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Preparation method of silibinin nano-cage type nanocrystalline injection

A technology of silibinin and nanocrystals, which is applied in the field of medicine, can solve the problems of difficulty in exerting drug effects, increasing the risk of liver and spleen damage, and weakening the treatment effect, so as to improve relative bioavailability, increase average residence time, prolong The effect of blood circulation time

Inactive Publication Date: 2019-06-18
QILU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This results in: (1) Reduced drug efficacy - nanocrystals are naturally targeted to organs with abundant MPS, such as the liver and spleen; while the lesions are tissues and organs with few or no macrophages, it is difficult to gather nanocrystal drugs, and it is difficult to Difficult to exert corresponding medicinal effect
(2) Increase the risk of liver and spleen damage—drugs that accumulate in large quantities in macrophage-rich organs such as the liver and spleen, especially antineoplastic drugs, will cause imbalances in cell homeostasis and cause drug-induced damage to organs such as the liver and spleen
[0016] Although silibinin has a variety of strong pharmacological effects, due to its low water solubility, it seriously affects its absorption and distribution in the body, which greatly reduces the bioavailability and weakens the therapeutic effect.
Although the solubility can be increased in the form of phospholipid complex or meglumine salt, there are problems such as instability and large local irritation of injection administration

Method used

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  • Preparation method of silibinin nano-cage type nanocrystalline injection
  • Preparation method of silibinin nano-cage type nanocrystalline injection
  • Preparation method of silibinin nano-cage type nanocrystalline injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1 Formula and preparation method of silibinin nanocage nanocrystal injection of the present invention

[0032] Formula and preparation of silibinin nanocage nanocrystal injection: Weigh 40mg of silibinin and dissolve it in 10ml of methanol, stir magnetically at room temperature until completely dissolved to obtain 4mg ml -1 The methanol solution of silibinin was used as the solvent phase. Weigh 40mg PEG-CS dissolved in 50ml ultrapure water as the anti-solvent phase. Use a syringe with a microporous filter (0.45 μm) to draw 4 ml of the anti-solvent phase solution and inject it into the vial, and in addition take a syringe with a microporous filter (0.45 μm) to draw 1 ml of silibinin methanol solution and quickly inject it into the bottle containing In the vial of the anti-solvent phase, after magnetic stirring for 1 min, add 0.8 mg PEG-PCL carrier into the solution, then add copper sulfate and sodium ascorbate in sequence, after standing for 20 min, ultraso...

Embodiment 2

[0034] Example 2 The process and preparation performance detection test of silibinin nanocage nanocrystal injection

[0035] (1) Repeated inspection

[0036] Three batches of silibinin nanocage nanocrystal injection were prepared under the prescription process conditions of Example 1, and the average particle size, particle size distribution (PDI) and Zeta potential were measured respectively, and the results are shown in Table 1. The optimized nanocrystal formulation process conditions have good repeatability.

[0037] Table 1 Repeatability investigation of silibinin nanocage nanocrystal injection process

[0038] batch

Average particle size (nm)

PDI

Zeta potential (mV)

1

126.34

0.114

-26.81

2

132.51

0.125

-27.54

3

121.64

0.119

-29.96

RSD(%)

4.30

4.62

5.87

[0039] (2) Morphological analysis

[0040] Select two mica sheets, stick the surface layer off with adhesive tape, then drop the ...

Embodiment 3

[0043] Example 3 Preliminary stability study of silibinin nanocage nanocrystal injection

[0044] In order to investigate the stability of the liquid preparation - silibinin nanocrystals, the silibinin nanocage nanocrystal injection prepared in Example 1 was stored at different temperatures (4°C and 25°C) for one month, and laser The nano particle size analyzer takes samples at 1, 2, 3, and 4 weeks respectively, observes the appearance change and measures the particle size and PDI. Each sample is measured 3 times, and the average value is calculated and the data is recorded.

[0045] Table 2 Stability test of silibinin nanocage nanocrystal injection at 4°C

[0046]

[0047] Table 3 Stability test of silibinin nanocage nanocrystal injection at 25°C

[0048]

[0049]

[0050] According to the test results, the silibinin nanocage nanocrystal injection maintained good stability under the storage condition of 4°C; precipitation. It can be concluded that the silibinin ...

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Abstract

The invention discloses a preparation method of a silibinin nano-cage type nanocrystalline injection and belongs to the technical field of medicines. The nano-cage type nanocrystalline injection is prepared from ingredients as follows: an active ingredient, namely, silibinin, a nano-cage type nanocrystalline drug release system and an organic solvent used for dissolving the active ingredient, namely, silibinin, wherein the nano-cage type nanocrystalline drug release system is formed by PEG-PCL (polyethylene glycol-polycaprolactone) and PEG-CS (polyethylene glycol-chitosan). The prepared silibinin nano-cage type nanocrystalline injection has good physical stability, the blood circulation time of the drug can be prolonged after drug administration, the relative bioavailability is improved, the average retention time in vivo is prolonged, and the silibinin nano-cage type nanocrystalline injection has long cyclicity and passive targeting property.

Description

technical field [0001] The invention relates to a preparation method of silibinin nanocage nanocrystal injection. The invention belongs to the technical field of medicine. Background technique [0002] In order to improve the solubility and bioavailability of poorly soluble drug candidates, Professor Müllar of the Free University of Berlin proposed nanocrystal technology for pharmaceutical preparations in 1991. Nanocrystals, also known as nanosuspensions, are heterogeneous submicron colloidal dispersion systems composed of a small amount of surfactants or (and) polymer materials as stabilizers, and pure drug particles of nanometer size. [0003] Currently, paclitaxel, amphotericin B, etoposide, teniposide, nevirapine, telmisartan, probucol, indomethacin, fenofibrate, pranlukast, rebamipide , Ezetimibe, Paliperidone Palmitate, Riboflavin Laurate, Baicalin, Quercetin, Resveratrol, Curcumin, Ursodeoxycholic Acid, Hydroxycamptothecin, Nanqiangectin , silybin, puerarin and man...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/34A61K47/36A61K31/357A61P1/16A61P31/12A61P3/06A61P3/10A61P7/02A61P9/00A61P9/10A61P7/04A61P35/00
Inventor 马迎迎王言才刘扬扬赵娟
Owner QILU UNIV OF TECH
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