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Ceritinib medicinal composition

A technology for ceritinib and a composition, which is applied in the field of ceritinib pharmaceutical compositions and their preparation, can solve problems such as difficulty in rapid dissolution, and achieve the effects of avoiding delayed absorption in vivo, rapid dissolution, and sufficient dissolution

Active Publication Date: 2016-12-07
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is difficult for insoluble drugs to dissolve quickly under many prescription preparation conditions. The dissolution of such drugs often becomes the rate-limiting condition for drug absorption and rapid onset of action. Ceritinib is an insoluble drug, and there is currently no ceritinib The relevant technical literature of the Nigerian pharmaceutical composition is disclosed

Method used

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  • Ceritinib medicinal composition
  • Ceritinib medicinal composition
  • Ceritinib medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6 and comparative example 1-2

[0041] Examples 1-6 and Comparative Examples 1-2: Preparation of pharmaceutical compositions with different particle sizes of ceritinib

[0042] Preparation method: mix ceritinib with microcrystalline cellulose, low-substituted hydroxypropyl cellulose and carboxymethyl starch sodium evenly, add water for wet granulation, after drying, add silicon dioxide and magnesium stearate Mix well, and fill the final mixture into gelatin capsules to prepare capsules.

[0043] Table 1 The prescription composition of embodiment 1-6 and comparative example 1-3 ceritinib pharmaceutical composition

[0044] prescription

Weight (mg)

weight percentage

Ceritinib

150.0

40％

microcrystalline cellulose

205.5

54.8％

Low-substituted hydroxypropyl cellulose

7.5

2％

Carboxymethyl Starch Sodium

7.5

2％

silica

1.5

0.4％

Magnesium stearate

3.0

0.8％

gross weight

375.0

100％

[0045] Table 2 The part...

Embodiment 7

[0047] Embodiment 7: Dissolution and content investigation of the pharmaceutical composition prepared in Examples 1-6 and Comparative Examples 1-3

[0048] Dissolution: According to the dissolution determination method (the second method of appendix XC of the Chinese Pharmacopoeia in 2010), 900mL of 0.1M hydrochloric acid solution was used as the dissolution medium, and the rotating speed was 60 revolutions per minute. Operate according to the law, respectively at 5, 10, and 15 , Sampling for 30 minutes, filtered, and the filtrate was taken as the test solution. According to ultraviolet-visible spectrophotometry (Chinese Pharmacopoeia 2010 edition two appendix IVA), measure absorbance at 339nm wavelength place.

[0049] Content: Determined according to high performance liquid chromatography (Appendix VD of Part Two of the Chinese Pharmacopoeia 2010 Edition). Precisely measure 20 μL each of the test solution and the reference solution and inject them into the liquid chromatogr...

Embodiment 8-10 and comparative example 4-5

[0053] Examples 8-10 and Comparative Examples 4-5: Preparation of ceritinib pharmaceutical composition with different additions of disintegrants

[0054] The disintegrants are low-substituted hydroxypropyl cellulose and sodium starch glycolate, and the particle size D90 of ceritinib is 50.6 μm.

[0055] The preparation method refers to Example 1.

[0056] Table 4 The prescription composition of the pharmaceutical composition prepared with different additions of disintegrants

[0057]

[0058] Remarks: the weight unit in the above table is mg; the percentage is the weight percentage of the pharmaceutical composition, and the unit is %; the total weight of the composition is 375.0mg.

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Abstract

The invention relates to a ceritinib medicinal composition. The medicinal composition contains ceritinib and at least one pharmaceutically acceptable carrier, and the raw material particle size D90 is 20-80 [mu]m. The medicinal composition has the advantages of rapid release and stable quality. The invention also relates to a preparation method of the medicinal composition. The preparation method has the advantages of simple preparation process, and suitableness for industrial large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ceritinib pharmaceutical composition and a preparation method thereof. Background technique [0002] Ceritinib, English name: Ceritinib, chemical name: 5-chloro-N 4 -[2-(isopropylsulfonyl)phenyl]-N 2 -[5-Methyl-2-isopropoxy-4-(piperidin-4-yl)phenyl]-2,4-pyrimidinediamine, structural formula: [0003] Ceritinib is an antineoplastic drug developed by Novartis. It was approved by the FDA in April 2014. The trade name is For the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) whose disease has progressed or cannot be tolerated after crizotinib treatment. Ceritinib is a kinase inhibitor. The inhibitory targets of ceritinib include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR) and ROS1. Among these targets, ceritinib has the strongest activity against ALK. The ALK gene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61P35/00
Inventor 刘峰张红芬杜丹郭文敏王燕娇刘静媛
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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