Chlorogenic acid (CA) and chitosan microspheres as well as preparation process and application thereof

A technology of chitosan microspheres and preparation technology, which is applied in the field of biomedicine, can solve the problems of low bioavailability, insufficient affinity, short half-life, etc., and achieve the goal of increasing permeability, improving oral bioavailability, and improving limitations Effect

Active Publication Date: 2015-08-19
SICHUAN JIUZHANG BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, chlorogenic acid is an active small molecular substance with good hydrophilicity but poor lipophilicity. Its affinity with cells is insufficient and its half-life is short, making its bioavailability low when taken orally.

Method used

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  • Chlorogenic acid (CA) and chitosan microspheres as well as preparation process and application thereof
  • Chlorogenic acid (CA) and chitosan microspheres as well as preparation process and application thereof
  • Chlorogenic acid (CA) and chitosan microspheres as well as preparation process and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Embodiment 1: Utilize emulsification cross-linking method to prepare chlorogenic acid chitosan microspheres

[0063] 1. Experimental Materials and Instruments

[0064] Chlorogenic acid, chitosan (210kDa, Jinan Haidebei Marine Biological Engineering Co., Ltd.), trimethyl chitosan (Jinan Haidebei Marine Biological Engineering Co., Ltd.), Glutaraldehyde, Span 80 and Tween 80 (all purchased from Chengdu Baoxin Reagent Co., Ltd.), edible soybean oil, salad oil, wheat germ oil, etc.

[0065] Hitachi high-tech scanning electron microscope (Hitachi), high performance liquid chromatography (Shimadzu, Japan), magnetic stirrer, electronic balance, vacuum drying oven, laser particle size analyzer (Malvern), etc.

[0066] 2. Preparing the formulation and method

[0067] The preparation recipes of different chlorogenic acid chitosan microspheres are shown in Table 1.

[0068] After mixing the chitosan or trimethyl chitosan of the prescription amount of chlorogenic acid and the pre...

Embodiment 2

[0084] Embodiment 2: utilize spray-drying method to prepare chlorogenic acid chitosan microsphere

[0085] 1. Experimental reagents and instruments

[0086] Chlorogenic acid, chitosan (210kDa, Jinan Haidebei Marine Biological Engineering Co., Ltd.), trimethyl chitosan (Jinan Haidebei Marine Biological Engineering Co., Ltd.), hydrochloric acid, which are extracted from honeysuckle with a purity of 99.9% , small spray dryer (Switzerland Richi), Hitachi high-tech scanning electron microscope (Hitachi), high performance liquid chromatography (Shimadzu, Japan), magnetic stirrer, electronic balance, vacuum drying oven, laser particle size analyzer (Malvern), etc. .

[0087] 2. Preparation method

[0088] The specific prescription is shown in Table 4.

[0089] Chlorogenic acid is mixed with chitosan or trimethyl chitosan and dissolved in 0.1 mol / L hydrochloric acid to form a chlorogenic acid chitosan solution. Wherein, the mass ratio of chlorogenic acid to chitosan or trimethyl c...

Embodiment 3

[0103] Embodiment 3: The experiment that gel method prepares chlorogenic acid chitosan microsphere

[0104] 1. Experimental Materials and Instruments

[0105] Chlorogenic acid, chitosan (210kDa, Jinan Haidebei Marine Bioengineering Co., Ltd.), high performance liquid chromatography (Shimadzu, Japan), magnetic stirrer, electronic balance, Vacuum drying oven, laser particle size analyzer (Malvern), etc.

[0106] 2. Preparation method

[0107] The specific prescription groupings are shown in Table 7.

[0108] After mixing chlorogenic acid and chitosan, dissolve it in an acetic acid solution with a volume concentration of 3% to form a chlorogenic acid-chitosan solution, wherein the mass ratio of chlorogenic acid to chitosan is 1.5:1; Under the condition of stirring, slowly add the chlorogenic acid chitosan solution into the anionic gelling agent aqueous solution with a concentration of 1mg / mL with a syringe, and after filtering, wash and dry the obtained microspheres to obtain ...

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Abstract

The invention discloses chlorogenic acid (CA) and chitosan microspheres as well as a preparation process and application thereof. The CA and chitosan microspheres are prepared by using CA as a main medicine and chitosan or trimethyl chitosan as a carrier material. The preparation process of CA comprises an emulsion-crosslinking method, a spray drying method and a gelatination method. The CA and chitosan microspheres are applied to preparation of medicines. The CA and chitosan microspheres are prepared from chitosan and CA by adopting an appropriate method, thus being capable of effectively improving the permeability of CA toward biological membranes, improving the oral bioavailability of CA, helping CA give play to the effects in bodies, helping change the defects of physicochemical properties of CA, improving the oral bioavailability limitation of CA and providing more references and ideas for development and application of CA.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and more specifically relates to a chlorogenic acid chitosan microsphere and its preparation process and application. Background technique [0002] Chlorogenic acid (CA) is a phenylpropanoid synthesized by plants during aerobic respiration, with the molecular formula C 16 o 18 o 9 And the molecular weight is 345.30. It is the main active ingredient of many Chinese herbal medicines such as honeysuckle, Eucommia, capillary, etc., and is also an important active ingredient in many fruits and vegetables. [0003] Chlorogenic acid has various functions such as scavenging free radicals, antibacterial and anti-inflammatory, anti-virus, hypoglycemic, lipid-lowering, liver protection and gallbladder protection. Anti-cancer, anti-AIDS drugs. At the same time, as a good antioxidant, chlorogenic acid is widely used in various fields such as medicine and food. [0004] However, chlorogenic acid is an...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/36A61K31/216A61P39/06A61P31/04A61P29/00A61P31/12A61P3/10A61P3/06A61P1/16A61P35/00A61P31/18
Inventor张洁张梦甜
OwnerSICHUAN JIUZHANG BIO TECH CO LTD