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Tolvaptan composition and preparation method thereof

A technology of tolvaptan and its composition, which is applied in the field of tolvaptan composition and its preparation, can solve the problems of low oral bioavailability, etc., and achieve the effects of improving oral bioavailability, low cost, and simple preparation method

Active Publication Date: 2014-12-24
广州市美澳健生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Tolvaptan is effective in the treatment of hyponatremia caused by congestive heart failure, liver cirrhosis, and antidiuretic hormone deficiency syndrome, but its oral bioavailability is poor due to poor solubility in water

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Dissolve 0.1 g of urocanic acid in 100 mL of ethanol, then add 0.1 g of sodium stearyl fumarate to obtain a dispersion of the auxiliary material; dissolve 0.1 g of tolvaptan with 50 mL of ethanol to obtain a dispersion of the drug; Mix evenly with the drug dispersion, recover ethanol under vacuum at 40°C, and dry at 40°C for 6 hours to obtain the product.

Embodiment 2

[0014] Dissolve 0.1 g of urocanic acid in 100 mL of ethanol, then add 0.1 g of sodium stearyl fumarate to obtain a dispersion of the auxiliary material; dissolve 0.1 g of tolvaptan with 20 mL of ethanol to obtain a dispersion of the drug; Mix evenly with the drug dispersion, recover ethanol under vacuum at 40°C, and freeze-dry to obtain the product.

Embodiment 3

[0016] Dissolve 0.1 g of urocanic acid in 200 mL of ethanol, then add 0.1 g of sodium stearyl fumarate to obtain a dispersion of the auxiliary material; dissolve 0.1 g of tolvaptan with 100 mL of ethanol to obtain a dispersion of the drug; Mix evenly with the drug dispersion, recover ethanol under vacuum at 30°C, and freeze-dry to obtain the product.

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PUM

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Abstract

The invention provides a tolvaptan composition with relatively high oral bioavailability and a preparation method of composition. The composition is characterized by comprising tolvaptan, sodium stearyl fumarate and urocanic acid, wherein the mass ratio of tolvaptan to sodium stearyl fumarate to urocanic acid is preferably 1 to 1 to 1. The preparation method comprises the following steps: dissolving urocanic acid by ethanol, and adding sodium stearyl fumarate to obtain auxiliary material dispersion liquid; dissolving tolvaptan by ethanol to obtain drug dispersion liquid; uniformly mixing the auxiliary material dispersion liquid with the drug dispersion liquid, recovering ethanol, and drying to obtain the composition.

Description

technical field [0001] The invention relates to a tolvaptan composition and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Tolvaptan is effective in the treatment of hyponatremia caused by congestive heart failure, liver cirrhosis, and antidiuretic hormone deficiency syndrome, but its oral bioavailability is very low due to poor solubility in water. Contents of the invention [0003] The object of the present invention is to provide a tolvaptan composition with higher oral bioavailability and a preparation method thereof. [0004] For the purpose of the above invention, the present invention provides the following technical solutions: [0005] Tolvaptan composition of the present invention is characterized in that containing tolvaptan, sodium stearyl fumarate and urocanic acid; The mass ratio of tolvaptan, sodium stearyl fumarate and urocanic acid is preferably 1:1:1. [0006] The method for the tolvaptan compos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55A61K9/19A61P3/12
Inventor 罗瑞雪
Owner 广州市美澳健生物科技有限公司