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Phosphate adsorption composite nanomaterial as well as preparation and application thereof

A nano-composite and phosphorus-absorbing technology, applied in the field of nanomaterials, can solve the problems of blood phosphorus rebound rebound, patient tolerance limit, and inability to improve endogenous phosphorus increase, achieving large phosphorus adsorption, easy control of conditions, The effect of reducing the risk of cardiovascular disease

Active Publication Date: 2017-12-01
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in addition to food, the main source of blood phosphorus is the release of phosphate from bones into the blood circulation, so taking drugs cannot improve the increase in endogenous phosphorus
The usual hemodialysis means that the patient sends blood to the hemodialysis machine for 6-8 hours a day three days a week to remove small molecule toxins, and can also effectively remove blood phosphorus, but blood phosphorus often rebounds during the interval of dialysis At present, the best measure to reduce phosphorus is long-term dialysis at night, which may be limited by factors such as treatment costs and patient tolerance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of Liposome / Silamer:

[0030] (1) Mix phospholipid molecule DSPE-PEG5000-COOH (Xi’an Ruixi Biotechnology Co., Ltd.) and lecithin at a ratio of 1:20, add ethanol and stir thoroughly to obtain clear liquid 1.

[0031] (2) Pour 500ml of sterile double-distilled water into a sterilized beaker, slowly inject liquid 1 into the beaker, stir while injecting, to obtain liposomes, centrifuge, remove the supernatant, and repeat with a 100nm filter Filter 10 times to obtain homogeneous liposomes with a particle size of about 100 nm.

[0032] (3) Dissolve the purchased chemical raw material 2-propene-1-amine and the polymer carbonate of epichlorohydrin (trade name: Silam Carbonate) in sterilized double distilled water, fully stir to obtain a suspension Liquid 2.

[0033] (4) Pour suspension 2 into the prepared homogeneous liposomes, then add 150ml of N-hydroxysuccinimide (NHS) and 1-(3-dimethylaminopropyl)-3-ethane Carbodiimide hydrochloride (EDC·HCL), stirred for 2 h...

Embodiment 2

[0037] Adopt the preparation method similar to embodiment 1, difference is:

[0038] (1) The molar ratio of DSPE-PEG5000-COOH to lecithin is 1:15;

[0039] (2) the mass ratio of the polymer carbonate of nano-carrier microspheres and 2-propylene-1-amine and epichlorohydrin is 3:1;

[0040] (3) The added N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and the added 2-propen-1-amine and epoxy The mass ratio of the polymer carbonate of chloropropane is 20:20:1;

[0041] (4) The storage temperature of the final product is -10°C.

[0042] The material prepared above was used to give mice with hyperphosphatemia, and it was observed that the blood phosphorus content of the mice was controlled within 2 hours and lasted for more than 3 days.

Embodiment 3

[0044] Adopt the preparation method similar to embodiment 1, difference is:

[0045] (1) The molar ratio of DSPE-PEG5000-COOH to lecithin is 1:25;

[0046] (2) the mass ratio of the polymer carbonate of nano-carrier microspheres and 2-propylene-1-amine and epichlorohydrin is 12:1;

[0047] (3) The added N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and the added 2-propen-1-amine and epoxy The mass ratio of the polymer carbonate of chloropropane is 100:100:1;

[0048] (4) The storage temperature of the final product is -30°C.

[0049] The material prepared above was used to give mice with hyperphosphatemia, and it was observed that the blood phosphorus content of the mice was controlled within 1.5 hours and lasted for more than 3 days.

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Abstract

The invention relates to a phosphate adsorption composite nanomaterial as well as preparation and an application thereof. The composite nanomaterial comprises a nano-carrier and Sevelamer carbonate in the mass ratio being (3-12):1, wherein the nano-carrier comprises lipidosome, and Sevelamer carbonate is polymer carbonate of 2-propen-1-amine and epoxy chloropropane. The phosphate adsorption nano-composite material is used for preparing a medicine for reducing serum phosphate. Compared with the prior art, the excellent adsorption performance of polymer carbonate of 2-propen-1-amine and epoxy chloropropane is sufficiently utilized, the advantages that the long-circulation nano-carrier is non-toxic, stable and not easily captured by a phagocytic system in a body are played, and the high-biocompatibility lipidosome / Sevelamer composite nanomaterial easy to excrete is prepared. The method adopts a simple preparation process and easily controllable conditions and is thus suitable for clinic treatment of intractable hyperphosphatemia.

Description

technical field [0001] The invention relates to the technical field of nanomaterials, in particular to a nanocomposite phosphorus adsorption material and its preparation and application. Background technique [0002] Phosphorus is a constant element that plays an important role in the growth of the human body and the normal operation of the metabolic system. However, patients with chronic renal failure (CKD) suffer from hyperphosphatemia. Hyperphosphatemia refers to the fact that the serum phosphorus level exceeds the upper limit of the normal value set by the laboratory (>1.45mmol / L ). Excessive blood phosphorus can cause vascular calcification, which mainly occurs in the middle layer of the heart valve, aorta, abdominal aorta, femoral artery and other large arterial walls, causing various cardiovascular diseases, and cardiovascular diseases are the main death of CKD patients reason. Relevant studies have shown that for every 1 mg / dl increase in blood phosphorus level...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/785A61K47/24A61P3/12
CPCA61K9/1271A61K31/785
Inventor 朱玉赖青海
Owner TONGJI UNIV
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