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Method for rapidly controlling and evaluating release of macitentan tablet

A macitentan, rapid control technology, applied in the field of medicine, can solve the problems of no patents for controlling and evaluating the release of macitentan tablets, etc., to ensure effectiveness and safety, improve production quality and requirements, and test quick effect

Inactive Publication Date: 2021-02-09
南京斯泰尔医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, the patents on macitentan tablet preparations are mainly on the prescription composition and preparation method, and there are no patents on controlling and evaluating the release of macitentan tablets

Method used

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  • Method for rapidly controlling and evaluating release of macitentan tablet
  • Method for rapidly controlling and evaluating release of macitentan tablet
  • Method for rapidly controlling and evaluating release of macitentan tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] In production, the raw material of macitentan obtained through the refining process of organic reagents generally has a larger particle size. Samples were taken for microscopic observation, such as figure 1 The physical form of the raw materials shown is flaky crystals, which are relatively brittle.

Embodiment 2

[0036] The macitentan raw material is pulverized by a jet mill to obtain raw materials with different particle sizes. Measure the particle size separately.

[0037] project d(0.1)μm d(0.5)μm d(0.9)μm raw material 1 9.043 43.841 91.298 raw material 2 7.395 25.901 51.082 raw material 3 1.236 9.777 36.03 raw material 4 0.751 2.882 9.807

[0038] Adopt above-mentioned raw material of different granularity to prepare macitentan tablet through identical process, carry out dissolution rate and release rate measurement respectively, take pH6.8 phosphate buffer solution 900ml as dissolution medium, rotating speed is 75 revolutions per minute, in 10 minutes, Sampling and testing at 15 minutes, 20 minutes, 30 minutes, 45 minutes and 60 minutes. Compared with the samples of commercially available preparations, comparative research was carried out.

[0039] Table 2 shows the release rate of macitentan tablets in Example 2.

[0040] ...

Embodiment 3

[0043] Dissolution determination is an important index to evaluate the dissolution behavior in vitro. The choice of the dissolution medium has an extremely important effect on the dissolution results. The same batch of macitentan tablets was adopted for dissolution and release determination, respectively adopting pH6.8 phosphate buffer solution containing different proportions of cetyltrimethylammonium bromide as the dissolution medium, and the rotating speed was 75 revolutions per minute, Samples were taken at 10 minutes, 15 minutes, 20 minutes, 30 minutes, 45 minutes and 60 minutes.

[0044] Table 3 shows the release rate of macitentan tablets in Example 3.

[0045]

[0046] Conclusion: The results of dissolution curves are quite different with different concentrations of cetyltrimethylammonium bromide in the dissolution medium. The discriminating power was weaker under the conditions of 0.05% and 0.1% cetyltrimethylammonium bromide in the dissolution medium, and the di...

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Abstract

The invention discloses an important method for rapidly controlling and evaluating the release of a macitentan tablet. The method comprises the following steps that the macitentan tablet is simply prepared, and the release speed is mainly influenced by controlling the particle size of a bulk drug and a dissolution medium; in the particle size range, the particle size of raw materials is preferablyabout 10-50 um; the dissolution medium is preferably selected from 0.02%-0.1% of hexadecyl trimethyl ammonium bromide; and high performance liquid chromatography is adopted for determination, and determination is completed within 3 minutes. The quality of the macitentan tablet meets the standard, the macitentan tablet has release similarity with similar preparations sold in the market, quality research and control are carried out before production, rework can be effectively reduced, the production cost is saved, energy consumption is reduced, and the production efficiency is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a method for rapidly controlling and evaluating the release of macitentan tablets. Background technique [0002] Pulmonary hypertension is an extremely serious disease, and patients often have shortness of breath, fainting, chest pain and edema. Moreover, the pulmonary hypertension of the patient will gradually increase, and in severe cases, the life span may even be shortened. [0003] Macitentan is a sulfadiazine derivative and an endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension to delay disease progression. [0004] The pharmacokinetics of macitentan is proportional to the dose (range of 1 mg to 30 mg), it is slowly absorbed after oral administration, and reaches the maximum plasma concentration in about 8 hours. [0005] Macitentan Tablets is an oral solid preparation, which can be further absorbed only by dissolution in the body, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/38A61K47/26A61K47/18A61K31/506A61P9/12A61P11/00G01N30/02G01N30/74
CPCA61K9/2013A61K9/2018A61K9/2054A61K31/506A61P9/12A61P11/00G01N30/02G01N30/74
Inventor 周国才雍永佳
Owner 南京斯泰尔医药科技有限公司
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