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Biogastrone acid prosome liposome with long circulation function and preparation method thereof

A technology of proliposome and glycyrrhetic acid, which is applied in the directions of liposome delivery, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problems such as the lack of proliposomes , to achieve the effect of simple and easy preparation method

Inactive Publication Date: 2009-02-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the research reports on glycyrrhetinic acid, Chinese patents and documents mainly focus on the invention patents of structural modification, Japan has more reports on the pharmacological effects of glycyrrhetinic acid, there is no proliposome, especially no PEG modification patents and literature reports of new liposome inventions

Method used

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  • Biogastrone acid prosome liposome with long circulation function and preparation method thereof
  • Biogastrone acid prosome liposome with long circulation function and preparation method thereof
  • Biogastrone acid prosome liposome with long circulation function and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] (1) Synthesis of intermediate lactide

[0054] Put quantitative lactic acid into the three-necked bottle, pass N 2 Gas, add zinc oxide under mechanical stirring, heat to 120°C, and evaporate the water contained in the lactic acid. Then the temperature was raised to about 140°C, and the reaction was performed for 1 hour under reduced pressure to distill off the water generated during the reaction. Repeat many times until no water evaporates. Then the temperature was raised to 180°C, the fractions were collected, and recrystallized twice with ethyl acetate to obtain white flaky crystals.

[0055]

[0056] (2) Synthesis of mPEG2000-PLA block copolymer

[0057] Add a certain proportion of lactide and mPEG2000 into the three-necked bottle, seal it, N 2 Air was removed under flow, and the heating mantle was heated to 160°C. After the contents were completely melted, 0.5 wt% stannous octoate was added, and the reaction was stopped for 8 hours under magnetic stirring. T...

Embodiment 2

[0070] Prescription: Percentage (%)

[0071] Glycyrrhetinic acid 2.50

[0072] Hydrogenated soybean lecithin 80.0

[0073] Cholesterol 7.50

[0074] Sodium chenodeoxycholate 10.0

[0075] Glycyrrhetinic acid, hydrogenated soybean phosphatidylcholine, cholesterol and sodium chenodeoxycholate were sonicated with 50mL of absolute ethanol; another 50mL of pH7.4 phosphate buffer was placed in a pear-shaped bottle, heated and stirred at 60°C for uniformity. Slowly inject the ethanol solution into the phosphate buffer, sonicate for 20 minutes to form a lipid solution, remove the ethanol by rotary evaporating the lipid solution at 45°C, pass through a 0.22 μm filter membrane three times, and remove the pyrogen to obtain glycyrrhetinic acid liposome suspension. The above-mentioned liposome is hydrated and reconstituted with 5% glucose aqueous solution to obtain the glycyrrhetinic acid liposome suspension for intravenous injection. The particle d...

Embodiment 3

[0077] Prescription: Percentage (%)

[0078] Glycyrrhetinic acid 1.12

[0079] Egg yolk lecithin 40.45

[0080] Cholesterol 6.74

[0081] Sodium glycinoxycholate 2.25

[0082] mPEG2000-PLA 4.49

[0083] Lactose 44.94

[0084] Glycyrrhetinic acid, phospholipids, cholesterol, mPEG2000-PLA and sodium glycoxycholate were ultrasonically dissolved in 50 mL of ethanol, and the ethanol was removed by rotary evaporation at 45°C to form a colloidal solution. Lactose was dissolved in an appropriate amount of purified water, and pH 7.4 phosphoric acid was added. Dilute the colloidal solution with 50 mL of salt buffer solution, sonicate for 20 minutes, pass through 0.8, 0.45 and 0.22 μm filter membranes successively, filter the membrane three times repeatedly, remove pyrogen, and obtain glycyrrhetinic acid by freeze-drying method. Body liposome preparations. Hydrate and reconstitute the above proliposome with 0.9% sodi...

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Abstract

The invention belongs to the new technical field of a drug preparation and in particular relates to a precursor liposome containing a glycyrrhetinic acid and a method for preparing the same. The precursor liposome containing the glycyrrhetinic acid consists of glycyrrhetinic acid, phospholipids, cholesterol, a surfactant and a water-soluble material; a suspension solution of the glycyrrhetinic acid liposome is prepared by an ethanol injection method or a thin-film dispersion method; and solid liposome powder is prepared by a freeze drying method or a spray drying method. The precursor liposome has simple process and good repeatability, is suitable for industrialized production; through drug administration by intravenous injection, the precursor liposome has long-circulating function, can remarkably reduce the toxicity of drug and achieve the function of prolonging the drug effect; and through oral administration, a solid preparation of the liposome can increase absorption and improve bioavailability by three to five times.

Description

technical field [0001] The invention belongs to the new technical field of pharmaceutical preparations, in particular to a proliposome preparation containing an insoluble drug glycyrrhetinic acid and a preparation method for industrial application thereof. In particular, the preparation can achieve the purpose of long-circulation effect through injection administration, and has the function of improving liver targeting. In addition, solid proliposomes can be prepared into hard capsules, tablets or granules, and the bioavailability can be significantly increased by 3 to 5 times through oral administration. Background technique [0002] Glycyrrhetinic acid (Glycyrrhetinic acid), also known as glycyrrhetinic acid, is a kind of triterpenoid saponin glycyrrhizic acid in licorice hydrolyzed to remove the product of sugar acid chain. Glycyrrhetinic acid has anti-hepatitis, anti-tumor, anti-immunity, hypolipidemic, anti-ulcer, anti-tetanus toxin and anti-HIV activities [Xie Shirong...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/56A61K47/24A61K47/34A61P1/16A61P35/00A61P37/00A61P3/06A61P1/04A61P31/00A61K47/28
Inventor 李娟王广基李帅李铁陆洋范铭
Owner CHINA PHARM UNIV
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