Preparation and application of Silybin/Silymarin polymer micelle

A technology of silymarin and silibinin, which is applied in the field of pharmaceutical preparations, can solve problems such as difficulty in ensuring safety, and achieve the effects of improving bioavailability, improving liver targeting, and promoting absorption

Inactive Publication Date: 2009-10-14
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since salt formation requires strong acid or strong base conditions; co-solvents that increase drug solubility by forming complexes with drugs, the safety of these methods is not easy to guarantee
Chinese patent application CN101317840 prepared a liver-targeted nanocomposite of wheat prolamin and silibinin, but the protein carrier has immune safety problems

Method used

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  • Preparation and application of Silybin/Silymarin polymer micelle
  • Preparation and application of Silybin/Silymarin polymer micelle
  • Preparation and application of Silybin/Silymarin polymer micelle

Examples

Experimental program
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Effect test

Embodiment 1

[0050] Example 1: Take 15 mg of polyoxyethylene-polylysine and 10 mg of silymarin, dissolve it in N,N-dimethylformamide (DMF), ultrasonicate for 10 minutes, and dialyze the solution in a dialysis bag (MWCO=12000-14000) for 24 hours , through a 0.45 μm filter membrane to obtain a drug-loaded micellar solution. The average particle size of the obtained micelles was 183.4nm, the Zeta potential was +29.7mV, the encapsulation efficiency was 33.6%, and the drug loading was 18.3%.

Embodiment 2

[0051] Example 2: Take 15 mg of polyethylene glycol-phosphatidylethanolamine and 10 mg of silymarin, dissolve it in N,N-dimethylformamide (DMF), put the solution into a dialysis bag (MWCO=12000-14000) for 24 hours, and pass through 0.45 μm filter membrane to obtain the drug-loaded micellar solution. The average particle diameter of the obtained micelles is 212.5nm, the Zeta potential is -30.3mV, the encapsulation efficiency is 41.6%, and the drug loading capacity is 21.7%.

Embodiment 3

[0052] Example 3: Take 15 mg of ethyl methacrylate-acrylic acid copolymer and 10 mg of silymarin, dissolve it in N, N-dimethylformamide (DMF), and dialyze the solution in a dialysis bag (MWCO=12000-14000) for 24 hours. 0.45μm filter membrane to obtain the drug-loaded micellar solution. The average particle size of the obtained micelles is 252.1nm, the Zeta potential is +28.6mV, the encapsulation efficiency is 23.1%, and the drug loading is 12.6%.

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Abstract

The invention relates to a Silybin / Silymarin (SLB / SM) micellar preparation using amphiphilic polymers as a carrier. By using the amphiphilic polymers as a solubilization carrier, the preparation can greatly increase the solubility of SLB / SM; the oral administration thereof can remarkably promote the absorption of SLB / SM in the gastrointestinal tract and improve the bioavailability of SLB / SM; and the injection administration thereof can achieve the liver-targeting effect of the drug, thereby improving the curative effect of the drug.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations. The invention relates to a preparation method and application of silybin and silymarin micellar preparations with amphiphilic polymers as carriers. Background technique [0002] Silymarin (Silymarin, SM) is a natural flavonoid lignan compound, which is a mixture obtained by extracting and refining the fruit of the Compositae plant Silymarin, which can directly scavenge active oxygen, inhibit 5'-lipoxygenase, and protect liver cell membranes , Promote damaged liver cells to synthesize DNA and structural proteins, immune regulation and anti-hepatic fibrosis and other pharmacological effects. In recent years, pharmacological studies have also shown that it has anti-tumor, treatment of lung injury, myocardial cell injury and other effects. Therefore, silymarin is a drug with good application prospects. The main components of silymarin are flavonoid lignans and a small amount of fatty oil...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/48A61K9/08A61K9/19A61K31/357A61K47/36A61K47/34A61K47/32A61P1/16A61P3/06A61P11/00A61P9/10A61P7/02A61P35/00A61K47/10
Inventor 周建平霍美蓉吴益平张勇李虹于迪
Owner CHINA PHARM UNIV
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