, place in an air shaker at 25°C, and shake 48h to reach equilibrium.

[0034] Table 2 Effects of polyphenols in different amounts on particle size, PDI and encapsulation efficiency of nobiletin solution

[0035] Polyphenol dosage

Embodiment 3

[0037] Dissolve nobiletin in absolute ethanol to make a concentration of 7mg / ml nobiletin ethanol solution; get tannic acid and dissolve it with ultrapure water to make a polyphenol aqueous solution with a concentration of 40mg / ml; under the condition of magnetic stirring Next, 500 μl of nobietin ethanol solution was quickly poured into 10ml of phosphate buffer solution with pH=7.0, 7.2, 7.4, 7.6, 7.8, and 8.0 by means of a pipette, and then 150 μl of polyphenol aqueous solution was added. Place in an air shaker at 25°C and shake for 48 hours to achieve equilibrium.

[0038] Table 3 Effects of different pH on particle size, PDI and encapsulation efficiency of nobiletin solution

[0039] pH

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Abstract

The invention discloses a stable nobiletin liquid preparation and a preparing method thereof; the stable nobiletin liquid preparation is composed of the following components in parts by volume: 1-10 parts of a nobiletin ethanol solution with a concentration of 1-10 mg/ml; 0.5-3 parts of a polyphenol aqueous solution with a concentration of 10-50 mg/ml; and 50-150 parts of a buffer solution with the pH of 7-8. Polyphenol substances are subjected to oxidative polymerization reaction under a weak alkaline condition, and a layer of uniform hydrophilic thin film is formed on the surface of a hydrophobic drug nobiletin, plays a role in embedding the hydrophobic drug and also is a thermodynamic stable system, so that the stability of nobiletin in an aqueous solution is effectively improved, the drug is prevented from being separated out and precipitates are prevented from being generated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a stable nobiletin liquid preparation and a preparation method thereof. Background technique [0002] Some highly hydrophobic drugs such as nobiletin and other natural polymethoxyflavonoids (PMFs) have a wide range of biological activities, such as anti-inflammation, anti-cancer, anti-oxidation, inhibition of thrombosis, anti-arteriosclerosis, Inhibition of obesity and improvement of insulin resistance have attracted great attention from chemists and medicinal chemists in recent years. Although such substances have good biological activity and nutritional value, because PMFs contain more methoxyl groups , high hydrophobicity, resulting in extremely low water solubility and easy crystallization, resulting in low bioavailability after oral administration. After oral intake, it is difficult to be absorbed by small intestinal epithelial cells in the small intestine and ente...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/352A61K47/26A61K47/22A61K47/46A61K47/10A61P29/00A61P35/00A61P39/06A61P7/02A61P9/10A61P3/04A61P5/50
CPCA61K9/08A61K31/352A61K47/10A61K47/22A61K47/26A61K47/46
Inventor 梁宏闪吴迪李斌李艳李晶
Owner HUAZHONG AGRI UNIV
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