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4-(4-(3-trifluoromethyl)benzamido-phenoxy)-2-(methyl-ammonia-formoxyl)pyridine NANO suspension as well as preparation method and application thereof

A benzamidophenoxy and methylcarbamoyl technology, applied in the field of medicine, can solve the problems of difficulty in forming highly dispersed particle groups and poor water solubility, and achieve high product uniformity, less excipients, and high stability Effect

Active Publication Date: 2012-11-14
SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0013] The inventor tried to solve the technical problem of poor water solubility of SKLB 610 with a nano-suspension, but in the trial production process, the particle size of the obtained suspension was usually at the micron level, and the smallest was around 1-2 microns, and it was difficult to form a particle size The highly dispersed particle group below 1000nm, in order to solve the problem of particle size, the inventor made many adjustments to the preparation process of nano-suspension, auxiliary materials and other parameters, and finally formed a nano-mixture with a particle size range of 150-800nm Suspension, the particle size range can even be controlled within a small range of 150-300nm

Method used

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  • 4-(4-(3-trifluoromethyl)benzamido-phenoxy)-2-(methyl-ammonia-formoxyl)pyridine NANO suspension as well as preparation method and application thereof
  • 4-(4-(3-trifluoromethyl)benzamido-phenoxy)-2-(methyl-ammonia-formoxyl)pyridine NANO suspension as well as preparation method and application thereof
  • 4-(4-(3-trifluoromethyl)benzamido-phenoxy)-2-(methyl-ammonia-formoxyl)pyridine NANO suspension as well as preparation method and application thereof

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preparation example Construction

[0070] The following is the screening process of the preparation process of the nanosuspension of the present invention.

[0071] 1. Screening of wet grinding stabilizers

[0072] 1. The inventor investigated the situation when the following several auxiliary materials were used as stabilizers for nanosuspensions alone: ​​when the dosage of the drug SKLB 610 was 200 mg, the rotating speed was 45 Hz, and the time was 2 hours, the auxiliary materials were investigated as follows, and the results are shown in Table 1.

[0073] Table 1

[0074]

[0075] It can be seen from Table 1 that when a stabilizer is used alone, the particle size range of the obtained nanosuspension particles is 500-1200nm, which belongs to the situation with a large particle size range, but the particles of PVP, SDS, F68, and EL among them The diameter range can reach a relatively small range of 500-800nm.

[0076] 2. In order to further reduce the particle size range, the inventors have made various a...

Embodiment 1

[0122] First weigh 0.2gPVP and dissolve 0.04gSDS in 40ml of purified water to obtain a solution; ) pyridine is dispersed in the above-mentioned solution to prepare a common suspension; the gained common suspension is added to a ball mill jar, and 70g of zirconia particles with a diameter of 0.2mm are added; after the ball mill jar is sealed, put it into a ball mill, Set the rotation speed to 45Hz and grind for 2 hours; then use a glass sand funnel to filter out the zirconia particles to obtain 4-(4-(3-trifluoromethyl)benzamidophenoxy)-2-(methyl Carbamoyl) pyridine nanosuspension. The measured particle diameter is: 202nm, and the PDI is 0.201.

Embodiment 2

[0124] First weigh 0.2g of PVP and dissolve 0.02g of SDS in 40ml of purified water to obtain a solution; ) pyridine is dispersed in the above-mentioned solution to prepare a common suspension; the gained common suspension is added to a ball mill jar, and 70g of zirconia particles with a diameter of 0.2mm are added; after the ball mill jar is sealed, put it into a ball mill, Set the rotation speed to 35Hz, grind for 12 hours; then use a glass sand funnel to filter out the zirconia particles to obtain 4-(4-(3-trifluoromethyl)benzamidophenoxy)-2-(methyl Carbamoyl) pyridine nanosuspension; its particle diameter is measured as: 198nm, and its PDI is 0.188. Then add 2% mannitol, divide the sample into 2ml vials, pre-freeze at -80°C for 12 hours, and then freeze-dry in a freeze dryer for 24 hours to obtain a loose freeze-dried powder, then add purified water Redissolved, the particle size increased within 10%.

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Abstract

The invention belongs to the field of medicines, and particularly relates to 4-(4-(3-trifluoromethyl)benzamido-phenoxy)-2-(methyl-ammonia-formoxyl)pyridine (SKLB610 for short) nano suspension as well as a preparation method and an application thereof. The SKLB610 is low in water solubility, so that the nano suspension with the particle size of 150 to 800 nm is supplied. Specifically, the nano suspension is prepared by adopting wet grinding, used as an intermediate product and used for preparing an oral preparation or an injection preparation. The nano suspension mainly comprises 1 to 10 parts of SKLB610 and 1 to 10 parts of stabilizing agent. The preparation method comprises the following steps of: (A) dissolving the stabilizing agent into water, dispersing the SKLB610 into the solution, and obtaining a common suspension; and (B) adding the common suspension, and preparing the nano suspension by adopting wet grinding. The particle size of the nano suspension can be effectively and intensively controlled within a range of 150 to 300 nm; and the nano suspension is high in uniformity and small in particle size.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to 4-(4-(3-trifluoromethyl)benzamidophenoxy)-2-(methylcarbamoyl)pyridine nanosuspension and its preparation method and application . Background technique [0002] At present, more than 40% of the world's new compound entities (NCEs) and candidate drugs are poorly water-soluble drugs, and some are even oil-water-insoluble drugs. [0003] Chinese patent application CN101362718A, the application number is 200810304730.5, which discloses 4-(4-benzamidophenoxy)-2-(methylcarbamoyl)pyridine derivatives shown in formula I and their preparation methods and uses : [0004] [0005] Among them, R 1 is hydrogen, halo, trifluoromethyl, nitro, alkoxy, dimethoxy or amino; [0006] R 2 is hydrogen, halo, trifluoromethyl, nitro, alkoxy, dimethoxy or amino; [0007] R 3 is hydrogen, halo, trifluoromethyl, nitro, alkoxy, dimethoxy or amino. [0008] After further screening, the inventors found that ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/44A61P35/00
Inventor 余洛汀罗珣黄云窗魏于全
Owner SICHUAN UNIV
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