Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Ursodeoxycholic acid solid dispersoid, preparation method and solid preparation

A technology of ursodeoxycholic acid and solid dispersion, which is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, and pill delivery, etc. It can solve the problems of dissolution and so on

Inactive Publication Date: 2010-09-22
SHANGHAI HUIDE MEDICINE SCI & TECH +1
View PDF2 Cites 15 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after the prepared solid dispersion is placed for a short period of time, the drug will crystallize and precipitate from the solid dispersion, thereby reducing its solubility
[0009] Therefore, so far, there is no ursodeoxycholic acid preparation that can improve the dissolution rate very well, and even in the Chinese Pharmacopoeia, there is no record about the dissolution rate standard for the current preparations, which also shows that ursodeoxycholic acid Existing preparations of cholic acid fail to solve the problem of dissolution well, thereby improving bioavailability

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Ursodeoxycholic acid solid dispersoid, preparation method and solid preparation
  • Ursodeoxycholic acid solid dispersoid, preparation method and solid preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030] (2) The preparation method of ursodeoxycholic acid solid dispersion

[0031] The preparation method of the ursodeoxycholic acid solid dispersion provided by the invention includes a melting method, a solvent method or a solvent melting method. Among them, the solvent method is preferable.

[0032] The melting method is to mix the drug and the carrier evenly (the carrier is coarsely powdered), heat it in a water bath or an oil bath until it melts, or heat the carrier to melt, then add a surfactant to melt, and finally add the drug to stir to dissolve, and then Under vigorous stirring, the melt was rapidly cooled into a solid.

[0033] The melting method according to the present invention comprises the following steps:

[0034] Take an appropriate amount of hydrophilic material, heat it in a water bath at 40-90°C to melt it, then add a surfactant, stir for 20-50 minutes to melt it, then add ursodeoxycholic acid, and stir again for 30-150 minutes , then pour out the mel...

Embodiment 1

[0060] According to the formula shown in Table 1, put ursodeoxycholic acid and poloxamer into a beaker, add absolute ethanol, stir to dissolve completely, add sodium dodecylsulfonate, stir to dissolve. In a 40°C water bath, evaporate the solvent with a rotary evaporator for 35 minutes, and evaporate the solvent to dryness. Transfer to a vacuum drying oven to continue drying for 24 hours, take out, grind, and pass through an 80-mesh sieve to obtain a solid dispersion of ursodeoxycholic acid.

[0061] The above-mentioned ursodeoxycholic acid solid dispersion of the present invention is compressed into tablets to obtain the tablet of the present invention. The dissolution and productivity of the tablet of the present invention were measured, and the results are shown in Table 1.

[0062] Table 1

[0063] Raw materials

Embodiment 2

[0065] According to the formula shown in Table 2, the ursodeoxycholic acid was weighed and added into 90% ethanol, stirred and dissolved to a clear solution, and the formulated amount of PVPK30 was added, stirred and dissolved to obtain a clear solution.

[0066] Weigh the amount of sodium lauryl sulfate dissolved in water, stir to dissolve until the solution is clear.

[0067] The above two solutions are mixed to form a mixed solution or a homogeneous suspension.

[0068] The coating is carried out in a fluidized bed spray coating machine. After the machine is started, the blank ball core is placed in the fluidized bed coating machine, and under the action of hot air flow, it is in a suspended state. The above liquid medicine is transported to the fluidized bed by a peristaltic pump, sprayed and coated until all the liquid medicine is coated, then fluidized and dried in the fluidized bed. The parameters of the fluidized bed are as follows: bottom spray; fan frequency 20; mat...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention provides an ursodeoxycholic acid solid dispersoid, a preparation method and a solid preparation. The solid dispersoid comprises ursodeoxycholic acid (A), a surfactant (B) and a hydrophilic material (C), wherein the weight ratio of (A) and (C) is 1:5-1:0.1, and the content of (B) in the ursodeoxycholic acid solid dispersoid is 2-60wt%.

Description

technical field [0001] The invention relates to a solid dispersion of ursodeoxycholic acid, a preparation method and a solid preparation. Background technique [0002] Ursodeoxycholic Acid (Ursodeoxycholic Acid), its chemical name is 3α, 7β-dihydroxy-5β-cholestane-24-acid, molecular formula C 24 h 40 o 4 , molecular weight: 392.57, has the following chemical structure, [0003] [0004] Ursodeoxycholic acid was first isolated from bear bile. Under physiological conditions, it accounts for no more than 2% of bile acids in the human body. It is a hydrophilic third-level bile acid. In addition to effectively dissolving cholesterol gallstones, ursodeoxycholic acid also has the functions of promoting gallbladder and protecting liver cells, immune regulation, especially reducing the immune response of intrahepatic lymphocytes and bile duct epithelium; inhibiting cell apoptosis, etc. Nearly 30 years of clinical use have proved that ursodeoxycholic acid is the only effective ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/16A61K9/48A61K9/20A61K9/00A61K31/575A61K47/20A61K47/34A61P1/16A61K47/10A61K47/26
Inventor 吴伟阙俐陈虎林舒晓明
Owner SHANGHAI HUIDE MEDICINE SCI & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com