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Soft nintedanib ethanesulfonate capsule and preparation method thereof

A technology of nintedanib ethanesulfonate and soft capsules, which is applied in the field of medicine, can solve the problems that the physical stability of the undisclosed suspension has an important impact, high production costs, and cumbersome processes, etc., so as to improve product stability and reduce Production cost and process requirements, the effect of reasonable process

Inactive Publication Date: 2018-05-29
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Although the patent CN102056598 discloses the preparation method of the content suspension of the soft capsule, and points out that the physical stability of the content suspension is crucial to the release of the active substance from the dosage form, it does not disclose the impact of the particle size of the raw material on the physical stability of the suspension. Stability has a major impact
[0013] Purchased 3 batches of nintedanib soft capsules developed by Boehringer Ingelheim. The D90 of the raw materials in the content was determined to be within the range of 30μm±3μm. The particle size control is relatively fine, the production cost is high, and the process is cumbersome and needs to be crushed repeatedly Sieve treatment, and there is a problem of easy curing

Method used

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  • Soft nintedanib ethanesulfonate capsule and preparation method thereof
  • Soft nintedanib ethanesulfonate capsule and preparation method thereof
  • Soft nintedanib ethanesulfonate capsule and preparation method thereof

Examples

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Embodiment 1

[0034] A nintedanib ethanesulfonate soft capsule, the content of which is composed of the following raw materials in parts by weight: 18.06 g of nintedanib ethanesulfonate, 15.0 g of medium-chain triglycerides, 7 g of stearin and 0.05 g of lecithin .

[0035] Preparation method: crush nintedanib ethanesulfonate through a 200-mesh sieve, measure the average particle size D90 to be 80 μm±5 μm, and set aside. Melt medium-chain triglycerides, lecithin, and stearin, then add raw materials, homogenize, and degas.

Embodiment 2

[0037] A nintedanib ethanesulfonate soft capsule, the raw and auxiliary materials used are the same as in Example 1, and the preparation method is as follows: nintedanib ethanesulfonate is pulverized through a 230-mesh sieve, and the average particle size D90 is 60 μm±5 μm. Melt medium-chain triglycerides, lecithin, and stearin, then add raw materials, homogenize, and degas.

Embodiment 3

[0039] A nintedanib ethanesulfonate soft capsule, the raw and auxiliary materials used are the same as in Example 1, and the preparation method is: nintedanib ethanesulfonate is pulverized through a 325 mesh sieve, and the average particle size D90 is 40 μm±3 μm. Melt medium-chain triglycerides, lecithin, and stearin, then add raw materials, homogenize, and degas.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a content of a soft nintedanib ethanesulfonate capsule. The content is prepared from nintedanib ethanesulfonate, wherein the grain size distribution range of the nintedanib ethanesulfonate is D90 from 40 mu m to 80 mu m. By studying the stability of a suspension system of the content of the soft nintedanib ethanesulfonate capsule and determining in-vivo pharmacokinetic parameters of wistar rats, the influence of the grain size of the nintedanib esylate as a raw material on the physical stability and bioavailability of the soft nintedanib ethanesulfonate capsule is discovered to be great, and the soft nintedanib ethanesulfonate capsule is ultimately discovered to have good physicalstability and be similar to pharmacokinetic behaviors of reference preparations in terms of absorption when the grain size of the nintedanib ethanesulfonate material is 40 mu m to 80 mu m, and moreover, since the grain size control range of the raw material is broadened, the production cost and the technological requirements are reduced. The invention further provides the preparation method of the content, the process of which is reasonable.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a nintedanib ethanesulfonate soft capsule and a preparation method thereof. Background technique [0002] Idiopathic pulmonary fibrosis is a chronic progressive disease of unknown etiology characterized by progressive fibrotic damage in the lungs, and is the most common idiopathic interstitial pneumonia. There is currently no preventive method or internationally recognized curative treatment other than lung transplantation. The worldwide prevalence reaches 14-43 cases / 100,000 people. Based on this, it is estimated that there are about 600,000 patients with idiopathic pulmonary fibrosis in my country. Due to the rapid progression and poor prognosis, the disease is highly morbid and fatal. Patients have an average life expectancy of 3-5 years from diagnosis, or 4-6 years from onset of symptoms. [0003] Idiopathic pulmonary fibrosis has long been recognized as an ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K47/14A61K47/24A61K47/12A61K31/496A61P11/00
CPCA61K9/4808A61K9/4858A61K31/496
Inventor 苗得足胡清文王宏光吕帅艾玉曾丽丽
Owner REYOUNG PHARMA
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