Method for preparing naringenin/hydroxypropyl-Beta-cyclodextrin microcapsules by supercritical anti-solvent process

A supercritical anti-solvent, naringenin technology, applied in microcapsules, antidote, capsule transportation and other directions, can solve the problems of slow dissolution rate, poor water solubility of naringenin, limited application, etc. Availability and the effect of improving solubility

Active Publication Date: 2017-01-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although naringenin has a wide range of biological activities, naringenin has poor water solubility, low solubility in the gastrointestinal tract, slow dissolution rate, and low bioavailability, which greatly limit its clinical application.

Method used

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  • Method for preparing naringenin/hydroxypropyl-Beta-cyclodextrin microcapsules by supercritical anti-solvent process
  • Method for preparing naringenin/hydroxypropyl-Beta-cyclodextrin microcapsules by supercritical anti-solvent process
  • Method for preparing naringenin/hydroxypropyl-Beta-cyclodextrin microcapsules by supercritical anti-solvent process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: single factor method determines the preferred value range of each key parameter

[0034] Experimental Instruments and Materials

[0035] The main instruments used in the experiment are shown in Table 1, and the main raw materials and reagents are shown in Table 2.

[0036] Table 1 Main Instruments

[0037] device name model Manufacturer Supercritical Particle Preparation System Helix AppliedSeparations, USA Series1500 high pressure infusion pump Helix AppliedSeparations, USA air compressor pump TYW-2 Suzhou Tongtong Electromechanical Co., Ltd. Low temperature constant temperature bath SDC-6 Nanjing Xinchen Biotechnology Co., Ltd. UV-visible spectrophotometer UV-1800 Shimadzu Corporation Intelligent Dissolution Tester ZRS-8L Tianjin Tianda Tianfa Technology Co., Ltd. Analytical Balances BS124S Beijing Sartorius Instrument System Co., Ltd.

[0038] Table 2 Main raw materials ...

Embodiment 2

[0067] Embodiment 2: Orthogonal optimization of the best test parameters

[0068] Orthogonal experimental design and results

[0069] With the recovery rate as an index, an orthogonal experiment is designed to investigate crystallization pressure (A), crystallization temperature (B), solution concentration (C), and solution volume flow rate (D). Table 4 is a factor level design table, and Table 5 is an orthogonal experiment Design and Results.

[0070] Table 4 Factor level table

[0071]

[0072] Table 5 Orthogonal design and results

[0073] Test No. A / MPa B / ℃ C / g·L -1 D / mL·min -1 Recovery rate / % 1 1 1 1 1 75.43 2 1 2 2 2 68.16 3 1 3 3 3 65.58 4 2 1 2 3 84.76 5 2 2 3 1 83.24 6 2 3 1 2 78.23 7 3 1 3 2 72.38 8 3 2 1 3 58.25 9 3 3 2 1 79.34 K 1 69.723 77.523 70.637 79.337 K 2 82.077 69.883 77.420 72.923 K 3 69.990 74.383 73.733 69.530 ...

Embodiment 3

[0080] Example 3: Characterization analysis of naringenin / HP-β-CD microcapsules

[0081] DSC analysis

[0082] DSC analysis of naringenin / HP-β-CD microcapsules such as Figure 6 It can be seen from C that the melting point of naringenin is 251.7°C. It can be seen from A and B that the melting point peak of naringenin at around 251.7°C disappears, which proves that naringenin is successfully included in HP-β-CD.

[0083] Solubility test

[0084] Take the excess naringenin raw material drug and 3 parts of naringenin / HP-β-CD microcapsule samples prepared under the optimal process, put them in a 20mL conical flask with a stopper, and add 20mL of purified water. Shake at a constant temperature at 37°C for 48 hours, take the supernatant, filter it with a 0.45 μm microporous membrane, measure the absorbance value at a wavelength of 288 nm after appropriate dilution of the subsequent filtrate, and substitute the absorbance value into the standard curve equation to calculate The ...

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Abstract

The invention discloses a method for preparing naringenin / hydroxypropyl-Beta-cyclodextrin microcapsules by supercritical anti-solvent process, comprising the steps of S1, dissolving naringenin and hydroxypropyl-Beta-cyclodextrin in an organic solvent to obtain a sample solution; S2, introducing CO2 into a crystallizer, and adjusting temperature and pressure in the crystallizer; S3, continually introducing CO2 at a flow speed, maintaining the temperature and pressure in the crystallizer constant, and introducing the sample solution of step S1 into the crystallizer; S4, after introduction of the sample solution, continuously introducing CO2, maintaining the temperature and pressure in the crystallizer constant, and relieving the pressure over a period of time; when the pressure in the crystallizer drops to atmospheric pressure, opening the crystallizer to collect the naringenin / hydroxypropyl-Beta-cyclodextrin microcapsules. The method provided herein wraps naringenin in HP-Beta-CD by using supercritical anti-solvent process, dissolving property of the naringenin in an aqueous solution is greatly improved, dissolvability is significantly improved, and bioavailability of the naringenin can be improved.

Description

technical field [0001] The invention relates to the preparation of naringenin / cyclodextrin microcapsules, in particular to a method for preparing naringenin / hydroxypropyl-β-cyclodextrin microcapsules by using a supercritical antisolvent method. Background technique [0002] Naringenin is a class of natural flavonoids, aglycone of naringin, a monomer extracted from Rutaceae vegetable oil, widely found in lemon, husk, grape juice, fenugreek, and pomelo peel , Huazhong Holly and so on. There are many studies abroad on the biological activity of naringenin. Data show that naringenin has biological activities such as anti-cancer, anti-oxidation, anti-ulcer, anti-atherosclerosis, anti-inflammatory, and lipid-lowering. Although naringenin has a wide range of biological activities, naringenin has poor water solubility, low solubility in the gastrointestinal tract, slow dissolution rate, and low bioavailability, which greatly limit its clinical application. Therefore, improving th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/352A61K47/48A61P35/00A61P39/06A61P9/10
CPCA61K9/5036A61K31/352
Inventor 王志祥缪虹刚宋雅琴刘尚德陈震王为彦徐文博高赵华
Owner CHINA PHARM UNIV
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