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Preparing method of corrosion type silicon dioxide xerogel drug sustained-release material

A technology of silicon dioxide and sustained-release materials, which is applied in pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve the problems of low protein loading rate, waste of protein drugs, and complicated preparation process, and achieves shortening preparation time, delivery time, etc. The effect of reducing the link structure and controlling the degree of cross-linking

Active Publication Date: 2013-12-04
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation process of this method is cumbersome, the protein loading rate is low (only 20-40%), and the protein drug is seriously wasted.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Put 1 g of methyl orthosilicate, 0.4 g of 3-(triethoxysilyl) propyl succinic anhydride, 0.2 ml of hydrochloric acid, and 1 ml of deionized water into a flat-bottomed glass bottle, at room temperature (about 25 o C) Under magnetic stirring for 30 minutes, carry out co-hydrolysis and co-polycondensation to form a homogeneous sol, add bovine serum albumin 25 mg (Note: the amount of bovine serum albumin added is methyl orthosilicate and 3-(triethoxysilane) Propyl succinic anhydride both add 1.8% of the total weight), after mixing evenly (that is, after completely dissolving), drop into 0.1ml 1N sodium hydroxide solution drop by drop, stir for 15 minutes to make the mixed solution rapidly cross-link to form a network structure, place at 40 o C is dried in a vacuum oven to a constant weight to obtain a silica xerogel loaded with bovine serum albumin, i.e. 0.70 g of an erosion type silica xerogel drug sustained-release material. 3.6%.

[0029] Grind and sieve the silica xero...

Embodiment 2

[0032] Tetraethyl orthosilicate 1g, 3-(triethoxysilyl)propyl succinic anhydride 0.25g, hydrochloric acid 0.3ml, deionized water 1ml, magnetically stirred at room temperature for 1 hour, carried out co-hydrolysis and co-polycondensation to form a homogeneous sol , add 25 mg of bovine serum albumin (note: the amount of bovine serum albumin added is 2.0% of the total weight of ethyl orthosilicate and 3-(triethoxysilyl) propyl succinic anhydride), mix well and gradually Add 0.15ml 1N sodium hydroxide solution drop by drop, stir for 15 minutes to make the sol quickly cross-link the network structure, place at 40 o C dried in a vacuum oven to constant weight to obtain 0.58 g of eroded silica xerogel drug sustained-release material, at which time the drug loading accounted for 4.3% of the total mass of the xerogel.

[0033] After adding the alkali catalyst, the shape and size of the product silica xerogel can be flexibly adjusted. The silica xerogel prepared above can be ground and s...

Embodiment 3

[0035] Tetraethyl orthosilicate 1g, 3-(triethoxysilyl) propyl succinic anhydride 0.10g, hydrochloric acid 0.5ml, deionized water 1ml, magnetically stirred at room temperature for 30 minutes, carried out co-hydrolysis and co-polycondensation to form a homogeneous sol, adding Bovine serum albumin 30 mg (note: the amount of bovine serum albumin added is 2.7% of the total weight of tetraethyl orthosilicate and 3-(triethoxysilyl) propyl succinic anhydride), mix well and drop by drop Add 0.15ml of 1N potassium hydroxide solution, stir for 10 minutes to make the sol quickly form a cross-linked network structure, place at 40 o C dried in a vacuum oven to constant weight to obtain 0.49 g of erodible silica xerogel drug sustained-release material, at which time the drug loading accounted for 6.1% of the total mass of the xerogel.

[0036] Grind and sieve the silica xerogel prepared above into particles of 40-70 μm, accurately weigh 25 mg and place it in 10 ml of the tris buffer describe...

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PUM

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Abstract

The invention discloses a preparing method of a corrosion type silicon dioxide xerogel drug sustained-release material. The preparing method comprises the following steps: mixing and stirring 50-99 percent by weight of organo-siloxanes of which silicon atoms are all connected with alkoxy, 1-50 percent by weight of organo-siloxanes of which alkoxy is partly replaced with alkyl branches difficult to hydrolyze, a certain amount of solvent, and acid catalysts for 10-120 minutes at the temperature of 20-60 DEG C, performing the cohydrolysis and the copolycondensation, adding drug of which the weight is 0.1-50% of the total weight of the two kinds of organo-siloxanes after the sufficient reaction, adding the base catalysts to enable hydrolysates be to quickly crosslinked after the complete dissolution, stirring for 1-30 minutes, and drying to obtain the drug sustained-release material after the product is solidified. The preparing method can calculate and control the drug load accurately, and the shape and the size of the drug sustained-release material can be adjusted flexibly according to the drug releasing requirement. The preparing method is simple in process, good in biocompatibility, and non-toxic to the human body, and has a wide application prospect in controllable release and clinical trials of drug suitable for sustained-release application.

Description

technical field [0001] The invention relates to a preparation method of an erosion-type silica xerogel drug slow-release material, and belongs to the technical field of drug slow-release material preparation. Background technique [0002] As a widely used drug release carrier, the silica xerogel (xerogel for short) prepared by the room temperature sol-gel method has good biocompatibility, good chemical stability and dimensional stability, non-toxicity, and reactivity. The advantages of mild conditions, simple and easy-to-control process, and flexible and adjustable matrix microstructure have attracted extensive attention from scholars. Due to its mild reaction conditions, there is basically no effect on the activity of drug molecules during the preparation and loading of xerogels, and it is very suitable for the release of unstable drugs such as peptides, proteins and DNA in vivo and in vitro. [0003] The release of drugs in xerogels is generally controlled by regulating t...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/04
Inventor 陈蓉郭少云张聪
Owner SICHUAN UNIV
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