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Liquidambaric acid or ursolic acid nano-granule and preparation method thereof

A Lulutong acid and nanoparticle technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as low bioavailability, and achieve good effects and stable performance. , good stability

Active Publication Date: 2015-06-24
SHANGHAI APPLIED TECHNOLOGIES COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although many pentacyclic triterpene compounds are active, the use of prototype triterpene compounds cannot simply solve their solubility or particle size problems at the same time, so that there are problems in their use and cannot be further applied. One of the purposes of the present invention is to solve the above-mentioned problem. Pentacyclic triterpene acids such as lutonic acid or ursolic acid are insoluble in water and have low bioavailability due to insufficient absorption. Low technical problem and provide a kind of Passepartout acid nanoparticle or ursolic acid nanoparticle and preparation method thereof, this Passepartout acid nanoparticle or ursolic acid nanoparticle can enhance water solubility and cell permeability greatly, overcome Technical issues of low absorption and low bioavailability

Method used

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  • Liquidambaric acid or ursolic acid nano-granule and preparation method thereof
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  • Liquidambaric acid or ursolic acid nano-granule and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0066] A Passepartout acid nanocapsule particle, which uses Passepartout acid as a core material and rubusoside as a wall material. The amounts of the core material and the wall material are calculated according to the mass ratio, and the core material: wall material is 1:10.

[0067] The above-mentioned preparation method of Passepartout acid nanocapsule particles is prepared by high-energy ball milling, and the steps are as follows:

[0068] Accurately weigh 1g of BEA and 10g of rubusoside, put them in an 80ml grinding bowl, use a planetary high-energy enhanced ball mill (FRITSCH premium line Planetary Mills, PULVERISETTE 7, Germany), select parameters: 80ml embedded grinding bowl with self-locking function, dry Grinding method, 3mm grinding ball, 20g steel ball, rotating speed 1100 rpm, reaction time 7min, drug loading = 1:10, finally got Passepartout acid nanocapsules.

[0069] The particle diameter of the above-mentioned obtained Passepartout acid nanocapsule particles is...

Embodiment 2

[0075] A ursolic acid nanocapsule particle, which uses ursolic acid as a core material and stevioside as a wall material. The amounts of the core material and the wall material are calculated by mass ratio, and the core material: wall material is 1:20.

[0076] The preparation method of above-mentioned a kind of ursolic acid nanocapsule particle adopts high-energy ball milling method to prepare ursolic acid nanoparticle, specifically as follows:

[0077] Accurately weigh 0.5g of URA and 10g of stevioside, and place them in an 80ml grinding bowl, using a planetary high-energy enhanced ball mill (FRITSCH premium line Planetary Mills, PULVERISETTE 7, Germany), selection parameters: 80ml embedded grinding bowl with self-locking function , Dry grinding, 3mm grinding ball, 20g steel ball, rotating speed 900rpm, reaction time 9min, drug loading = 1:20, and finally ursolic acid nanocapsule particles were obtained.

[0078] The particle diameter of the ursolic acid nanocapsule particle...

Embodiment 3

[0083] A Passepartout acid nanocapsule particle, which uses Passepartout acid as a core material and tea saponin as a wall material. The amounts of the core material and the wall material are calculated by mass ratio, and the core material: wall material is 1:30.

[0084] The above-mentioned preparation method of Passepartout acid nanocapsule particles is prepared by an ultrasonic high-speed homogenizer method, which specifically includes the following steps:

[0085] (1) The core material Passepartout acid was added to ethanol, and after ultrasonic treatment and mixing evenly, an ethanol solution of Passepartout acid with a mass percentage concentration of 25% was obtained;

[0086] (2) Dissolving the wall material tea saponin in distilled water, and after ultrasonic treatment and mixing evenly, an aqueous solution of tea saponin with a concentration of 25% by mass is obtained;

[0087] (3), the Passepartout acid ethanol solution obtained in step (1) and the tea saponin aqueo...

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Abstract

The invention discloses a liquidambaric acid or ursolic acid nano-granule, a preparation method and an application thereof. The liquidambaric acid or ursolic acid nano-granule is prepared by the following steps: taking the liquidambaric acid or ursolic acid as a core material, taking one or two mixtures of the gelatin, B-cyclodextrin, rubusoside, soluble starch, stevioside and thea saponin as a wall material, wherein the mass ratio of the core material to the wall material is 1:(5-100). The preparation method is an ultrasonic high-speed refiner method or a high energy ball milling method. By adopting the liquidambaric acid or ursolic acid nano-granule, the cell permeability can be improved and the growths of the human colon carcinoma cell HT-29, the human prostate cancer cell DU145 or the human breast cancer cell MDA-MB-231 can be inhibited.

Description

technical field [0001] The invention relates to a Passepartout acid nanoparticle or ursolic acid nanoparticle and a preparation method thereof. Compared with the original compound Passepartout acid or ursolic acid nanoparticle, the water-soluble The properties of Passepartout Acid Nanoparticles or Ursolic Acid Nanoparticles have improved cell permeability compared with Passepartout Acid or Ursolic Acid at the same time, and the Passepartout Acid Nanoparticles or Ursolic Acid Nanoparticles Has anti-tumor cell proliferation properties. The nano particle of the present invention is a drug raw material and a drug intermediate with the effect of anti-tumor cell proliferation. Background technique [0002] Tumor is a serious disease that endangers human health. Among them, the antitumor activity of triterpenes and their homologues in natural products has attracted the attention of researchers. In recent years, many pharmacological activities of triterpenes have been reported, inc...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/56A61K47/26A61K47/36A61K47/40A61K47/46A61P35/00
Inventor 张健刘志军侴桂新
Owner SHANGHAI APPLIED TECHNOLOGIES COLLEGE
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