Long-circulating liposome freeze-drying oral preparation of magnolia cortex total phenol and preparation method of freeze-drying oral preparation

A long-circulation liposome and oral preparation technology, which is applied in liposome delivery, freeze-drying delivery, anti-inflammatory agents, etc., can solve the problems of no new dosage form of magnolol total phenols and limit the clinical application of magnolia , to achieve the effects of prolonging the residence time, reducing the number of medications and high blood drug concentration

Inactive Publication Date: 2018-05-08
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are research reports on new dosage forms such as honokiol and magnolol monomer micelles, β-cyclodextrin nanopartic

Method used

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  • Long-circulating liposome freeze-drying oral preparation of magnolia cortex total phenol and preparation method of freeze-drying oral preparation
  • Long-circulating liposome freeze-drying oral preparation of magnolia cortex total phenol and preparation method of freeze-drying oral preparation
  • Long-circulating liposome freeze-drying oral preparation of magnolia cortex total phenol and preparation method of freeze-drying oral preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Magnolol long-circulating liposome lyophilized oral preparation, the composition of which is as follows:

[0033]

[0034] Preparation method: Weigh 6 mg of magnolol total phenols, 48 ​​mg of soybean lecithin, 6 mg of cholesterol, and 6 mg of DPPE-MPEG2000, add them to 220 ml of methanol-chloroform mixed organic solvent (4:1, v / v), place in an eggplant-shaped bottle, Stir at room temperature until completely dissolved to obtain a mixed solution with a total concentration of 0.3 mg / ml. The mixed solution was rotary evaporated under reduced pressure at 40° C. to remove the organic solvent until a thin film was formed on the inner wall of the bottle, and the vacuum was continued for 1 h to remove the residual organic solvent. Add 20ml of ultrapure water to the dried eggplant-shaped bottle to fully submerge the film on the wall of the bottle, stir and hydrate at 60°C for 1 hour, and then ultrasonicate at intervals in an ice bath (power 80W, ultrasonic at intervals of 4 s...

Embodiment 2

[0036] Magnolol long-circulating liposome lyophilized oral preparation, the composition of which is as follows:

[0037]

[0038] Preparation:

[0039] (1) Total magnolol, soybean lecithin, cholesterol, DPPE-MPEG2000 are added in methanol-chloroform mixed organic solvent (6:1, v / v), make total magnolol, soybean lecithin, cholesterol, DPPE-MPEG2000 The total concentration is 0.5mg / ml, stirred at room temperature until completely dissolved;

[0040] (2) Rotate the mixed solution under reduced pressure at 45°C to remove the organic solvent and form a thin film;

[0041] (3) Add water to the film, stir at 50°C, then sonicate in an ice bath, and finally pass through a microporous membrane (0.22 μm) to obtain a liposome suspension;

[0042] (4) Adding a lyoprotectant (trehalose: mannitol = 5:1) to the liposome suspension, freeze-dried to obtain.

Embodiment 3

[0044] Magnolol long-circulating liposome lyophilized oral preparation, the composition of which is as follows:

[0045]

[0046] Preparation:

[0047] (1) Total magnolol, soybean lecithin, cholesterol, DPPE-MPEG2000 are added in methanol-chloroform mixed organic solvent (10:1, v / v), make total magnolol, soybean lecithin, cholesterol, DPPE-MPEG2000 The total concentration is 0.7mg / ml, stirred at room temperature until completely dissolved;

[0048] (2) Rotate the mixed solution under reduced pressure at 50°C to remove the organic solvent and form a thin film;

[0049] (3) Add water to the film, stir at 70°C, then sonicate in an ice bath, and finally pass through a microporous membrane (0.22 μm) to obtain a liposome suspension;

[0050] (4) Adding a lyoprotectant (trehalose: mannitol = 9:1) to the liposome suspension and freeze-drying.

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Abstract

The invention discloses a long-circulating liposome freeze-drying oral preparation of magnolia cortex total phenol, which comprises the following ingredients by weight percentage: 2-10% of magnolia cortex total phenol, 40-70% of soybean lecithin, 2-10% of cholesterol, 2-10% of DPPE-MPEG (dipalmitoylphosphatidylethanolamine-methoxy polyethylene glycol) 2000 and 15-30% of freeze-drying protective agent. The liposome freeze-drying preparation of the magnolia cortex total phenol has a slow release effect in vitro; a medicine can be slowly released within 24h, so that the in-vivo retention time ofthe medicine is prolonged; and the medication frequency is reduced. A pharmacokinetic experiment result shows that the liposome freeze-drying preparation of the magnolia cortex total phenol has a higher blood concentration and a longer half life after intragastric administration; the medicine is absorbed quickly and eliminated slowly, is high in bioavailability and can serve as a long circulatingoral preparation; a new magnolia cortex total phenol dosage form that is safer and more effective and has a lasting effect is provided clinically.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an oral preparation of total magnolol, especially a freeze-dried oral preparation of total magnolol long-circulation liposome, and also relates to a preparation method of the preparation. Background technique [0002] Magnolia officinalis is an important traditional Chinese medicinal material in my country, among which honokiol and magnolol are the main components, which have anti-oxidation, antibacterial, anti-virus, anti-tumor, anti-inflammatory and analgesic, anti-tumor, myocardial protection, Blood protection, calmodulin antagonism, liver protection, liver protection, anti-anxiety, anti-depression, anti-senile dementia, anti-morphine withdrawal reaction, inhibition of catecholamines, anti-coagulation, anti-ulcer and other pharmacological effects in Parkinson's disease. Honokiol and magnolol have poor water solubility and are easily oxidatively degraded. Their oral bioa...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K36/575A61K47/26A61K47/10A61K9/19A61P39/06A61P31/04A61P31/12A61P35/00A61P29/00A61P9/00A61P9/10A61P3/14A61P1/16A61P25/22A61P25/24A61P25/28A61P25/36A61P25/16A61P7/02A61P1/04A61P17/02
CPCA61K9/127A61K9/19A61K36/575A61K47/10A61K47/26
Inventor 陈勇刘红陈一桢张文娟王俏朱明丽秦吟刘文锦
Owner HUBEI UNIV
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