Unlock instant, AI-driven research and patent intelligence for your innovation.

Porous silicon dioxide medicinal accessory for solubilizing itraconazole as well as preparation and applications of porous silicon dioxide medicinal accessory

A technology of porous silica and itraconazole, which is applied in the direction of drug delivery, drug combination, and medical preparations of non-active ingredients, etc., can solve problems such as the treatment of dysentery mycosis, and achieve the promotion of dissolution onset and reduction of drug side effects , reduce the effect of intestinal irritation

Inactive Publication Date: 2017-06-23
QUFU NORMAL UNIV
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Itraconazole is a high-efficiency antifungal agent that has a good inhibitory effect on the above two fungi, but it is difficult to apply to the treatment of gastric mycosis because of its low water solubility

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Porous silicon dioxide medicinal accessory for solubilizing itraconazole as well as preparation and applications of porous silicon dioxide medicinal accessory

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Such as figure 1 As shown, add 30mL of toluene, 0.11g of aminopropyltriethoxysilane, and 6g of commercial drug flow agent silicon oxide in the three-necked flask successively, and the specific surface area of ​​the silicon oxide is 410m 2 / g, pore size 3-15nm, reflux at 80°C for 24h. Then the obtained product was subjected to suction filtration, washed three times with 20 mL of ethanol respectively, and the product obtained by suction filtration was dried in an oven at 60° C. for 12 hours to obtain the aminopropyl-modified silicon oxide drug excipient of this example.

[0036] Dissolve 1 g of itraconazole into a beaker of 30 mL of dichloromethane, add 1 g of aminopropyl-modified silicon oxide, and stir at room temperature for 0.5 hours. The mixed solution was transferred to a rotary evaporator, set the temperature at 30°C, and distilled under reduced pressure until the dichloromethane volatilized completely. Then put the product in an oven at 60° C. and dry it for 10 ...

Embodiment 2

[0040] Such as figure 1 As shown, add 30mL of methanol, 0.28g of methyltrimethoxysilane, and 6g of mesoporous silica to the three-necked flask in sequence. The mesoporous silica is SBA-15 with a specific surface area of ​​740m 2 / g, pore size 6-8nm, reflux at 70°C for 24h. Then the obtained product was subjected to suction filtration, washed three times with 20 mL of ethanol, and the product obtained by suction filtration was dried in an oven at 60° C. for 12 hours. After the drying was completed, the methyl-modified SBA-15 silicon oxide pharmaceutical excipient of this example was obtained.

[0041] Dissolve 1 g of itraconazole into a beaker of 30 mL of dichloromethane, then add 2 g of aminopropyl-modified silicon oxide, and stir at room temperature for 0.5 hours. The mixed solution was transferred to a rotary evaporator, set the temperature at 30°C, and distilled under reduced pressure until the dichloromethane volatilized completely. Then place the product in an oven at 6...

Embodiment 3

[0045] Add 40mL of toluene, 0.16g of hexamethyldisilazane, and 6g of mesoporous silica to the three-necked flask in sequence. The mesoporous silica is MCM-41 with a specific surface area of ​​820m 2 / g, pore size 3-4nm, reflux at 80°C for 24h. Then the obtained product was subjected to suction filtration, washed three times with 20 mL of ethanol, and the product obtained by suction filtration was dried in an oven at 60° C. for 12 hours. After the drying was completed, the methyl-modified MCM-41 silicon oxide drug excipient of this example was obtained.

[0046] Dissolve 1 g of itraconazole into a beaker of 30 mL of dichloromethane, then add 0.5 g of methyl-modified MCM-41 silicon oxide, and stir at room temperature for 0.5 hours. The mixed solution was transferred to a rotary evaporator, set the temperature at 30°C, and distilled under reduced pressure until the dichloromethane volatilized completely. Then place the product in an oven at 60° C. and dry it for 10 minutes to ob...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Specific surface areaaaaaaaaaaa
Apertureaaaaaaaaaa
Specific surface areaaaaaaaaaaa
Login to View More

Abstract

The invention discloses a porous silicon dioxide medicinal accessory for solubilizing itraconazole as well as preparation and applications of the porous silicon dioxide medicinal accessory, relating to the fields of medicinal accessories. Silane groups are grafted to the surface and / or in holes of silicon dioxide, wherein the silane groups are -(SiO)n-Si-[(CH2)j-NH2]m or -(SiO)n-Si-[(CH2)j-CH3]m, (m+n)=4 and (m*n) is greater than 0, and j is a value selected from (0-5). For the porous silicon dioxide medicinal accessory, by adjusting the hydrophobicity of silicon dioxide, itraconazole is effectively loaded and the controlled release is also realized.

Description

technical field [0001] The invention relates to the field of pharmaceutical excipients, in particular to a porous silicon oxide pharmaceutical excipient for solubilizing itraconazole and its preparation and application. Background technique [0002] Itraconazole: 4-[4-[4-[4-[[cis-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-yl Methyl)-1,3-dioxolane-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-[1-methyl Propyl]-3H-1,2,4-Triazol-3-one; a triazole antifungal agent indicated for the treatment of systemic fungal infections including aspergillosis, candidiasis, cryptococcal meningitis, tissue Phytoplasmosis, paracoccidioidomycosis, chromomycosis, odontosis, gynecologic vulvovaginal candidiasis, dermatological / ophthalmic tinea versicolor, dermatophytosis, fungal keratitis and oral candidiasis and caused by Mycoses caused by dermatophytes or yeasts are disclosed in US-4,267,179. [0003] Itraconazole has a strong lipophilicity, that is, a hydrophobic substance, which ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/24A61K31/496A61P31/10A61P1/00
CPCA61K9/0002A61K31/496A61K47/24
Inventor 岳明波郇义红李言信苗杰颜秉雪
Owner QUFU NORMAL UNIV