Domperidone particles, domperidone preparation and preparation method thereof

A technology of domperidone and microparticles, applied in the direction of pill delivery, digestive system, diseases, etc., to achieve the effect of easy industrial production, low cost and good dissolution performance

Inactive Publication Date: 2014-07-02
EAST CHINA UNIV OF SCI & TECH +1
View PDF3 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to overcome the various defects of the current method for reducing the drug particle size, and provide a preparation of domperidone microparticles with an average particle size of less than 20 microns, low pollution and loss, high safety, and easy operation Method, and preparation method of pharmaceutical preparation containing domperidone microparticles and good dissolution rate

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
  • Domperidone particles, domperidone preparation and preparation method thereof
  • Domperidone particles, domperidone preparation and preparation method thereof
  • Domperidone particles, domperidone preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1 prepares domperidone microparticles

[0041] (1) Add 10 grams of domperidone coarse crystals and 2 grams of poloxamer 188 into 60 grams of 70% ethanol aqueous solution, stir to disperse, add 4.7 grams of 20% hydrochloric acid and stir until completely dissolved to obtain solution I.

[0042] (2) Add about 11 grams of 10% sodium hydroxide aqueous solution to a pH value of 7.3 under stirring at room temperature (stirring linear velocity 100 m / min), continue stirring for 5 minutes, add 50 grams of water and stir for another 5 minutes, and separate out by suction filtration The microparticles were washed twice with 10 grams of water and suction-filtered respectively, and dried under reduced pressure at 60° C. for 4 hours to obtain 9.31 grams of domperidone microparticles, with a yield of 93.1% and a content of 99.1%.

Embodiment 2

[0043] Embodiment 2 prepares domperidone microparticles

[0044] (1) Add 10 grams of domperidone coarse crystals and 3 grams of Tween 80 into 50 grams of 80% ethanol aqueous solution, stir to disperse, add 4.7 grams of 20% hydrochloric acid and stir until completely dissolved to obtain solution I.

[0045] (2) Add about 10.5 grams of 10% sodium hydroxide aqueous solution to a pH value of 6.8 under stirring at room temperature (stirring linear velocity 100 m / min), continue stirring for 5 minutes, add 50 grams of water and stir for another 5 minutes, and separate out by suction filtration The microparticles were washed twice with 10 grams of water and suction-filtered respectively, and dried under normal pressure at 60°C for 6 hours to obtain 9.06 grams of domperidone microparticles, with a yield of 90.6% and a content of 98.9%.

Embodiment 3

[0046] Embodiment 3 prepares domperidone microparticles

[0047] (1) Add 10 grams of domperidone coarse crystals to 60 grams of 50% ethanol aqueous solution, stir to disperse, add 4.7 grams of 20% hydrochloric acid and stir, warm at 50°C until completely dissolved, add 2 grams of poloxamer 188 to dissolve, and obtain solution I.

[0048] (2) Add about 11 grams of 10% sodium hydroxide aqueous solution to a pH value of 7.0 under stirring (stirring line speed 100 m / min), continue stirring for 5 minutes, add 50 grams of water and stir for another 5 minutes, set high-speed milk to homogenize After spinning at 10,000 rpm for 10 minutes, the precipitated particles were suction filtered, washed twice with 10 grams of water and filtered separately, and dried at 50°C under normal pressure for 7 hours to obtain 9.12 grams of domperidone particles, with a yield of 91.2% and a content of 99.3%. .

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 sizeaaaaaaaaaa
specific surface areaaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses a preparation method of domperidone particles. The method comprises the following steps: dispersing domperidone and dispersion aids into a solvent; adding an acid to dissolve to obtain a solution I; adding an alkali liquor to the solution I under an agitation condition, so as to obtain a mixture containing the domperidone particles; separating the domperidone particles, wherein the mean grain size of the obtained particles is smaller than 20mum, the particles have the specific surface area equivalent to over twice of those of common domperidone particles and are high in dissolution rate. The invention also discloses a preparation method of the preparation containing the domperidone particles. The method for preparing the domperidone particles is simple and convenient to operate, free of harsh process condition and equipment, low in cost and easy for realization of industrial production.

Description

technical field [0001] The invention relates to a preparation method of domperidone microparticles, a preparation method of domperidone preparations, a domperidone microparticles and a domperidone preparation containing the same. Background technique [0002] Domperidone is an anti-dopamine drug that selectively blocks peripheral dopamine and acts directly on the gastrointestinal wall to increase the tension of the lower esophageal sphincter, enhance gastric motility, promote gastric emptying, and coordinate gastric and duodenal motility. Clinically, it is generally used to relieve indigestion symptoms caused by delayed gastric emptying, gastrointestinal reflux, and esophagitis, such as: upper abdominal distension, abdominal distension, upper abdominal pain, belching, flatulence, and mouth with or without Heartburn with regurgitation of gastric contents, treatment of functional, organic, infectious, dietary, radiation therapy, or chemotherapy-induced nausea, vomiting, and so...

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): A61K9/16A61K9/10A61K9/14A61K9/20A61K9/48A61K31/454A61P1/14A61P1/08A61P15/14
Inventor 任福正郑斯骥景秋芳于艳刘潇怡
Owner EAST CHINA UNIV OF SCI & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products