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A preparation method of erosion-type silica xerogel drug sustained-release material

A technology of silicon dioxide and sustained-release materials, applied in pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve the problems of low protein loading rate, waste of protein drugs, complicated preparation process, etc., and achieve flexible and acceptable shape and size. control, increase steric hindrance, and control the degree of cross-linking

Active Publication Date: 2016-02-10
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this method preparation process is loaded down with trivial details, and protein loading rate is low (only 20-40%), and protein drug waste is serious

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Put 1g of methyl orthosilicate, 0.4g of 3-(triethoxysilyl)propyl succinic anhydride, 0.2ml of hydrochloric acid, and 1ml of deionized water into a flat-bottomed glass bottle, and magnetically stir at room temperature (about 25℃) for 30 Minutes, carry out co-hydrolysis and co-condensation to form a uniform sol, add 25mg bovine serum albumin (Note: the addition amount of bovine serum albumin is both methyl orthosilicate and 3-(triethoxysilyl)propyl succinic anhydride 1.8% of the total weight), after mixing evenly (that is, after completely dissolving) drop by drop 0.1ml of 1N sodium hydroxide solution, stirring for 15 minutes to quickly crosslink the mixed solution to form a network structure, and place it in a vacuum oven at 40℃ to dry until The silica xerogel loaded with bovine serum albumin was obtained at constant weight, that is, 0.70 g of erodible silica xerogel drug sustained-release material, and the drug loading accounted for 3.6% of the total mass of the xerogel. ...

Embodiment 2

[0030] 1g of ethyl orthosilicate, 0.25g of 3-(triethoxysilyl)propyl succinic anhydride, 0.3ml of hydrochloric acid, 1ml of deionized water, magnetically stirred at room temperature for 1 hour, co-hydrolysis and co-polycondensation to form a homogeneous sol , Add 25mg bovine serum albumin (note: the addition amount of bovine serum albumin is 2.0% of the total weight of ethyl orthosilicate and 3-(triethoxysilyl)propyl succinic anhydride), mix well and drop by drop Drop 0.15ml of 1N sodium hydroxide solution, stir for 15 minutes to make the sol quickly cross the network structure, and place it in a vacuum oven at 40°C to dry to a constant weight to obtain 0.58g of a corrosion-resistant silica xerogel drug sustained-release material. The drug loading accounted for 4.3% of the total mass of the dry gel.

[0031] After the alkali catalyst is added, the shape and size of the product silica xerogel can be adjusted flexibly. The silica xerogel prepared above can be ground and sieved into ...

Embodiment 3

[0033] 1g of ethyl orthosilicate, 0.10g of 3-(triethoxysilyl) propyl succinic anhydride, 0.5ml of hydrochloric acid, 1ml of deionized water, magnetic stirring at room temperature for 30 minutes, co-hydrolysis and co-polycondensation to form a homogeneous sol, add Bovine serum albumin 30mg (Note: the addition amount of bovine serum albumin is 2.7% of the total weight of both ethyl orthosilicate and 3-(triethoxysilyl) propyl succinic anhydride), mix well and then drop by drop 0.15ml of 1N potassium hydroxide solution, stirring for 10 minutes to make the sol rapidly form a cross-linked network structure, and place it in a vacuum oven at 40℃ to dry to a constant weight to obtain 0.49g of a corrosion-resistant silica xerogel drug sustained release material. The load accounted for 6.1% of the total mass of the dry gel.

[0034] The silica xerogel prepared above was ground and sieved into particles of 40-70 μm, 25 mg was accurately weighed and placed in 10 ml of the tris buffer describe...

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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 sustained-release material, and belongs to the technical field of the preparation of a drug sustained-release material. Background technique [0002] As a widely used drug delivery carrier, 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 reaction The advantages of mild conditions, simple process and easy control, and flexible and adjustable matrix microstructure have attracted wide attention from scholars. Due to its mild reaction conditions, the dry gel preparation and drug loading process basically has no effect on the activity of drug molecules, and is very suitable for the release of peptides, proteins, DNA and other unstable drugs in vivo and in vitro. [0003] The release of drugs in xerogels is generally controlled by the regulation of its...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/04
Inventor 陈蓉郭少云张聪
Owner SICHUAN UNIV
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