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Renvatinib composition

A technology of lenvatinib and its composition, which is applied in the field of pharmaceutical preparations, can solve problems such as poor dissolution rate, and achieve the effects of simplifying production steps, increasing bioavailability, and avoiding solubility decline

Active Publication Date: 2022-04-12
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Through a lot of research, we found that the combination of acidic and alkaline regulators greatly improved the phenomenon of gelation of lenvatinib mesylate in contact with water, and also solved its dissolution at a pH above 6.8. The problem of poor dissolution in the environment

Method used

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  • Renvatinib composition
  • Renvatinib composition
  • Renvatinib composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Embodiment 1: the selection of different acid / alkaline regulator types

[0069] Using the following prescription, using non-micronized raw materials (particle size distribution: D10 = 2.45 μm, D50 = 23.4 μm, D90 = 186 μm), according to the preparation method of Comparative Example 1 (additional addition of alkaline modifier) ​​to prepare different Capsule preparations, and 12 capsules of different prescriptions were taken to test the dissolution.

[0070] Table 5 Prescribing Information-1

[0071]

[0072]

[0073] Table 6 Prescribing Information-2

[0074]

[0075] The dissolution results of lenvatinib mesylate capsules prepared with different acidic and alkaline regulators in the dissolution medium of pH 6.8 were determined.

[0076] Table 7 Dissolution Results (n=12)

[0077]

[0078]

[0079] According to the stripping result of table 7, it can be seen that, with respect to the stripping of the preparation prepared by the non-micronized raw materia...

Embodiment 2

[0083] Embodiment 2: the impact of different ratios of acidic regulator and basic regulator on dissolution

[0084] Adopt the following prescription, use non-micronized raw materials (particle size distribution: D10=2.45 μm, D50=23.4 μm, D90=186 μm), and obtain different capsules according to the preparation method of Comparative Example 1 (additional addition of alkaline regulator) Preparations, and 12 capsules of different prescriptions were taken to test the dissolution.

[0085] Table 8 Prescribing Information

[0086]

[0087]

[0088] The dissolution results of lenvatinib mesylate capsules prepared by using different proportions of acidic and alkaline regulators in the dissolution medium of pH 6.8 were determined.

[0089] Table 9 Dissolution Results (n=12)

[0090] prescription time / min 10 15 20 30 45 60 90 120 2-1 mean% 2 4 8 15 26 32 39 42 2-2 mean% 20 42 53 69 80 83 83 84 2-3 mean% 31 57 68 78 82 88 ...

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Abstract

The invention provides a revatinib composition. The problem that revatinib is gelled when encountering water is solved by adding an acidic regulator and an alkaline regulator. The pH value of the dissolution system is reduced by adding the acidic regulator, the problem that the dissolvability of the revatinib mesylate which is dependent on the pH value is reduced is further avoided, and the bioavailability of the revatinib is increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a lenvatinib composition. Background technique [0002] Lenvatinib is a tyrosine kinase (RTK) receptor inhibitor that can inhibit the kinase activity of the vascular endothelial growth factor (VEGF) receptor, and can also inhibit other pathways related to angiogenesis and tumorigenesis RTK. [0003] On the one hand, lenvatinib mesylate encounters severe gelation in water or an aqueous solution, which seriously affects the preparation and quality of the preparation. CN101001629A discloses a lenvatinib pharmaceutical composition, which uses silicate as a gelation preventing agent. However, the amount of silicic acid compounds used in the composition is large, and the density of such compounds is extremely small, and they are easy to fly during production, which will cause serious damage to the respiratory system of operators. At the same time, during the mixing process...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/47A61K47/38A61K47/26A61K47/12A61K47/02A61P35/00
Inventor 任军乐贾广辉吕高星安立鑫孙晓伟尹璐张乐文董丹丹
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD