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Nilotinib composition with improved solubility

A technology of nilotinib and composition, which is applied in the directions of drug combination, organic active ingredients, medical preparations of non-active ingredients, etc., can solve problems such as poor water solubility and the like

Active Publication Date: 2021-02-02
NEOFORM BIOPHARMACEUTICAL LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the nilotinib hydrochloride used in commercially available products includes various solid forms such as anhydrate, hydrate and solvate, they all have poor water solubility

Method used

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  • Nilotinib composition with improved solubility
  • Nilotinib composition with improved solubility
  • Nilotinib composition with improved solubility

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0126] Preparation and Analysis of Embodiment 1 Nilotinib HPMCP Salt

[0127] Nilotinib: The preparation of HPMCP salt is as follows: Nilotinib free base and HPMCP are added in the mixed solvent of methanol and dichloromethane (1:1 volume ratio) to form a solution, basic Nilotinib and acidic polymer HPMCP form ionic bonds. 1.2 g of HPMCP was dissolved in a certain volume of solvent by magnetic stirring, then 0.8 g of nilotinib free base was added and allowed to dissolve. Transfer the solution to a 100mL volumetric flask, and add a certain volume of solvent to constant volume.

[0128] The resulting nilotinib HPMCP salt containing 40% nilotinib (mass ratio) was separated by spray drying with a Buchi miniature spray dryer B290 (BüCHI Labortechnik AG, Switzerland) equipped with an inert cycle B295. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter setti...

Embodiment 2

[0146] Embodiment 2 in vivo test

[0147] The prepared nilotinib HPMCP salt composition was tested in vivo in rats: young Sprague-Durer rats (generally n=4-6) fasted the day before were treated with fasted or fed state (fasting state: from 12 hours before the medication to 4 hours after the medication is not allowed to take food) test or control.

[0148] Test compositions and controls were administered orally by gavage through PE205 tubing attached to a syringe with water or 0.5% HPMC to aid wetting and prevent clumping. Rats were returned to the IVC cages and had normal access to water. Alternatively, capsules or tablets may also be administered. The test and control formulations were identical except for the presence or absence of polymer. Alternatively, the control may consist of drug only.

[0149] Blood samples were taken from the neck of the rats at 0.5, 1, 2, 6, 24 and 48 hours (sometimes 12 hours) post-injection using 1 mL disposable syringes and 20 gauge needles....

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Abstract

The present invention provides compositions of nilotinib with a salt of a polymer. According to the nilotinib composition provided by the invention, the solubility and bioavailability are improved, and the nilotinib composition can be used for treating uncontrolled cell proliferation diseases. The invention also provides a preparation method and application of the nilotinib and polymer salt composition.

Description

technical field [0001] The invention relates to the field of pharmaceutical composition preparation and application. Specifically, the present invention provides a salt composition of nilotinib and a polymer, a preparation method and application thereof, which improve solubility and bioavailability. Background technique [0002] Nilotinib, the chemical name is 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridine- 3-ylpyrimidin-2-yl)amino]benzamide having the formula [0003] [0004] Nilotinib is indicated for the treatment of Philadelphia chromosome-positive chronic myelogenous leukemia. Nilotinib belongs to the class of tyrosine kinase inhibitors that have revolutionized the way cancer is treated because it has a more defined effect on malignant cells than conventional cytotoxic chemotherapy. However, although the nilotinib hydrochloride used in commercially available products includes various solid forms such as anhydrate, hydrate and solv...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K31/506A61P35/02A61P35/00
CPCA61K47/61A61K31/506A61P35/02A61P35/00A61K9/146A61K47/38A61K9/0053A61K47/6921
Inventor 斯蒂芬·R·布林丹·史密斯安妮·齐默尔曼比亚克·斯特罗姆·拉森田芳
Owner NEOFORM BIOPHARMACEUTICAL LTD
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