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

Tolvaptan preparation containing micronized tolvaptan and water-soluble auxiliary materials

A water-soluble excipient, tolvaptan technology, applied in the field of tolvaptan preparations, orally disintegrating tablets or orally dissolving tablets, can solve a large number of organic solvents and other problems, and achieve improved dissolution rate, good taste and good absorption Effect

Inactive Publication Date: 2017-06-23
TIANJIN TAIPU PHARMA SCI & TECH DEV
View PDF1 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent JP11021241A applied by the original research manufacturer Japan Otsuka Pharmaceutical Co., Ltd. discloses that tolvaptan and hydroxypropyl cellulose are dissolved in a mixed solvent of dichloromethane and ethanol, and spray-dried to form a pharmaceutical composition to improve its solubility, but in A large amount of organic solvent is required in the preparation process, and explosion-proof is required in production

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
  • Tolvaptan preparation containing micronized tolvaptan and water-soluble auxiliary materials
  • Tolvaptan preparation containing micronized tolvaptan and water-soluble auxiliary materials
  • Tolvaptan preparation containing micronized tolvaptan and water-soluble auxiliary materials

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025]

[0026] Process: Mix the prescribed amount of tolvaptan, lactose, microcrystalline cellulose, sucralose, hydroxypropyl cellulose and low-substituted hydroxypropyl cellulose (50%), add 1% lauryl sulfate Sodium solution is used as a wetting agent to make soft materials, granulated with a 20-mesh screen, dried at 55°C, and granulated, adding low-substituted hydroxypropyl cellulose (50%), silicon dioxide and magnesium stearate in the prescribed amount, Mix well and compress into tablets.

Embodiment 2

[0028] Tolvaptan was pulverized until the D90 particle size was not greater than 75 microns, and about 1000 tablets were prepared according to Example 1, each containing 15 mg of tolvaptan.

Embodiment 3

[0030] Tolvaptan was pulverized until the D90 particle size was no more than 50 microns, and about 1000 tablets were prepared according to Example 1, each containing 15 mg of tolvaptan.

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
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a tolvaptan preparation containing micronized tolvaptan and water-soluble excipients. Each tablet contains tolvaptan 7.5 mg-60 mg and 90% of the cumulative particle size of tolvaptan is not greater than 75 microns; Each tablet contains no more than 60% of the tablet weight as water-soluble excipients, and the weight ratio of tolvaptan to water-soluble excipients is 1:2.5~1:10. The invention solves the problem of poor compliance during the use of tolvaptan tablets and provides a new and excellent dosage form for clinical use.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and relates to orally disintegrating tablets or orally dissolving tablets of tolvaptan. More specifically, it is a tolvaptan formulation comprising micronized tolvaptan and water-soluble excipients. Background technique [0002] Tolvaptan, its chemical name is: N-[4-[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-methyl Acyl]-3-methylphenyl]-2-methylbenzamide is a selective antidiuretic hormone V2 receptor antagonist. On May 19, 2009, the U.S. FDA approved the new molecular drug combination of Otsuka Pharm - Tolvaptan Tablets (trade name: Samsca) for the treatment of hypervolaemia or isovolumic hyponatremia Hyperemia with heart failure, liver cirrhosis, syndrome of abnormal secretion of antidiuretic hormone. [0003] Tolvaptan is a BCS Class IV drug, that is, a low-solubility and low-osmosis drug. Its dissolution is the rate-limiting step of drug absorption, and...

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): A61K9/20A61K31/55A61K47/26A61P3/12A61P9/04A61P1/16A61P5/00
CPCA61K31/55A61K9/0056A61K9/2018
Inventor 代奕许莉莉韩建萍王志鹏
Owner TIANJIN TAIPU PHARMA SCI & TECH DEV
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