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Tolvaptan tablet

A technology for tolvaptan and tolvaptan tablets, which is applied in the field of tolvaptan tablets and a preparation thereof, can solve the problems of poor solubility of tolvaptan, failure to solve the dissolution rate of tolvaptan, and the like, and achieves dissolution The effect of stable in vitro dissolution curve and high yield

Inactive Publication Date: 2017-12-05
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The existing technology adopts various methods to solve the technical obstacle of poor solubility of tolvaptan, but none of them can solve the dissolution rate of tolvaptan during 0 days or long-term storage, and fail to solve the problem of tolvaptan within the validity period. Can release more than 85% within 15 minutes

Method used

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  • Tolvaptan tablet
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Examples

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Effect test

Embodiment 1

[0016] prescription:

[0017] Tolvaptan 30g

[0018] Sorbitol 30g

[0019] Calcium hydrogen phosphate 150g

[0020] Micronized silica gel 5g

[0021] Magnesium Stearate 1g

[0022] Preparation method: heat and melt sorbitol in a hot-melt extruder, then add tolvaptan to melt, extrude the molten liquid to make granules, and directly compress it with calcium hydrogen phosphate, micro-powder silica gel, and magnesium stearate

Embodiment 2

[0024] prescription:

[0025] Tolvaptan 30g

[0026] Sorbitol 150g

[0027] Calcium hydrogen phosphate 200g

[0028] Micronized silica gel 5g

[0029] Magnesium Stearate 2g

[0030] Preparation method: heat and melt sorbitol in a hot-melt extruder, then add tolvaptan to melt, extrude the molten liquid to make granules, and directly compress it with calcium hydrogen phosphate, micro-powder silica gel, and magnesium stearate.

Embodiment 3

[0032] prescription:

[0033] Tolvaptan 30g

[0034] Sorbitol 90g

[0035] Calcium hydrogen phosphate 220g

[0036] Micronized silica gel 10g

[0037] Magnesium Stearate 2g

[0038] Preparation method: heat and melt sorbitol in a hot-melt extruder, then add tolvaptan to melt, extrude the molten liquid to make granules, and directly compress it with calcium hydrogen phosphate, micro-powder silica gel, and magnesium stearate.

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Abstract

The present invention relates to a kind of tolvaptan tablet, and the invention belongs to the new technical field of medicine manufacturing, specifically relates to tolvaptan tablet and a kind of preparation method thereof, and this tablet is tolvaptan as main component, is produced by tolvaptan Protan solid dispersion granules and auxiliary materials are directly compressed into tablets. The tolvaptan tablet of the invention solves the problem of in vitro dissolution of the tolvaptan, improves the curative effect of the drug, and has a more ideal therapeutic effect.

Description

technical field [0001] The invention belongs to the field of new technology for medicine manufacture, and in particular relates to a tolvaptan tablet and a preparation method thereof. Background technique [0002] Tolvaptan was developed by Japan’s Otsuka Pharmaceutical Company and was launched in the United States and Europe in 2009. Its chemical name is: N-[4-[(5R)-7-chloro-5-hydroxy-2,3,4,5- Tetrahydro-1-benzazepine-1-formyl]-3-methylphenyl]-2-methylbenzamide, mainly used in the treatment of heart failure, liver cirrhosis and antidiuretic hormone deficiency syndrome Hyponatremia in patients. [0003] Tolvaptan is a category IV drug in the BCS classification, that is, a drug with low solubility and low permeability. For poorly soluble drugs, dissolution is the rate-limiting process of absorption and is often the most important factor affecting their bioavailability. [0004] The existing technology adopts various methods to solve the technical obstacle of poor solubilit...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/55A61K47/10A61P9/04A61P1/16A61P3/12
CPCA61K31/55A61K9/2018A61K9/2095
Inventor 严洁王志凤
Owner TIANJIN HANKANG PHARMA BIOTECH
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