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Medicinal solid preparation of tolvaptan and preparation method

A solid preparation, tolvaptan technology, applied in the field of pharmaceutical preparations, can solve the problems of large material loss, many types of organic solvents, poor control of the particle size of amorphous substances, etc., and achieve high bioavailability and good bioavailability Effect

Pending Publication Date: 2020-11-06
FUAN PHARMA LYBON PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In the Chinese patent CN107963991A, in order to improve the solubility, tolvaptan is dissolved and re-precipitated, and then freeze-dried to obtain the amorphous substance; there are many types of organic solvents used, which is not conducive to the concept of green chemistry; and this technology is not easy to control the particle size of the amorphous substance
[0008] The authorized patent CN102406622B of Zhejiang Huahai Pharmaceutical Co., Ltd. uses spray drying to process tolvaptan, but does not mention the control of particle size
[0009] The authorized patent CN102366412B of Sichuan Baili Pharmaceutical Co., Ltd. mentions that tolvaptan spray powder is pulverized and sieved to control the particle size.

Method used

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  • Medicinal solid preparation of tolvaptan and preparation method
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Examples

Experimental program
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Effect test

Embodiment 1

[0032] Embodiment 1 Preparation of Tolvaptan Solid Formulation Tablet

[0033] Mix 1:0.5 tolvaptan and hydroxypropyl cellulose, add absolute ethanol and dichloromethane to dissolve completely, carry out spray drying, adjust the air inlet temperature at 130 degrees, spray pressure at 0.06MPa, liquid delivery speed 20rpm, air volume 0.3m 3 / h, obtain solid dispersion amorphous powder, measure that its particle diameter D90 is 21 microns.

[0034] Adopt above-mentioned process gained spray-dried amorphous powder, carry out tolvaptan medicine solid preparation preparation by fluidized bed process, obtain tolvaptan tablet, prescription is as follows:

[0035] Table 1 Example prescription

[0036]

[0037] Preparation method: Weigh microcrystalline cellulose, corn starch, lactose and tolvaptan solid dispersion powder, disperse through a 60-mesh sieve; add the binder solution prepared by hydroxypropyl cellulose, and perform one-step fluidized bed granulation and drying; then ad...

Embodiment 2

[0038] Example 2 Preparation of Tolvaptan Solid Formulation Tablet

[0039] Mix 1:0.5 tolvaptan and hydroxypropyl cellulose, add absolute ethanol and dichloromethane to dissolve completely, and carry out spray drying; adjust the air inlet temperature at 130 degrees, spray pressure at 0.045MPa, liquid delivery speed 25rpm, air volume 0.3m 3 / h, obtain solid dispersion amorphous powder, measure that its particle diameter D90 is 39 microns.

[0040] The spray-dried amorphous powder obtained in the above process is used to prepare the tolvaptan drug solid preparation through a fluidized bed process to obtain tolvaptan tablets. The granulation prescription process is the same as in Example 1.

Embodiment 3

[0041] Example 3 Preparation of Tolvaptan Solid Formulation Tablet

[0042] Mix 1:0.5 tolvaptan and hydroxypropyl cellulose, add absolute ethanol and dichloromethane to dissolve completely, and carry out spray drying; adjust the air inlet temperature at 130 degrees, the spray pressure at 0.03MPa, and the liquid delivery speed 25rpm, air volume 0.3m 3 / h, obtain solid dispersion amorphous powder, measure that its particle diameter D90 is 56 microns.

[0043] The spray-dried amorphous powder obtained in the above process is used to prepare the tolvaptan drug solid preparation through a fluidized bed process to obtain tolvaptan tablets. The granulation prescription process is the same as in Example 1.

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Abstract

The invention discloses a medicinal solid preparation containing tolvaptan and a preparation method. The preparation method comprises steps of converting active pharmaceutical ingredients of tolvaptaninto amorphous forms by spray-drying. The preparation method is characterized by controlling the amorphous solid dispersible powder to be 35-80 [mu]m in particle size D90. The preparation method alsocomprises steps of adding lactose, corn starch, microcrystalline cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, magnesium stearate and other auxiliary materials, and conducting granulation through a fluidized bed to obtain the medicinal solid preparation of tolvaptan with good in-vivo solubility and high bioavailability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical solid preparation of tolvaptan and a preparation method thereof. Background technique [0002] Tolvaptan was developed by Otsuka Pharmaceutical Company of Japan, and it was launched in the United States and Europe in 2009 under the trade name: SAMSCA. 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 a selective V2 vasopressin receptor antagonist that can be used to treat hyponatremia caused by congestive heart failure, liver cirrhosis, and antidiuretic hormone hyposecretion syndrome. Tolvaptan pharmaceutical solid preparations can increase the concentration of sodium ions in plasma and help excrete excess water from urine. [0005] Tolvaptan BCS is classified as Class IV, insoluble and difficult ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K47/38A61K47/26A61K47/36A61K31/55A61P3/12
CPCA61K9/1652A61K9/1623A61K9/1682A61K9/2095A61K9/2054A61K9/2059A61K9/2018A61K31/55A61P3/12
Inventor 张涛赵小洁王立
Owner FUAN PHARMA LYBON PHARMA TECH
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