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A kind of nano gel preparation with double sustained-release effect and preparation method thereof

A nano-gel and slow-release technology, applied in the field of pharmaceutical preparations, can solve the problems of slow-release effects, slow swelling steps, low ability to change, etc. small effect

Active Publication Date: 2021-09-07
EZHOU INST OF IND TECH HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the scheme described in the above-mentioned patent application, the components: digalactosyldiacylglycerol and other lipid substances can also form gel preparations during the mutual fusion process of polar solvents, but the lamellar liquid crystal structure viscosity of the gel High, causing its swelling step to be extremely slow, and the viscosity of its gel formulation is not changed by temperature changes. When the human body or other living organisms use injection reagents for other purposes, the required viscosity will also be different, and its ability to change is low
In terms of sustained release, digalactosyldiacylglycerol can be degraded in the body, and the galactose unit in each lipid molecule contains a polar head gene, which has a stabilizing effect on liposome preparations. After injection, it is in the blood It exists for a long time, but the sustained release effect still cannot achieve the expected effect

Method used

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  • A kind of nano gel preparation with double sustained-release effect and preparation method thereof
  • A kind of nano gel preparation with double sustained-release effect and preparation method thereof
  • A kind of nano gel preparation with double sustained-release effect and preparation method thereof

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Effect test

Embodiment 1

[0045] This embodiment provides a nanogel preparation with double sustained release, which is prepared from the following raw materials in weight percentage:

[0046] Paclitaxel 10%

[0047] Liquid crystal material 40% (phospholipid: glycerol: co-solvent = 6: 1: 0.5)

[0048] Rheology modifier 50%

[0049] The preparation method of the nanogel preparation with double sustained release is as follows:

[0050] S1 Weigh phosphatidylcholine, diolein, ethanol and 10% paclitaxel in a weight ratio of 6:1:0.5 according to 40% of the total weight and mix and stir for 30 minutes;

[0051] S2 adding a small amount of water to the precursor solution obtained in S1 for high-shear dispersion, and then performing high-pressure homogenization of the obtained mixture to obtain drug-loaded liquid crystal nanoparticles;

[0052] S3, then add 50% of the total weight of poloxamer 407 to the mixed solution of S2, stir slowly for 2 hours, and control the temperature at about 4°C, so that the syst...

Embodiment 2

[0055] This embodiment is basically the same as Embodiment 1, the difference lies in the following aspects:

[0056] A nanogel preparation with double sustained release and a preparation method thereof, prepared from the following raw materials in percentage by weight:

[0057] Paclitaxel 10%

[0058] Liquid crystal material 40% (phospholipid: glycerol: co-solvent = 10: 4: 1.5)

[0059] Rheology modifier 50%

[0060] The release efficiency of the nanogel preparation prepared in this example with double sustained release was investigated, and the encapsulation rate was 82%, and the cumulative release rate within one week was 33%.

Embodiment 3

[0062] This embodiment is basically the same as Embodiment 1, the difference lies in the following aspects:

[0063] A nanogel preparation with double sustained release and a preparation method thereof, prepared from the following raw materials in percentage by weight:

[0064] Paclitaxel 10%

[0065] Liquid crystal material 40% (phospholipid: glycerol: co-solvent = 8: 2: 1)

[0066] Rheology modifier 50%

[0067] The release efficiency of the nanogel preparation prepared in this example with double sustained release was investigated, and the encapsulation rate was 86%, and the cumulative release rate within one week was 30%.

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Abstract

The invention relates to a nano-gel preparation with dual sustained-release effects and a preparation method thereof. The nano-gel preparation is composed of 0.001-10 wt % of preloaded drug, 40-70 wt % of component A liquid crystal material, and component B rheological adjustment. It is composed of 20-50 wt% of the drug, the present invention has dual sustained-release effects, which can greatly improve the water-solubility and fat-solubility of the drug, and has a rheology modifier, which can make the gel significantly increase the viscosity of the gel as the temperature increases. , can maintain a good viscosity at skin temperature, suitable for transdermal drug delivery system; the formed gel preparation can have a longer release time in the body, which can significantly improve the absorption rate of the drug in the body and improve the bioavailability of the drug Spend.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a nanogel preparation with double sustained-release effects and a preparation method thereof. Background technique [0002] Gel is a new drug dosage form that has emerged in recent years. The research abroad is earlier and the development is faster. Domestic development started from hospital preparations, and now a variety of gels have been approved by the state, showing more advantages and effects of gels. The more commonly used routes of administration for gels are transdermal administration, oral administration, eye administration, nasal cavity administration, vaginal administration and rectal administration. Different administration routes can receive high drug concentrations. , Satisfactory effect of duration of action. The gel has the characteristics of fast absorption, high bioavailability, good biocompatibility, and uniform texture, easy to spread ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/10A61K9/51A61K47/24A61K47/14A61K45/00
CPCA61K9/06A61K9/5123A61K31/337A61K45/00A61K47/10
Inventor 罗亮黄丽萍孟凡玲
Owner EZHOU INST OF IND TECH HUAZHONG UNIV OF SCI & TECH
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