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Solid dispersion prepared from magnolol, honokiol or mixture of magnolol and honokiol and preparation method of solid dispersion by hot-melt extrusion

A solid dispersion and honokiol technology, which is applied in the direction of active ingredients of hydroxyl compounds, medical preparations of non-active ingredients, antipyretics, etc., can solve the problems of unstable preparations and inability to apply to industrialized large-scale production, and achieve increased Dissolution, bioavailability improvement, and simple preparation process

Inactive Publication Date: 2015-11-04
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned published patents can effectively improve the bioavailability of magnolol or honokiol or a mixture of the two, there are problems such as unstable preparations and inability to be applied to large-scale industrial production.

Method used

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  • Solid dispersion prepared from magnolol, honokiol or mixture of magnolol and honokiol and preparation method of solid dispersion by hot-melt extrusion
  • Solid dispersion prepared from magnolol, honokiol or mixture of magnolol and honokiol and preparation method of solid dispersion by hot-melt extrusion
  • Solid dispersion prepared from magnolol, honokiol or mixture of magnolol and honokiol and preparation method of solid dispersion by hot-melt extrusion

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Magnolol (1%), xylitol (10%), copovidone S-630 (89%) are mixed homogeneously, cross 60 mesh sieves, be prepared into physical mixture, the extrusion temperature of twin-screw extruder is set At 90°C, after the temperature rises to the set value and stabilizes, slowly increase the rotation speed to 50rpm, add the physical mixture at a constant speed to obtain a strip-shaped extrudate, cool, and pulverize through a 20-mesh sieve to obtain a magnolol solid dispersion powder.

Embodiment 2

[0021] Magnolol (20%), xylitol (20%), copovidone S-630 (60%) are mixed homogeneously, cross 80 mesh sieves, be prepared into physical mixture, the extrusion temperature of twin-screw extruder is set At 90°C, after the temperature rises to the set value and stabilizes, slowly increase the rotation speed to 50rpm, add the physical mixture at a constant speed to obtain a strip-shaped extrudate, cool, and crush through a 100-mesh sieve to obtain a magnolol solid dispersion powder.

Embodiment 3

[0023] Honokiol (50%), mannitol (10%), polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (40%) are mixed homogeneously, cross 100 mesh sieves, be prepared into physical mixture , set the extrusion temperature of the twin-screw extruder at 90°C. After the temperature rises to the set value and stabilizes, slowly increase the speed to 50rpm, add the physical mixture at a uniform speed, and obtain a strip-shaped extrudate, cool it, and crush it through 60 mesh Sieve to obtain magnolol solid dispersion powder.

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Abstract

The invention belongs to the field of pharmaceutical preparations and particularly discloses solid dispersion prepared from magnolol, honokiol or a mixture of the magnolol and the honokiol and a preparation method of the solid dispersion by hot-melt extrusion. The solid dispersion is mainly characterized in that polyethylene glycol, copovidone S-630, hydroxy propyl cellulose, acrylic resin or polyethylene caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer serves as a main adjuvant of a dispersion supporter, a sugar alcohol adjuvant is added to serve as a plasticizer when necessary, and the HME (hot-melt extrusion) technology serves as the preparation technology, so that medicines are dispersed in the adjuvant of the supporter in an amorphous state, dissolution rate of the medicines is increased, and bioavailability of the medicines is improved. Compared with a conventional solid dispersion preparation technology, the hot-melt extrusion technology adopted in the preparation method has the advantages of nonuse of organic solvents, safety, no pollution, stable process, continuous operation and easiness for enlarged industrialized production.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to a hot-melt extrusion method for preparing a solid dispersion of magnolol or honokiol or a mixture of the two. Background technique [0002] Magnolol (magnolo) and honokiol (honokiol) are active ingredients isolated from Magnoliaceae Magnolia officinalis, and belong to biphenol compounds. Studies have found that magnolol and honokiol have good pharmacological activities such as anti-inflammatory, anti-bacterial, anti-depressant, anti-tumor, muscle relaxation, lowering cholesterol and anti-aging, and are very promising economic crops of traditional Chinese medicine. However, due to the low solubility of magnolol and honokiol in water, their oral bioavailability is very low. Solid dispersion technology can disperse drugs in carrier excipients in an amorphous form, effectively increasing the dissolution of drugs, thereby improving their bioavailability. [0003] Hot-melt extrusion technology i...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/14A61K31/05A61K47/34A61K47/32A61K47/38A61K47/48A61P29/00A61P31/04A61P35/00A61P21/02A61P3/06A61P39/06
Inventor 狄留庆李杰李俊松康安乔宏志
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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