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Clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and salt thereof, preparation method thereof, and application thereof

A technology of benzamide and pyridine carboxamide, which is applied in the field of medicine, can solve the problems of low solubility and achieve the effects of promoting absorption, improving drug solubility, and improving bioavailability

Active Publication Date: 2012-10-17
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to solve the technical problems of its low solubility and bioavailability, the present invention seeks different preparation means, and finds that SKLB 610 and SKLB 710 are used as active components respectively, and carrier material β-cyclodextrin (hereinafter abbreviated as β-CYD ), hydroxypropyl-β-cyclodextrin (hereinafter abbreviated as HP-β-CYD) or sulfobutyl ether-β-cyclodextrin (SBE-β-CYD); using three carrier materials Mixtures of the three, such as mixing two or three to form clathrates, can effectively improve bioavailability or increase solubility in water

Method used

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  • Clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and salt thereof, preparation method thereof, and application thereof
  • Clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and salt thereof, preparation method thereof, and application thereof
  • Clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and salt thereof, preparation method thereof, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Take 0.5g of SKLB 710 passed through an 80-mesh sieve, dissolve it in 50ml of ethanol, put it in a mortar with 1g of HP-β-CYD dispersed in water, grind it at a speed of 200rpm, and grind it for 30 minutes; dry it under reduced pressure for 4 hours, pass through a 120-mesh sieve, Instantly. The inclusion rate is 76.5%, and the in vitro dissolution curve is shown in figure 1 . Add lactose, magnesium stearate, sodium carboxymethyl starch, and talcum powder to directly compress into tablets to obtain oral tablets.

Embodiment 2

[0041] Take 1 g of SKLB610 passed through an 80-mesh sieve, dissolve it in 50 ml of ethanol, place it in a mortar with 1 g of β-CYD dispersed in water, and grind it at a speed of 200 rpm for 30 minutes. Pass through a 120-mesh sieve. The inclusion rate is 75.4%, and the in vitro dissolution curve is shown in figure 2 . Add lactose or pregelatinized starch, and directly fill capsules.

Embodiment 3

[0043] Add 0.5g of β-CYD and 0.5g of HP-β-CYD into distilled water, stir to dissolve, put them together with 10mg of SKLB 610 in a mortar, and grind at a speed of 100-600rpm for a grinding time of 20-60min. Freeze-drying, the freeze-drying time is 24h. Grind again and pass through a 200-mesh sieve to obtain the clathrate. The inclusion rate is 89%. The clathrate can be directly dissolved in water, which can increase the solubility of SKLB610 raw material drug in water (0.00098mg / ml) by nearly 1000 times. Add mannitol to adjust isotonicity, and then use a 0.22μm microporous membrane to sterilize, pack, Freeze-dried to obtain freeze-dried powder for injection.

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Abstract

The invention belongs to the field of medicine, and specifically relates to clathrates of N-methyl-4-(4-(3-trifluoromethyl)benzoylamino)phenoxyl)nicotinamide and a 4-methylbenzenesulfonate salt thereof, pharmaceutical compositions thereof, a preparation method thereof, and applications thereof. According to the invention, different preparation means are explored for resolving the technical problems of low solubility and low bioavailability of SKLB 610 and SKLB 710. As a result, the bioavailability or the water-solubility of SKLB 610 and SKLB 710 can be effectively improved by the following steps: adopting SKLB 610 and SKLB 710 as an active component; and adding a carrier material such as beta-cyclodextrin (beta-CYD), hydroxypropyl-beta-cyclodextrin (HP-beta-CYD), sulfobutyl ether-beta-cyclodextrin (SBE-beta-CYD), a mixture of two selected from the above, or a mixture of the three is added to the active component, such that a clathrate is prepared.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a package of N-methyl-4-(4-(3-trifluoromethyl)benzamido)phenoxy)pyridinecarboxamide and 4-methylbenzenesulfonate compound and its pharmaceutical composition, preparation method and application. Background technique [0002] Malignant tumors have become the second leading cause of human death, seriously threatening human health. In my country, according to the latest statistics, tumors have become the number one cause of death for our people. According to the latest epidemiological survey data, there are more than 3 million cancer patients in my country, and about 1.3 million patients die of malignant tumors every year. Every year, there are 1.6 to 2 million new cases of malignant tumors, and they are increasing at a rate of 3%, which poses a huge threat to the life and health of our people and brings huge pressure to society and families. To a certain extent, it restricts the sustainable ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/08A61K9/19A61K31/44A61P35/00
Inventor 宋相容余洛汀赵瀛兰杨胜勇魏于全
Owner SICHUAN UNIV
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