Cepharanthine nanosuspension and preparation method thereof

A nano-suspension, the technology of Stephalin, which is applied in the field of medicine, can solve the problems of not improving the dissolution rate and bioavailability of stepherin, not eliminating vascular irritation, and poor patient compliance, so as to improve the oral Bioavailability, increased specific surface area, and enhanced steric hindrance

Inactive Publication Date: 2019-08-23
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The preparation has low drug loading and most of them have poor stability
[0007] Chinese invention patent CN102475680A (publication number) discloses "a stepahin hydrochloride injection and its preparation method and detection method". , but because the preparation is an injection, the preparation process is complicated and the irrit

Method used

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  • Cepharanthine nanosuspension and preparation method thereof
  • Cepharanthine nanosuspension and preparation method thereof
  • Cepharanthine nanosuspension and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Embodiment 1: the preparation of stepahelin nanosuspension

[0043] Weigh 0.1 g of the stephenin raw material drug, add it into 50 mL of distilled water, stir evenly to obtain an aqueous stabilizer solution, and stir under magnetic stirring for 20 minutes to obtain a coarse suspension. Add 140 mL of grinding media (specification d=0.6-0.8 mm) into the grinding chamber of the sand mill, transfer the coarse suspension to the grinding chamber, and grind for 45 min at 2000 rpm to obtain rod-shaped nanomixed particles with a particle size of 585.65 nm. Suspension ( figure 1 a), XPS is the surface element analysis of patinol ( image 3 a), the crystalline state of the drug as Figure 5 a and Figure 6 a shows obvious characteristic peaks.

Embodiment 2

[0044] Embodiment 2: the preparation of paternogenin nanosuspension

[0045]Weigh 0.1 g of vitamin E polyethylene glycol 1000 succinate, add 50 mL of distilled water, and stir evenly to obtain an aqueous stabilizer solution, add 0.5 g of stepherin raw material under magnetic stirring, and stir for 20 minutes to obtain a coarse suspension. Add 140 mL of grinding media (specification d=0.6-0.8 mm) into the grinding chamber of the sand mill, transfer the coarse suspension to the grinding chamber, and grind for 45 min at 2000 rpm to obtain a particle size of 36.2 nm ( figure 1 c), a rod-shaped nanosuspension at a potential of 6.34 mV ( figure 2 b), XPS analysis shows that the stable nanosuspension of TPGS shows the decrease of the N element of the raw material drug and the adsorption amount of TPGS on the surface of the nanosuspension particles determined by TGA, all confirming that the carrier covers the surface of the nanoparticles ( image 3 c), ( Figure 4 ). In addition, ...

Embodiment 3

[0046] Embodiment 3: the preparation of stepahelin nanosuspension

[0047] Weigh 0.03g of sodium alginate and 0.01g of sodium lauryl sulfate, add 50mL of distilled water, and stir evenly to obtain an aqueous stabilizer solution, add 0.8g of stephadin raw material under magnetic stirring, and stir for 20 minutes to obtain a coarse suspension liquid. Add 140 mL of grinding medium (specification d=0.6-0.8 mm) into the grinding chamber of the sand mill, transfer the coarse suspension to the grinding chamber, and grind for 45 min at 2030 rpm to obtain an opalescent nanosuspension.

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Abstract

The invention relates to a cepharanthine nanosuspension and a preparation method thereof. The cepharanthine nanosuspension is obtained through nano-treatment of cepharanthine and a stabilizer aqueoussolution, wherein the stabilizer is one or any combinations of a space stereo stabilizer, a charge stabilizer and a super disintegrating agent. The prepared celastatin suspension has the advantages ofhigh dissolution and high bioavailability. The celastatin suspension can be used as a finished preparation or a preparation intermediate for preparing a solid/liquid cepharanthine preparation, and the stable absorption and effects of the drug can be both ensured. Moreover, the technology is feasible, stable and reliable, the production cost is low, and the scale industrial production is easy to achieve.

Description

technical field [0001] The present invention belongs to the technical field of medicine, and in particular relates to a stepherin nanosuspension and a preparation method thereof, and further relates to the use of the stepherin nanosuspension as a preparation intermediate to prepare other solid or liquid pharmaceutical preparations, and The obtained stepherin in solid or liquid state. Background technique [0002] Cepharanthine (CPA) is a bisbenzylisoquinoline alkaloid monomer compound, which is extracted and isolated from the tubers of the genus Stephaniaceae. Stephalin has a wide range of biological activities and has been used clinically, mainly for the treatment of leukopenia, with no obvious side effects. Studies have shown that stepherin also plays an important role in the development of anti-tumor. Stepherin can promote the apoptosis of various malignant tumor cells including human leukemia cell lines, cholangiocarcinoma cells and oral squamous cell carcinoma cells, b...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/38A61K47/32A61K47/22A61K47/36A61K47/20A61K47/10A61K47/24A61K31/4741A61K36/59A61P7/00A61P35/00A61P35/02
CPCA61K9/10A61K31/4741A61K36/59A61K47/10A61K47/20A61K47/22A61K47/24A61K47/32A61K47/36A61K47/38A61P7/00A61P35/00A61P35/02
Inventor 杨建宏付亭亭彭晓东侯延辉苟国敬
Owner NINGXIA MEDICAL UNIV
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