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
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  • 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

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  • 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

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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.

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Abstract

The invention discloses a tolvaptan preparation containing micronized tolvaptan and water-soluble auxiliary materials, each tablet contains tolvaptan 7.5mg-60mg and the 90% cumulative particle size of tolvaptan is not greater than 75 microns; Each tablet contains no more than 60% of the weight of the tablet, and the weight-number ratio of tolvaptan to the water-soluble auxiliary material is 1:2.5-1:10. The invention solves the problem of poor compliance of the tolvaptan tablet during use, and provides a new alternative 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

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Application Information

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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
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