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Preparation method of oleanolic acid slow-releasednano-microcapsule

A technology of nano-microcapsules and oleanolic acid, which is applied in the direction of nano-capsules, capsule delivery, medical preparations of non-active ingredients, etc., and can solve problems such as low bioavailability, poor intestinal permeability, and poor water solubility , to achieve the effect of strong practicability, simple preparation method and high efficiency of controlled release

Active Publication Date: 2019-10-15
HARBIN INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, poor aqueous solubility and poor intestinal permeability, together with concomitant low bioavailability, present severe barriers to the ubiquity of OA.

Method used

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  • Preparation method of oleanolic acid slow-releasednano-microcapsule
  • Preparation method of oleanolic acid slow-releasednano-microcapsule

Examples

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Effect test

Embodiment 1

[0027] A preparation method of oleanolic acid slow-release nano-microcapsules, comprising the following steps:

[0028] (1) Prepare the amphiphilic polymer wall material of sustained-release nano-microcapsules, the 1000Da chitosan oligosaccharide with a weight part of 19.630-21.442, the deoxycholic acid with a weight percentage of 58.890-64.325 and a weight percentage of 15%-20% The 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS) were dispersed in organic solvents, and chitosan and The mass ratio of deoxycholic acid is 1:3 to 1:5. After fully reacting with magnetic stirring, it is dialyzed in distilled water (1000Da dialysis bag), and freeze-dried to obtain the amphiphile of slow-release nano-microcapsules of deoxycholic acid modified chitosan oligosaccharides. permanent polymer wall material.

[0029] (2) Dissolve oleanolic acid with a weight part of 14.233-21.480 in an organic solvent to prepare a dispersion of oleanolic acid...

Embodiment 2

[0032] A preparation method of oleanolic acid slow-release nano-microcapsules, comprising the following steps:

[0033] (1) Prepare the amphiphilic polymer wall material of sustained-release nano-microcapsules, and the carboxymethyl chitosan of 80.839-83.641 parts by weight and the 1-(3-dimethylamino group of 15%-20% by weight Propyl)-3-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS) were respectively dispersed in organic solvents, and after fully reacting with magnetic stirring, placed in distilled water for dialysis (1000Da dialysis bag ), freeze-dried to obtain the amphiphilic polymer wall material of the sustained-release nano-microcapsules of deoxycholic acid-modified chitosan oligosaccharides.

[0034] (2) Dissolve oleanolic acid in parts by weight of 16.359-19.161 in an organic solvent to prepare a dispersion of oleanolic acid with a volume mass concentration of 1-2 mg / mL, and disperse it in the volume mass mass prepared in step (1). In the wall ma...

Embodiment 3

[0037] A preparation method of oleanolic acid slow-release nano-microcapsules, comprising the following steps:

[0038](1) Prepare the amphiphilic polymer wall material of the slow-release nano-microcapsules, the 3000Da chitosan oligosaccharide with the weight part of 18.614-20.210, the deoxycholic acid with the weight part of 55.842-60.629 and the weight percentage of 15%-20% The 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS) were dispersed in organic solvents, and chitosan and The mass ratio of deoxycholic acid is 1:3 to 1:5. After fully reacting with magnetic stirring, it is dialyzed in distilled water (1000Da dialysis bag), and freeze-dried to obtain the amphiphile of slow-release nano-microcapsules of deoxycholic acid modified chitosan oligosaccharides. permanent polymer wall material.

[0039] (2) Dissolve oleanolic acid in parts by weight of 19.161 - 24.544 in an organic solvent to prepare a dispersion of oleanolic acid...

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Abstract

The invention provides a preparation method of an oleanolic acid slow-releasednano-microcapsule. The aim is to design and optimize oleanolic acid (OA) nanoparticles with poor water solubility to improve the oral bioavailability of the oleanolic acid (OA) nanoparticles and prolong the duration of the treatment drug level. Nanoparticle wall material is an amphiphilic polymer formed by hydrophilic chitosan oligosaccharide and hydrophobic deoxycholic acid. The particle size of nanoparticles with different wall materials is 200-400nm, and distribution is uniform. Releasing in vitro experiment is conducted in simulated gastrointestinal tract environment, results show that the oleanolic acid nanocapsule is released slowly in the simulated gastric juice and gradually released in the intestinal juice; explosive releasing is showed in early stage of releasing in the PBS solution, and then releasing is slowly; and the oleanolic acid nanocapsule is released significantly in each solution. The oleanolic acid controlled-release nanocapsule improves the bioavailability of oleanolic acid, has obvious in vitro controlled-release effect, and can be used as an effective oral preparation for future liver injury treatment.

Description

technical field [0001] The invention belongs to the field of oleanolic acid drug carriers, in particular to a preparation method of oleanolic acid slow-release nano-microcapsules. Background technique [0002] Oral administration is the preferred route of drug delivery, which has the characteristics of convenience, painless administration and high compliance to patients, especially an important route for the treatment of patients with chronic diseases. Drugs can maintain a constant drug concentration in the circulation to increase therapeutic efficiency. However, multiple obstacles hinder the oral administration of drugs due to their poor bioavailability, including the physicochemical properties of the drug, physiological barriers in the gastrointestinal tract, and biochemical barriers in the gastrointestinal tract. At present, various strategies to overcome multiple obstacles have been developed for oral drug delivery to improve the stability of drugs, prolong the residenc...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K47/36A61K47/28A61K31/56A61P1/16A61P3/06A61P35/00A61P39/06A61P29/00A61P31/04A61P31/10A61P25/24
CPCA61K9/5123A61K9/5161A61K31/56A61P1/16A61P3/06A61P25/24A61P29/00A61P31/04A61P31/10A61P35/00A61P39/06
Inventor 王振宇刘双王佳慧
Owner HARBIN INST OF TECH
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