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SchisandrinB solid dispersion as well as preparation method and preparation thereof

A technology of schisandrin B and solid dispersion, which is applied in the directions of non-active ingredients, such as medical preparations, pharmaceutical formulations, and active ingredients of heterocyclic compounds, can solve the problem that patients take a large dose, and there is no literature report to increase the solubility of schisandra B. Dissolution, increase side effects and other problems, to achieve the effect of improving in vitro dissolution, improving bioavailability and formulation stability

Active Publication Date: 2013-12-25
ZHEJIANG DINGHUI PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, in the research, it was found that schisandrin B is easily soluble in organic solvents such as chloroform, ethanol, methanol, acetone, etc., but difficult to dissolve in water, and the oral availability is very low, resulting in a large actual dose of patients, potentially increasing side effects
Improving the solubility or dissolution rate of Schizandrin B can increase the bioavailability of the drug in the body, thereby achieving the purpose of reducing toxicity and increasing efficiency, but so far there is no literature report on measures to increase the solubility or dissolution rate of Schizandrin B

Method used

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  • SchisandrinB solid dispersion as well as preparation method and preparation thereof
  • SchisandrinB solid dispersion as well as preparation method and preparation thereof
  • SchisandrinB solid dispersion as well as preparation method and preparation thereof

Examples

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Effect test

Embodiment 1

[0026] Embodiment 1: Solvent method prepares Schizandrin B / PVP solid dispersion

[0027] Measure 500ml of ethanol, add 15g of povidone K90 into it, fully shake and dissolve. Then add 5 g of schisandrin B, add in a rotary evaporator, concentrate until the solvent is basically volatilized, quench, and dry, and the obtained solid is pulverized and passed through a 80-mesh sieve to obtain the solid dispersion of the present invention.

Embodiment 2

[0028] Embodiment 2: Solvent method prepares Schizandrin B / PVP solid dispersion

[0029] Measure 500ml of ethanol, add 20g of povidone K90 into it, fully shake and dissolve. Then add 5 g of schisandrin B, add in a rotary evaporator, concentrate until the solvent is basically volatilized, quench, and dry, and the obtained solid is pulverized and passed through a 80-mesh sieve to obtain the solid dispersion of the present invention.

Embodiment 3

[0030] Embodiment 3: Solvent method prepares Schizandrin B / PVP solid dispersion

[0031] Measure 500ml of ethanol, add 30g of povidone K90 into it, fully shake and dissolve. Then add 5 g of schisandrin B, add in a rotary evaporator, concentrate until the solvent is basically volatilized, quench, and dry, and the obtained solid is pulverized and passed through a 80-mesh sieve to obtain the solid dispersion of the present invention.

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Abstract

The invention provides a schisandrinB solid dispersion and a preparation method thereof as well as a medical preparation containing the solid dispersion. The schisandrinB solid dispersion is prepared from main raw materials including schisandrinB and povidone at the weight ratio of 1:(2-8) by a solvent method or a grinding method. The results of vitro dissolution, DSC and XRD examination and stability test of the obtained schisandrinB solid dispersion and the preparation thereof show that the prepared solid dispersion of the schisandrinB, disclosed by the invention, exists in an amorphism state or a molecular state, the vitro dissolution is greatly improved, the prepared preparation is stable, and the oral bioavailability of the schisandrinB is improved.

Description

(1) Technical field [0001] The invention relates to a solid dispersion of schisandrin B, a preparation method thereof, and a pharmaceutical preparation containing the solid dispersion. (2) Background technology [0002] Schisandrin B (SchB) mainly comes from Magnoliaceae plants, such as Magnoliaceae Schisandra (Schisandra chinensis (Turcz.) Baill), Magnoliaceae Schisandra (Schisandra sphenanthera Rehd.et Wils.), Magnoliaceae North Schisandra (Schisandra chinensis Baill), can also be artificially synthesized. Lignans are the main medicinal components of Schisandra chinensis, which mainly have anti-tumor, anti-virus, liver protection, and anti-aging effects. Schizandrin B, as one of the main active components of Schisandra lignans, has attracted much attention along with the research on lignans. Studies in recent years have shown that schisandra B has pharmacological effects such as liver protection, anti-cancer, and anti-ulcer. In recent years, it has also been reported th...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/36A61K47/32A61P1/16A61P35/00A61P1/04A61P31/04
Inventor 平其能张敏汪宇星
Owner ZHEJIANG DINGHUI PHARM
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