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Entecavir-loaded mesoporous silica nanoparticle and preparation method thereof

A mesoporous silicon dioxide and silicon dioxide technology, applied in the field of medicine, can solve the problems of no intravenous controlled injection preparation method, can not be used for patients with emergency patients and cannot be administered orally, etc., to improve bioavailability, Improve the effect of drug loading

Active Publication Date: 2016-04-06
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the pharmaceutical preparations of entecavir marketed at home and abroad are all oral dosage forms, which cannot be used for acute patients and patients who cannot be administered orally, and there is no intravenous slow control injection and related preparation methods

Method used

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  • Entecavir-loaded mesoporous silica nanoparticle and preparation method thereof
  • Entecavir-loaded mesoporous silica nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1 mesoporous silica nanoparticles (MSNs)

[0024] Take 1.0g of cetyltrimethylammonium bromide, 0.28g of sodium hydroxide, add 480ml of distilled water, stir and dissolve in a water bath at 80°C, and after stabilizing for 0.5h, slowly add 2mL of ethyl orthosilicate dropwise, continue to stir for 2h, and then naturally cool down. Collect nanoparticles by centrifugation, add a mixed solution of methanol and concentrated hydrochloric acid (3ml, 37.4%), heat at reflux for 24h, collect nanoparticles by centrifugation, wash with water and methanol 7 times, and dry in vacuo to obtain MSNs.

[0025] The average particle size of MSNs measured by high-resolution electron microscope is 100nm, and the average pore size is 3.52nm.

Embodiment 2

[0027] Take entecavir 0.5g, add the mixed solution 4ml of DMSO and dichloromethane (DMSO0.8ml, dichloromethane 3.2ml) and make it dissolve, add the MSNs1.0g that embodiment 1 makes, ultrasonic 15min, disperse evenly, then in Stir at 25° C. for 24 h at a stirring speed of 100 rpm. The above solution was centrifuged at 12,000 rpm for 10 min, the supernatant was discarded, and the precipitate was retained. The precipitate was placed in a vacuum drying oven and dried in vacuum for 24 hours to obtain entecavir-loaded mesoporous silica nanoparticle powder.

[0028] According to the method of Example 4, the drug loading amount is 25.11%.

Embodiment 3

[0030] Weigh 0.5 g of Entecavir, add 4 ml of mixed solution of DMSO and ethanol (DMSO 1 ml, ethanol 3 ml) to dissolve it, add 1.0 g of MSNs prepared in Example 1, sonicate for 20 min, disperse evenly, then stir at 25 ° C for 20 h, stir The speed is 150rpm. The above solution was centrifuged at 12,000 rpm for 10 min, the supernatant was discarded, and the precipitate was retained. The precipitate was placed in a vacuum drying oven and dried in vacuum for 24 hours to obtain entecavir-loaded mesoporous silica nanoparticle powder.

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Abstract

The invention belongs to the technical field of medicines, and relates to an entecavir-loaded mesoporous silica nanoparticle and a preparation method thereof. The entecavir-loaded mesoporous silica nanoparticle provided by the invention contains entecavir and mesoporous silica nanoparticle. According to the entecavir-loaded mesoporous silica nanoparticle provided by the invention, the bioavailability of the entecavir is improved; the entecavir-loaded mesoporous silica nanoparticle can be slowly released in a body; and according to the preparation method provided by the invention, the drug loading capacity is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an entecavir-loaded mesoporous silicon dioxide nanoparticle and a preparation method thereof. Background technique [0002] Entecavir, chemical name: 2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2methylenecyclopentane] -6H-purin-6-one, its structural formula is as follows: [0003] [0004] US Patent US5206244 discloses entecavir and its application for treating hepatitis B virus; WO9809964 discloses a new entecavir synthesis method; WO0164421 discloses low-dose entecavir solid preparations. [0005] Entecavir is a highly effective antiviral agent developed by Bristol-Myers Squibb in the 1990s and has a strong anti-HBV effect. It can become active triphosphate through phosphorylation, and the half-life of triphosphate in the cell is 15h. By competing with the natural substrate of HBV polymerase, deoxyguanosine triphosphate, entecavir triphosphate can inhibit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/522A61K47/04A61P1/16A61P31/20
CPCA61K9/0002A61K9/0019A61K9/143A61K31/522
Inventor 王善春张喜全顾红梅张雪王祥建张来芳耿文军
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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