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Tolvaptan solid preparation

A technology for tolvaptan and solid preparation, which is applied in the field of solid preparations containing tolvaptan, can solve the problems of unfavorable product promotion, complicated hydroxypropyl beta cyclodextrin process and high production cost

Active Publication Date: 2012-04-11
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of hydroxypropyl beta cyclodextrin in this process is not only complicated in process but also high in production cost, which is not conducive to product promotion

Method used

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  • Tolvaptan solid preparation
  • Tolvaptan solid preparation
  • Tolvaptan solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Component

[0045] The preparation process of tolvaptan tablets: add povidone and tolvaptan into 400ml absolute ethanol and heat until the solution is clear, weigh the lactose, part of pregelatinized starch, and microcrystalline cellulose into the Glatt flow The fluidized bed adopts a one-step granulation process for granulation. After the granulation is completed, the water content is measured and the granulation is passed through a 30-mesh sieve. After adding low-substituted hydroxypropyl cellulose and mixing uniformly, add magnesium stearate, mix for 5 minutes and then press tablets.

Embodiment 2

[0047] Component

[0048] The preparation process of the composition of tolvaptan and copovidone: adding copovidone and tolvaptan into 750ml of acetone and stirring until the solution is clear, and spray drying to obtain the composition of tolvaptan and copovidone.

[0049] Component

[0050] Preparation of tolvaptan tablets: Weigh the prescribed amount of tolvaptan composition, lactose, microcrystalline cellulose, and low-substituted hydroxypropyl cellulose, and mix them uniformly by an equal addition method, then add magnesium stearate and mix for 5 minutes After pressing the tablet.

Embodiment 3

[0052] Component

[0053] Tolvaptan and povidone composition preparation process: Povidone and tolvaptan are added to a mixed solvent of 180ml absolute ethanol and 520ml dichloromethane, after dissolving, tolvaptan is obtained by drying under reduced pressure combination.

[0054] Weigh an appropriate amount of the povidone, tolvaptan, and the obtained combination of tolvaptan and povidone for the above prescription, and use differential calorimetry (DSC) measurement and X-powder diffraction (XRPD) Measure, get attached Figure 1-6 The results showed that the tolvaptan and povidone composition obtained were amorphous in tolvaptan.

[0055] Component

[0056] The preparation process of tolvaptan tablets: Weigh the prescribed amount of tolvaptan composition, lactose, partially pregelatinized starch, microcrystalline cellulose, and cross-linked povidone, and mix them evenly by equal addition, then add Magnesium stearate, mixed for 5 minutes and then compressed.

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PUM

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Abstract

The invention provides a tolvaptan solid preparation. The solid preparation is prepared from tolvaptan amorphous composition which is prepared by dissolving and drying tolvaptan and a carrier, as well as other pharmaceutically acceptable auxiliary materials, wherein the weight ratio of tolvaptan to the carrier is between 1:1.5 and 1:5. The preparation has the advantages of good solubility, good stability and high bioavailability.

Description

Technical field [0001] The invention relates to a solid preparation containing tolvaptan. Background technique [0002] Tolvaptan was developed by Japan's Otsuka Pharmaceutical Co., Ltd., and was launched in the United States and Europe in 2009, under the trade name: SAMSCA. It is mainly used to treat hyponatremia in patients with heart failure, liver cirrhosis and syndrome of insufficient antidiuretic hormone secretion. Tolvaptan chemical name: N-[4-[(5R)-7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-formyl]- 3-methylphenyl]-2-methylbenzamide, its structural formula is as follows: [0003] [0004] Tolvaptan is the first oral non-peptide vasopressin V approved by the FDA 2 Receptor antagonists only need to be taken orally once a day. Tolvaptan is a selective arginine vasopressin V 2 Receptor antagonist, can prevent arginine vasopressin (AVP) from interacting with V in the distal nephron 2 Receptor binding produces drainage and diuresis without loss of electrolytes, so it...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K31/55A61K47/32A61K47/36A61K47/38A61P3/12
Inventor 魏方代孔恩葛光华彭俊清胡李斌李巧霞
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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