Emodin solid dispersion as well as preparation method and application thereof

A technology of solid dispersion and emodin, applied in the field of medicine, can solve the problems of weakening the advantages of solid dispersion, and achieve the effects of reducing Gibbs free energy and electrical conductivity, enhancing interaction, and improving supersaturation and stability.

Active Publication Date: 2021-11-09
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, previous studies have shown that emodin binary solid dispersions often exhibit a "spring parachute effect", which greatly weakens the advantages of solid dispersions

Method used

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  • Emodin solid dispersion as well as preparation method and application thereof
  • Emodin solid dispersion as well as preparation method and application thereof
  • Emodin solid dispersion as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Prescription: Preparation of Emodin Ternary Solid Dispersion by Hot Melt Extrusion (1 / 1 / 6)

[0052]

[0053] Weigh 60g of polyvinylpyrrolidone, 10g of emodin raw material, and 10g of nicotinamide in a polyethylene bag and mix thoroughly for 10min, then transfer to a twin-screw hot-melt extruder, and fully melt at 160°C for 10min at 10rpm. Then gradually increase the rotating speed and place it at 40rpm to extrude; after the extrudate is cooled to room temperature, use a small pulverizer to pulverize it, pass through a 100-mesh pharmacopoeia sieve, and obtain the emodin ternary solid dispersion.

Embodiment 2

[0055] Prescription: Preparation of Emodin Ternary Solid Dispersion by Hot Melt Extrusion (1 / 2 / 5)

[0056]

[0057] Weigh 50g of polyvinylpyrrolidone, 10g of emodin raw material, and 20g of nicotinamide in a polyethylene bag and mix thoroughly for 10 minutes, then transfer to a twin-screw hot-melt extruder, and fully melt at 160°C for 10 minutes at 10 rpm. Then gradually increase the rotating speed and place it at 40rpm to extrude; after the extrudate is cooled to room temperature, use a small pulverizer to pulverize it, pass through a 100-mesh pharmacopoeia sieve, and obtain the emodin ternary solid dispersion.

Embodiment 3

[0059] Prescription: Preparation of Emodin Ternary Solid Dispersion by Hot Melt Extrusion (2 / 1 / 5)

[0060]

[0061] Weigh 60g of polyvinylpyrrolidone, 20g of emodin raw material, and 10g of nicotinamide in a polyethylene bag and mix thoroughly for 10 minutes, then transfer to a twin-screw hot-melt extruder, and fully melt at 160°C for 10 minutes at 10 rpm. Then gradually increase the rotating speed and place it at 40rpm to extrude; after the extrudate is cooled to room temperature, use a small pulverizer to pulverize it, pass through a 100-mesh pharmacopoeia sieve, and obtain the emodin ternary solid dispersion.

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Abstract

The invention belongs to the technical field of medicines, and particularly discloses an emodin solid dispersion as well as a preparation method and application thereof. The emodin solid dispersion disclosed by the invention is obtained by mixing emodin, a high polymer carrier and a bonding agent and then treating through a hot melt extrusion technology, and the drug loading capacity of the emodin solid dispersion is 5-20%. Through Lewis acid-base and hydrogen-bond interaction, an emodin molecular dimer structure is broken, so that an amorphous drug is in a supersaturated state; meanwhile, the emodin solid dispersion system is relatively low in Gibbs free energy and molecular mobility and relatively strong in intermolecular interaction, so that the physical stability of the amorphous preparation is enhanced, and the in-vitro dissolution of the amorphous preparation is prolonged; according to the emodin solid dispersion and the preparation method thereof, no organic solvent is used, the preparation is safe and efficient, the obtained emodin solid dispersion improves the dissolution rate and solubility of insoluble drugs, the drug loading capacity is high, the stability is good, a good intermediate is provided for other oral solid preparations of emodin, and the preparation process is simple, efficient, safe and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an emodin solid dispersion, a preparation method thereof and its application in pharmaceutical intermediates. Background technique [0002] Rhubarb is the dry root and rhizome of Rheum palmatum L., Rheum tanguticum Maxim.Ex Balf. or medicinal Rheum officinale Baill. of the Polygonaceae plant. . Emodin is an anthraquinone derivative and the main effective monomer of the traditional Chinese medicine rhubarb. In recent years, clinical studies have shown that emodin has antibacterial, anti-inflammatory, anti-tumor, and immunosuppressive effects, and has received high attention. However, emodin has poor water solubility (<0.1g / 100mL, 19°C) and low bioavailability, which limits its clinical application effect. In addition, emodin has a pKa value of 6.30, which is weakly acidic and pH-dependent, and it is almost insoluble in the acidic environment of the stomach, but its solubility...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/122A61K47/54A61K47/58A61P29/00A61P31/04A61P35/00A61P37/06
CPCA61K31/122A61K47/542A61K47/545A61K47/58A61K9/146A61P29/00A61P31/04A61P35/00A61P37/06
Inventor 杨建宏张朝阳乔鑫李莉张茜赵启鹏
Owner NINGXIA MEDICAL UNIV
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