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A kind of preparation method of 1-deoxynojirimycin sustained-release preparation using mulberry leaf polysaccharide as carrier

A technology of deoxynojirimycin and mulberry leaf polysaccharide, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of short half-life and achieve the effect of improving the half-life

Active Publication Date: 2021-07-23
TARIM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the half-life of 1-DNJ in the body is very short, only about 2h

Method used

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  • A kind of preparation method of 1-deoxynojirimycin sustained-release preparation using mulberry leaf polysaccharide as carrier
  • A kind of preparation method of 1-deoxynojirimycin sustained-release preparation using mulberry leaf polysaccharide as carrier
  • A kind of preparation method of 1-deoxynojirimycin sustained-release preparation using mulberry leaf polysaccharide as carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Synthesis of Pranik Pluronic-polyethyleneimine PEI

[0027] In this example, the prolonged waddose uses the preparation of the members of this topical group (the optimization of hydraulic hypoglycemic extraction and its hypoglycemic activity; Han Jiazhi, Wang Lijun, Jia Qinghua, Wang Zhunkun, Ma Ling, Yang Ling; "China Brewing ", 2017, Vol. 86, No. 8, 139-143, page 139-143, the specific preparation method is as follows: The drug saulin leaves are pulverized after the dryness, and 60 mesh sieve the mulberry pulp, with a hot water of 90 ° C to carry out the mulberry pulp The impregnation extraction, the extraction time of 3 h, the liquid material is less than 25: 1 g / ml, centrifugally, 5000 r / min, centrifugal time is 5 min), concentrate the supernatant (rotary evaporator, temperature is 60 ° C) The rotation speed is 40 rpm.) The concentration extract is obtained, and the volume fraction of ethanol is added to the concentrated extract is 80% ethanol solution, and the c...

Embodiment 2

[0045] The difference between the embodiment and the first embodiment is:

[0046] In step (3), first, 0.5 mmol of PEI-Pol Pluronic-polyethyleneimide PEI-p-p-pBA is dissolved in 50 ml of tetrahydrofuran, and then add 0.05 mol of cycloyl group. The saturated ethanol solution of silicone forms a mixture.

[0047] In step (4), 100 mg of Pranik Pluronic-polyethyleneimine PEI-phenylene boronic acid PBA-drug mulgulululine polybar is first dissolved in 50 ml of tetrahydrofuran, and then 5 ml of triethanolamine, forming a mixture.

[0048] In this example, Pranik Pluronic-polyethyleneimine PE-phenyl boronic acid PBA-drug mulberry polygonacin is used to load 1-DNJ, and its drug rate and encapsulation rate are shown in Table 2; resulting 1- The release of deoxyomycin sustained release preparation under different pH conditions image 3 Indicated.

[0049] Table 2 Loading rate and encapsulation rate

[0050] Particle size (nm) Inclusion rate (%) Drug rate (%) Pharmango polysac...

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Abstract

The invention discloses a preparation method of 1-deoxynojirimycin sustained-release preparation using mulberry leaf polysaccharide as a carrier, comprising the following steps: synthesis of Pluronic-polyethyleneimine PEI; Pluronic-polyethylene Synthesis of imine PEI-phenylboronic acid PBA; Pluronic Pluronic-polyethyleneimine PEI-phenylboronic acid PBA-drug mulberry leaf polysaccharide nanocarrier. The invention uses the active polysaccharide of mulberry leaves as a base material, self-assembles into a nano-carrier after modification, and is used for loading and transporting the hypoglycemic drug 1-DNJ; The ratios were relatively high, and the particle size was basically unchanged before and after drug loading. The 1-deoxynojirimycin sustained-release preparation can maintain the slow release of 1-DNJ under different physiological conditions, improve the half-life, and at the same time enable the drug mulberry polysaccharide carrier and DNJ to exert a synergistic hypoglycemic effect.

Description

Technical field [0001] The present invention relates to the field of drug sustained release applications. Specifically, a method of preparing a 1-deoxyomycin formulation in a carrier is a carousel. Background technique [0002] The medicine is the only black smented mulberry species in my country. It is mainly cultivated in the Xinjiang Aksu, Kuqiu and Hetian area, has been used as the Uighur folk medicinal materials, mulberry leaves, mulberry, mulberry, bloody, blood and sedation, etc. Medicinal effect. [0003] Studies have shown that drugs have significant hypoglycemic and inhibit blood lipids and have multi-directional regulatory effects on the treatment of diabetes. In addition, 1-deoxyomycin (1-DNJ) is a polyhydroxypiperidine alkali having a higher content of a pharmaceutical mulberry leaves, has a biological activity such as hypoglycemic, antiviral, anti-tumor, and has broad application prospects. However, the half-life of 1-DNJ in the body is very short, about 2 h. Theref...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K31/445A61K31/715A61P3/10C08B37/00
CPCA61K31/445A61K31/715A61K47/36A61P3/10C08B37/0003A61K2300/00
Inventor 汪河滨邱爱军杨玲刘龙飞刘晋文
Owner TARIM UNIV
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