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

Ulipristal acetate dispersible tablet and preparation method thereof

A technology of ulipristal acetate and dispersible tablets, which can be applied to medical preparations containing active ingredients, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of low affinity of estrogen and mineralocorticoid receptors, etc. The effect of high Lilistat content, fast disintegration and high dissolution rate

Inactive Publication Date: 2018-05-04
ZHENGZHOU TAIFENG PHARMA CO LTD
View PDF5 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In vitro, ulipristal acetate binds competitively to progesterone, glucocorticoid, and androgen receptors, but has minimal affinity for estrogen and mineralocorticoid receptors

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
  • Ulipristal acetate dispersible tablet and preparation method thereof
  • Ulipristal acetate dispersible tablet and preparation method thereof
  • Ulipristal acetate dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The main ingredients and excipients of Ulipristal Acetate Dispersible Tablets (1000 tablets) are as follows:

[0033] Ulipristal acetate 30 g (10%)

[0034] Lactose 166 g (55.33%)

[0035] Mannitol 50 g (16.67%)

[0036] Povidone K30 30 g (10%)

[0037] Dioctyl sodium sulfosuccinate 6 g (2%)

[0038] Croscarmellose Sodium 15 g (5%)

[0039] Magnesium stearate 3 g (1%).

[0040] The preparation method of above-mentioned ulipristal acetate dispersible tablet is as follows:

[0041] (1) Weigh the main ingredients and auxiliary materials according to the weight percentage, and pass through 80-mesh sieve respectively, and set aside;

[0042] (2) Povidone K30 is dissolved in an ethanol solution with a mass fraction of 75% to obtain a povidone solution, and the povidone mass fraction in the povidone solution is 20%; dioctyl sulfosuccinate Add sodium and ulipristal acetate to the povidone solution and mix well;

[0043] (3) Mix lactose, mannitol and croscarmellose sodiu...

Embodiment 2

[0047] The main ingredients and excipients of Ulipristal Acetate Dispersible Tablets (1000 tablets) are as follows:

[0048] Ulipristal acetate 30 g (10%)

[0049] Lactose 155 g (51.67%)

[0050] Microcrystalline Cellulose 46 g (15.33%)

[0051] Povidone K30 45 g (15%)

[0052] Sodium dodecylbenzenesulfonate 6 g (2%)

[0053] Crospovidone 15 g (5%)

[0054] Glyceryl Behenate 3 g (1%).

[0055] The preparation method of above-mentioned ulipristal acetate dispersible tablet is as follows:

[0056] (1) Weigh the main ingredients and auxiliary materials according to the weight percentage, and pass through 80-mesh sieve respectively, and set aside;

[0057] (2) Povidone K30 is dissolved in an ethanol solution with a mass fraction of 80% to obtain a povidone solution, and the mass fraction of povidone in the povidone solution is 30%; sodium lauryl sulfate and acetic acid Ulipristal is added to the povidone solution and mixed;

[0058] (3) Mix lactose, microcrystalline cellul...

Embodiment 3

[0062] The main ingredients and excipients of Ulipristal Acetate Dispersible Tablets (1000 tablets) are as follows:

[0063] Ulipristal acetate 30 g (10%)

[0064] Mannitol 136 g (45.33%)

[0065] Macrogol 6000 75 g (25%)

[0066] Povidone K30 30 g (10%)

[0067] Tween 80 9 g (3%)

[0068] Low-substituted hydroxypropyl cellulose 15 g (5%)

[0069] Stearic acid 3 g (1%)

[0070] Colloidal silicon dioxide 2 g (0.67%).

[0071] The preparation method of above-mentioned ulipristal acetate dispersible tablet is as follows:

[0072] (1) Weigh the main ingredients and auxiliary materials according to the weight percentage, and pass through 80-mesh sieve respectively, and set aside;

[0073] (2) Povidone K30 was dissolved in an ethanol solution with a mass fraction of 75% to obtain a povidone solution, and the mass fraction of povidone in the povidone solution was 30%; He added to povidone solution and mixed well;

[0074] (3) Mix mannitol, polyethylene glycol 6000, and low-sub...

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
quality scoreaaaaaaaaaa
Login to View More

Abstract

The invention discloses a ulipristal acetate dispersible tablet, which consists of the following components in percentage by weight: 3-15% of ulipristal acetate, 60-90% of a filler, 5-30% of povidone,2-7.5% of a surfactant, 2-5% of a disintegrant and 0.05-2% of a lubricant. The invention also discloses a preparation method of the ulipristal acetate dispersible tablet, wherein the preparation method comprises the following steps: dissolving the povidone in an ethanol solution, and then sequentially adding the surfactant and the ulipristal acetate, so that a prepared material is obtained; and uniformly mixing the filler and the disintegrant, adding the prepared material, implementing granulating and drying, straightening particles, adding the lubricant, uniformly mixing the materials and conducting tabletting, so that the dispersible tablet is obtained. The dispersible tablet prepared by the invention is high in disintegration rate, high in dissolution rate, good in dispersion uniformity and high in ulipristal acetate content; and the dispersible tablet is convenient to take and convenient to carry, and the compliance of clinical administration is greatly improved.

Description

technical field [0001] The invention belongs to the field of ulipristal acetate preparations, in particular to a ulipristal acetate dispersible tablet and a preparation method thereof. Background technique [0002] Ulipristal acetate, ulipristal acetate, chemical name: 17α-acetoxy-11β-(4-N,N-dimethyl-amino)-phenyl)-19-norpregna-4,9-di ene-3,20-dione. Developed by HRA Pharmaceuticals, it is mainly used as an emergency contraceptive for women to use within 5 days after unprotected sexual intercourse or contraceptive failure. In May 2009, it passed the review of the European pharmaceutical department and was launched in 22 European countries and Australia in October. The trade name is EllaOne®. In August 2010, Ulipristal acetate was approved by the U.S. FDA under the trade name Ella®. [0003] Mechanism of Action: Ulipristal acetate is a synthetic selective progesterone receptor modulator (SPRM). In vitro, ulipristal acetate competitively binds to progesterone, glucocorticoi...

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): A61K9/20A61K31/57A61K47/10A61K47/26A61P15/18
CPCA61K31/57A61K9/2018A61K9/2095
Inventor 沙薇高敬轩李婷张兴爽王国景
Owner ZHENGZHOU TAIFENG PHARMA CO LTD
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