Silybin nanometer suspension and preparation method thereof

A nano-suspension and silibinin technology, 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 wide particle size distribution, difficult promotion and use, and grinding Solve problems such as medium dissolution, achieve the effect of increasing solubility and dissolution rate, simple prescription and preparation process, and improving bioavailability

Inactive Publication Date: 2017-04-26
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN105476966A discloses a silibinin-phospholipid complex nano freeze-dried powder and its preparation method; Chinese patent CN104367546A discloses a targeted temperature-controlled silibinin-loaded thermosensitive liposome-microbubble complex Preparation method of drug delivery system; Chinese patent CN104398490A discloses a preparation method of nano-sized silibinin calcium phosphate composite microcapsules; Chinese patent CN103877021A discloses silibinin nanocrystalline self-stabilizing Pickering emulsion and its preparation method; China The patent discloses CN101185637B silybin dimer self-emulsifying microemulsion preparation and its preparation method; however, the above-mentioned preparations generally have problems such as low encapsulation efficiency, leakage and instability, and are restricted by toxicity and carrier materials. Complex, high preparation cost, difficult to popularize and use, not conducive to large-scale industrial production
The general literature believes that although the preparation process of the media grinding method is simple, it takes a long time to prepare, the particle size distribution of the product is wide, and there will be problems such as the dissolution and shedding of the grinding media during the grinding process, so it is rarely used.

Method used

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  • Silybin nanometer suspension and preparation method thereof
  • Silybin nanometer suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 0.010g sodium lauryl sulfate and 0.350g hydroxypropyl cellulose, put them in a beaker, add about 7g water to dissolve them completely, and make an aqueous stabilizer solution. Weigh 1.5g of silybin raw material, put it in a grinding tank, transfer all the stabilizer aqueous solution in the beaker to the grinding tank, add a small amount of water to rinse, and finally add water to 10g. Place the grinding jar in an ultrasonic cleaner for ultrasonic dispersion for 10 min. Add about 60g of zirconia grinding beads (the mass ratio of the large and small balls is 1:5, the diameter of the large ball is 5mm, and the diameter of the small ball is 0.5mm) into the grinding jar, and balance the grinding jar in pairs on the balance, and then install the grinding jar In a planetary ball mill, grind at 300r / min for 3h to obtain silibinin nano-suspension. The silibinin nano-suspension prepared by the method has an average particle diameter of 188.2nm and a PDI of 0.21.

[0026] ...

Embodiment 2

[0028] Weigh 0.1 g of sodium lauryl sulfate and 0.1 g of polyvinylpyrrolidone, put them in a beaker, add about 7 g of water to dissolve them completely, and prepare an aqueous stabilizer solution. Weigh 1.0 g of silybin raw material, put it in a grinding tank, transfer all the stabilizer aqueous solution in the beaker to the grinding tank, add a small amount of water to rinse, and finally add water to 10 g. Place the grinding jar in an ultrasonic cleaner for 10 min. Add about 50 g of zirconia grinding beads (the mass ratio of the large and small balls is 1:5, the diameter of the large ball is 5 mm, and the diameter of the small ball is 0.5 mm) into the grinding jar, and balance the grinding jar in pairs on the balance, and then install the grinding jar Grind in a planetary ball mill at 250r / min for 4h to obtain silibinin nano-suspension. The silibinin nano-suspension prepared by the method has an average particle diameter of 238.9 nm and a PDI of 0.18.

Embodiment 3

[0030] Study on the dissolution rate of silibinin nanosuspension in vitro

[0031] The silibinin raw material drug, physical mixture and the silibinin nanosuspension spray-dried powder of Example 1 of the present invention were subjected to a dissolution contrast experiment, and the samples at different time points were assayed and the cumulative dissolution percentage was calculated. The result shows that the dissolution rate of the silibinin nano-mixture spray-dried powder of the present invention is obviously higher than the silybin bulk drug and physical mixture, see appendix figure 2 .

[0032] Dissolution assay:

[0033] Get an appropriate amount of sample (equivalent to silibinin 35mg), according to the dissolution assay (Chinese Pharmacopoeia 2015 edition four general rules 0931 second method), with 0.5% SDS aqueous solution 900ml as the dissolution medium, the rotating speed is 100r / min, operate according to law, After 10, 15, 20, 30, 45, and 60 minutes, take 5ml o...

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Abstract

The invention relates to the field of medicinal preparations, and provides a silybin nanometer suspension and a preparation method thereof. The silybin nanometer suspension is prepared from silybin, a stabilizer and water. The mass ratio of silybin to the stabilizer is 2:1-10:1. The mass ratio of the stabilizer in the suspension is 2-5%, and the mass ratio of the medicine is 10-20%. An improved medium grinding method is adopted, the obtained silybin nanometer suspension is small in grain size, narrow in distribution and good in stability, the medicine dissolution rate can be remarkably increased, and the medicine in-vivo bioavailability can be improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a silibinin nano-suspension and a preparation method thereof. Background technique [0002] Compositae plant milk thistle has been a good drug for liver protection since ancient times. Silymarin is the total extract of milk thistle fruit, and silybin is the main active ingredient in silymarin. It has anti-lipid peroxidation, stable cell membrane, It can improve liver function, and has good curative effect on acute and chronic hepatitis, liver cirrhosis and metabolic toxic liver injury; silibinin can reduce blood cholesterol concentration and further remove lipid deposition in liver and kidney tissues. It can be used for hyperlipidemia, fatty liver and alcoholic liver; in addition, the anti-tumor effect of silibinin has been paid more and more attention, and it is expected to become a high-efficiency and low-toxic anti-tumor natural drug. [0003] Silybin is almost inso...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/357A61K47/38A61K47/20A61K47/32A61K47/26A61K47/10A61P1/16A61P3/06A61P35/00
CPCA61K47/10A61K47/20A61K47/26A61K47/32A61K47/38A61K9/10A61K31/357
Inventor 蒋曙光丁祎馨
Owner CHINA PHARM UNIV
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