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Nintedanib inclusion compound and preparation and preparation method thereofof preparation

A technology of nintedanib and clathrates, which is applied in the directions of pharmaceutical formulation, pill delivery, drug combination, etc., can solve the problems of residual organic solvents, high equipment cost, and difficulty in scale-up production, so as to promote drug efficacy, improve solubility, Ease of production

Pending Publication Date: 2018-06-12
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, related literatures reported that the solid dispersion of nintedanib was prepared by electrostatic spraying technology, which can improve the solubility of the drug in the medium of pH 6.8 plus 0.5% Tween 80, but this method has high equipment costs and is not easy to scale up Production, possible residual organic solvents and other disadvantages

Method used

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  • Nintedanib inclusion compound and preparation and preparation method thereofof preparation
  • Nintedanib inclusion compound and preparation and preparation method thereofof preparation
  • Nintedanib inclusion compound and preparation and preparation method thereofof preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] In this example, the purified water and hydroxypropyl-β-cyclodextrin were weighed according to the prescription ratio in Table 4 to make them fully dissolved, then slowly added nintedanib ethanesulfonate under stirring in a water bath at 55°C, and continued After stirring for 4 hours, it was divided into vials and freeze-dried. The freeze-dried samples were transferred from the vials and ground in a mortar to obtain a freeze-dried powder. The ingredients were mixed according to the prescription ratio in Table 4 for 5 minutes, and tableted to prepare nintedanib inclusion compound tablets.

[0057] The prescription form of table 4 embodiment 1

[0058]

Embodiment 2

[0060] In this example, the purified water and sulfobutyl ether-β-cyclodextrin were weighed according to the prescription ratio in Table 5 to make them fully dissolved, then slowly added nintedanib ethanesulfonate under stirring at room temperature, and continued to stir for 6 hours Finally, it is divided into vials and freeze-dried. The freeze-dried samples are transferred from the vials and ground in a mortar to obtain a freeze-dried powder. The ingredients were mixed according to the prescription ratio in Table 5 for 5 minutes, and tableted to prepare nintedanib inclusion compound tablets.

[0061] The prescription form of table 5 embodiment 2

[0062]

[0063]

Embodiment 3

[0065] In this example, weigh the purified water and sulfobutyl ether-β-cyclodextrin according to the prescription ratio in Table 6 to make them fully dissolved, slowly add nintedanib ethanesulfonate under stirring at room temperature, and continue stirring for 6 hours Finally, the inclusion solution of nintedanib ethanesulfonate was obtained. The nintedanib ethanesulfonate inclusion solution is used as the fluidized bed granulation liquid, and the microcrystalline cellulose is used as the granulation substrate for fluidized bed granulation to obtain the nintedanib ethanesulfonate dry granules, and then add the prescription amount The crospovidone and magnesium stearate are compressed into tablets to prepare nintedanib inclusion compound tablets.

[0066] The prescription form of table 6 embodiment 3

[0067] components

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Abstract

The invention provides a Nnintedanib inclusion compound and preparation and a preparation method thereofof the preparation. The inclusion compound comprises a main drug and an inclusion material, wherein the main drug is Nnintedanib or pharmaceutically acceptable salt in pharmacy, and the inclusion material is cyclodextrin or a derivative of cyclodrxtrin. The inclusion compound can sharply improvethe drug solubility of a simulated intestinal solution, the probability of the drug being separated out in the intestinal canal is lowered, and accordingly the bioavailability of the drug is improved. The inclusion compound and the preparation prepared from the inclusion compound and pharmaceutically acceptable ingredients in the pharmacy can outstandingly improve the dissolution degree and the dissolution rate of the drug in the simulated intestinal solution, the bioavailability of the drug is improved, meanwhile, the inclusion compound and the preparation have good stability, thus the flexibility and compliance of drug taking of patients are improved, and accordingly the treatment effect of the drug is improved. In addition, the invention provides a preparation method of the medicinal preparation of the Nnintedanib inclusion compound, no specific equipment is needed, the technology is simple, the production cost is low, and the preparation method is suitable for industrialized production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular, the invention relates to a nintedanib inclusion compound, a preparation and a preparation method thereof. Background technique [0002] Nintedanib is an oral triple angiokinase inhibitor developed by Boehringer Ingelheim, which can simultaneously block vascular endothelial growth factor receptor, platelet-derived growth factor receptor and fibroblast growth factor receptor signal transduction. Accumulating scientific evidence shows that these three different angiokinase receptors not only play an important role in angiogenesis, but also play an important role in tumor growth and metastasis. In October 2014, the US FDA approved (nintedanib) for the treatment of idiopathic pulmonary fibrosis (IPF), becoming the first tyrosine kinase inhibitor (TKI) approved for the treatment of IPF. [0003] Nintedanib is considered to have good application prospects in the fields of an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/496A61K9/20A61K9/48A61P11/00
CPCA61K9/20A61K9/48A61K31/496
Inventor 许玉珍黄心游劲松黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD
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