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New dosage form of selumetinib and derivative of selumetinib and preparation method of new dosage form

A technology of selumetinib and its derivatives, which is applied in the field of pharmaceutical preparations, can solve problems such as limited application and leukopenia, and achieve the effects of reducing drug dosage, fast onset of action, and reducing drug burden

Inactive Publication Date: 2019-10-29
ZHAOQING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Existing studies have found that the main adverse reactions of oral selumetinib tablets are leukopenia, rash, diarrhea, fatigue, etc., and severe adverse reactions limit its further application

Method used

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  • New dosage form of selumetinib and derivative of selumetinib and preparation method of new dosage form
  • New dosage form of selumetinib and derivative of selumetinib and preparation method of new dosage form
  • New dosage form of selumetinib and derivative of selumetinib and preparation method of new dosage form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Preparation of tablet of the present invention (selumetinib molar ratio 70:30 in the constant release part and the sustained release part)

[0068] Raw materials: 20g of selumetinib hydrochloride, 64.8g of hydroxypropyl methylcellulose (HPMC K4M), 110g of lactose, 100g of starch, 5g of microcrystalline cellulose (1000 pieces), the preparation method is as follows:

[0069] a, get selumetinib hydrochloride 6g, add hydroxypropyl methylcellulose (HPMC K4M) and lactose, pulverize, pass through a 100-mesh sieve after being ground into fine powder;

[0070] b. Add appropriate amount of ethanol to make a film;

[0071] c. Dry in a dryer at 85°C for 20 minutes;

[0072] d. Tablet pressing with a tablet press to prepare the inner core of the slow-release part;

[0073] e, get selumetinib hydrochloride 14g, add microcrystalline cellulose to pulverize, pass 100 mesh sieves after being ground into fine powder;

[0074] f. Add appropriate amount of sterile water to make a soft ta...

Embodiment 2

[0078] Preparation of tablet of the present invention (selumetinib molar ratio 65:35 in the constant release part and the sustained release part)

[0079] Raw materials: 40g of selumetinib hydrochloride, 20g of tragacanth gum, 1.5g of flavoring agent, appropriate amount of distilled water, 80g of starch, 20g of dextrin (1000 tablets), the preparation method is as follows:

[0080] a. Take 14 g of selumetinib hydrochloride, add tragacanth gum, pulverize, grind into fine powder and pass through a 100-mesh sieve;

[0081] b. Add appropriate amount of ethanol to make a film;

[0082] c. Dry in a dryer at 85°C for 20 minutes;

[0083] d. Tablet pressing with a tablet press to prepare the inner core of the slow-release part;

[0084] e, get selumetinib hydrochloride 26g, add dextrin, grind into a fine powder and pass through a 100-mesh sieve;

[0085] f. Add appropriate amount of sterile water to make a soft tablet, and coat the outer layer of the tablet core obtained in step d t...

Embodiment 3

[0089] Preparation of tablet of the present invention (selumetinib molar ratio 75:25 in the constant release part and the sustained release part)

[0090] Raw materials: 40g of selumetinib hydrochloride, 50g of hydroxypropyl methylcellulose (HPMC K100M), 45g of methylcellulose, 80g of starch, 20g of microcrystalline cellulose (1000 pieces), the preparation method is as follows:

[0091] a, get selumetinib hydrochloride 10g, add hydroxypropyl methylcellulose (HPMC K4M) and methylcellulose and starch, pulverize, cross 100 mesh sieves after being ground into fine powder;

[0092] b. Add appropriate amount of ethanol to make a film;

[0093] c. Dry in a dryer at 85°C for 20 minutes;

[0094] d. Tablet pressing with a tablet press to prepare the inner core of the slow-release part;

[0095] e, get 30g of selumetinib hydrochloride, add microcrystalline cellulose to pulverize, pass through a 100-mesh sieve after being ground into fine powder;

[0096] f. Add appropriate amount of ...

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Abstract

The invention relates to a new dosage form of selumetinib and a derivative of the selumetinib, and belongs to the field of medicine. According to the new dosage form of the selumetinib and the derivative of the selumetinib, the adverse reactions of leucopenia, rash, diarrhea and fatigue after use of the selumetinib are reduced. The new dosage form is a preparation prepared from an ordinary releasepart containing the selumetinib and the derivative of the selumetinib as active ingredients and a slow-release part containing the selumetinib and the derivative of the selumetinib as active ingredients; and the molar ratio of the selumetinib and the derivative of the selumetinib contained by the ordinary release part to the selumetinib and the derivative of the selumetinib contained by the slow-release part is (10-90) to (10-90). The invention further provides a preparation method of the pharmaceutical composition. A clinical test shows that the incidence rate of adverse reactions of the newdosage form is obviously lower than that of conventional tablets of selumetinib, and a safe new dosage form is provided for the clinical application of the selumetinib and the derivative of the selumetinib.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and specifically discloses a new dosage form and preparation method of selumetinib and its derivatives. Background technique [0002] Selumetinib, the chemical name is 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzene And imidazole-6-carboxamide, developed by British AstraZeneca company. [0003] Selumetinib is a mitogen extracellular kinase (MEK1 / 2) inhibitor, which can significantly inhibit ERK1 / 2 by inhibiting extracellular signal-regulated kinase (ERK / 2) and activating the cysteine ​​protease (caspase) pathway of phosphorylation. At present, it is mainly used in clinical research of cancers such as cholangiocarcinoma, colorectal cancer, and non-small cell lung cancer (NSCLC). A double-blind, randomized study was conducted on 87 patients with mutant NSCLC. Compared with the combination group of selumetinib and docetaxel (DOC) and the combination gr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/4184A61P35/00
CPCA61K9/2059A61K9/2095A61K31/4184A61P35/00
Inventor 曾鹏高佳酮林涛峰林婉周丽
Owner ZHAOQING UNIV
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