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Tolvaptan oral solid medicinal composition and preparation method thereof

A technology of tolvaptan and its composition, which is applied in the field of tolvaptan oral solid pharmaceutical composition and its preparation, can solve the problem that the process of amorphous tolvaptan composition is not easy to control, the preparation method is complicated, and it is not suitable for industrialization Production and other issues, to achieve the effect of being suitable for industrialized large-scale production, simple and easy process, and full absorption

Active Publication Date: 2011-11-02
福安药业集团庆余堂制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation method of this patent application is too complicated, and the process for preparing the amorphous tolvaptan composition is not easy to control, and is not suitable for industrial production

Method used

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  • Tolvaptan oral solid medicinal composition and preparation method thereof
  • Tolvaptan oral solid medicinal composition and preparation method thereof
  • Tolvaptan oral solid medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Embodiment 1: tolvaptan tablet

[0072] Preparation of tolvaptan solution with binder:

[0073] Dissolve 210g of tolvaptan in 6L of pure ethanol solution, heat and stir to make the solution clear, then add 42g of polyvinylpyrrolidone, stir to make it dissolve completely, and obtain a tolvaptan solution containing a binder.

[0074] Preparation of drug-loaded particles:

[0075] 560 g of lactose was placed in a fluidized bed granulator, and the tolvaptan solution containing the binder prepared in the previous step was used for fluidized bed granulation, followed by drying to obtain drug-loaded granules.

[0076] Mixed processing:

[0077] Mix 58g of drug-loaded granules obtained in the previous step, 26g of microcrystalline cellulose, 3.0g of cross-linked polyvinylpyrrolidone and 0.5g of magnesium stearate, punch tablets with 8.5mm dimples to obtain a tablet weight of 175mg containing 30mg of tolvap Tan tablet, about 5Kg hardness.

Embodiment 2

[0078] Embodiment 2: tolvaptan tablet

[0079] Mix the drug-loaded granule obtained in the embodiment 1 of 58g, the microcrystalline cellulose of 26g, the croscarmellose sodium of 3.0g and the magnesium stearate of 0.65g, with 8.5mm dimple punching tablet tablet weight is 175mg tablet containing 30mg tolvaptan, hardness about 5Kg.

Embodiment 3

[0080] Embodiment 3: tolvaptan tablet

[0081] Mix the drug-loaded granules obtained in the embodiment 1 of 58g, the microcrystalline cellulose of 26g, the polacrilin potassium of 3.0g and the magnesium stearate of 0.65g, with 8.5mm dimple punching tablet weight is 175mg and contains 30mg trolley The tablet of vaptan has a hardness of about 5Kg.

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Abstract

The invention provides a tolvaptan oral solid medicinal composition. The tolvaptan oral solid medicinal composition is prepared from the following components in percentage by weight: 3 to 50 percent of tolvaptan, 1 to 10 percent of adhesive, 20 to 80 percent of hydrophilic carrier, 0 to 20 percent of disintegrant, 5 to 60 percent of filler, 0 to 5 percent of flow aid, and 0.1 to 3.0 percent of lubricant. The tolvaptan medicinal composition is an oral solid preparation and is preferably tablets and capsules. The invention also provides a method for preparing the medicinal composition. The tolvaptan oral solid medicinal composition has good disintegration performance and dissolution performance; the composition has lower impurity content and is steadier; the preparation process is simple and easy; and the method is suitable for industrialized mass production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a tolvaptan oral solid pharmaceutical composition and a preparation method thereof. Background technique [0002] Tolvaptan is an oral selective non-peptide novel arginine vasopressin V developed by Otsuka Corporation of Japan 2 receptor antagonists. Approved by the FDA in 2009, it is used for the treatment of hyponatremia (serum sodium <125mg / L, or mild symptoms) with normal blood volume or hypervolemia in the circulatory system, including heart failure, liver cirrhosis, and syndrome of abnormal secretion of antidiuretic hormone of patients. Its chemical name is N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepine -1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide, the structural formula is as follows: [0003] [0004] Tolvaptan structure [0005] Tolvaptan belongs to BCS Class IV drugs, which are low solubility and low permeability drugs. Althoug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/20A61K9/48A61K31/55A61K47/38A61K47/36A61K47/32A61P3/12
Inventor 张先华徐霞刘瑞娥陈小勇张稳稳
Owner 福安药业集团庆余堂制药有限公司
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