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Ceritinib pharmaceutical composition

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

Active Publication Date: 2020-06-23
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 pharmaceutical composition
  • Ceritinib pharmaceutical composition
  • Ceritinib pharmaceutical 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 particle size of raw materials in the pharmaceutical...

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] Refer to Example 1 for the preparation method.

[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 pharmaceutical composition of ceritinib, which contains ceritinib and at least one pharmaceutically acceptable carrier, the particle size D90 of the raw material is in the range of 20 μm to 80 μm, and the pharmaceutical composition releases rapidly , stable quality; the present invention also relates to a preparation method of the pharmaceutical composition, the preparation method has a simple preparation process and is suitable for large-scale industrial 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 Patents(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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