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Construction of long-circulating liposome of fraxetin and its research on anti-enteritis effect

A technology of long-circulating liposomes and qupretin is applied in the directions of liposome delivery, medical preparations of non-active ingredients, and active ingredients of heterocyclic compounds, which can solve the problems of low in vitro release and bioavailability, and achieve Low cost, simple preparation method, and the effect of improving solubility

Pending Publication Date: 2021-05-07
ZHANGJIAGANG HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The purpose of the present invention is to solve the problems of poor water solubility, in vitro release and low bioavailability of afredetin, and provide a method for the construction of afredetin long-circulating liposomes and its anti-enteritis effect. The preparation of growing circulating liposomes can significantly improve the solubility and in vitro release of fencetin, thereby further improving the curative effect of fencetin pharmaceutical preparations, and its preparation method should be simple

Method used

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  • Construction of long-circulating liposome of fraxetin and its research on anti-enteritis effect
  • Construction of long-circulating liposome of fraxetin and its research on anti-enteritis effect
  • Construction of long-circulating liposome of fraxetin and its research on anti-enteritis effect

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Experimental program
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Effect test

Embodiment 1

[0031] The construction of a long-circulating liposome of afracetin and its anti-intestinal inflammatory effect The mass ratio of phospholipid to cholesterol in the prescription (A), the ratio of drug to phospholipid (B) and the dosage of DSPE-PEG 2000 (C) and other influencing factors OK for:

[0032] Taking the mass ratio of phospholipid to cholesterol (A), the ratio of drug to phospholipid (B) and the amount of DSPE-PEG 2000 (C) as the influencing factors, the construction of a long-circulating liposome of afracetin was optimized by orthogonal experiments and its anti-enteritis effect research prescription. Secondly, the quality of the construction of a frucetin long-circulating liposome and its anti-enteritis effect was investigated with the particle size and encapsulation efficiency as indicators. The factor level table is shown in Table 1, and the experimental results are shown in Table 2.

[0033] Table 1 Influencing factors and levels of orthogonal test

[0034] ...

Embodiment 2

[0039] Construction of a long-circulating liposome of fencetin and its preparation for anti-enteritis research:

[0040] The formulation factors affecting EE% and particle size were determined by orthogonal experimental design. In the experimental design, K1, K2 and K3 were used to represent the sum of each level (Table 2). The order of the influence of various factors on the EE% and particle size of afracetin long-circulating liposomes is B>A>C>D, and the best prescription is A 2 B 1 C 2 . The results showed that the frucetin long-circulating liposomes prepared at this time had the smallest particle size and the highest EE%.

[0041] Long-circulating liposomes were successfully prepared by thin-film dispersion method. Lecithin, cholesterol, DSPE-PEG and afracetin were co-dissolved in 20mL absolute ethanol and put into a round bottom flask. The ratio of phospholipids to cholesterol is 10:1, the ratio of fencetin to phospholipids is 1:8, and the dosage of DSPE-PEG2000 is 8%...

Embodiment 3

[0045] Study on Pharmacokinetics of Long-Circulating Liposomes of Frucetin

[0046] (1) In vivo studies

[0047] Sprague-Dawley (SD) rats (200±20g, male) were provided by the Animal Experiment Center of Zhangjiagang Hospital of Traditional Chinese Medicine Affiliated to Nanjing University of Traditional Chinese Medicine. Before the experiment, all mice were fasted for 12 h, but allowed to drink water freely. The 12 rats were randomly divided into two groups, ie, the free frucetin group and the frucetin long-circulating liposome group, with 6 rats in each group. The two groups of rats were given the same dose (200 mg / kg) of free afrescetin (suspended in 0.5% sodium carboxymethylcellulose solution) and afrescetin long-circulating liposomes. Whole blood samples (0.5 mL each) were collected at different time points (0.08, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 h) after administration. Plasma was collected after whole blood was centrifuged (3700rpm, 10min), and store...

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Abstract

The invention discloses construction of a long-circulating liposome of fraxetin and its research on anti-enteritis effect, belongs to the field of pharmaceutical preparations, and aims to provide a long-circulating liposome of fraxetin capable of improving the drug loading capacity so as to improve the solubility and oral bioavailability of fraxetin and improve its effect on enteritis. The key point of the technical scheme is the construction of the long-circulating liposome of fraxetin and its research on the anti-enteritis effect. The liposome is composed of a liposome bilayer and fraxetin, and is prepared by adopting a film dispersion method. The liposome bilayer contains phospholipid, cholesterol and a PEG (Polyethylene Glycol) modifier. The preparation method is simple, easy to operate and good in repeatability. The prepared long-circulating liposome of fraxetin has a small particle size and a high drug encapsulation efficiency, the in-vitro solubility and the in-vivo bioavailability of the long-circulating liposome of fraxetin are enhanced, and the anti-enteritis treatment effect of the long-circulating liposome of fraxetin is enhanced. According to the invention, preliminary information is provided for clinical application of the fraxetin and other similar water-insoluble compounds.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to the construction of a long-circulating liposome of afrucetin and the research on its anti-enteritis effect [0002] technical background [0003] Qinpi is a commonly used Chinese herbal medicine. It was first recorded in "Shen Nong's Materia Medica", and it was derived from the bark or stem of Qinpi, Xiaoyeqinpi or Baiwa in the Qinling area. Its main effects are clearing away heat and dampness, relieving asthma and relieving cough, clearing away heat and improving eyesight. It is clinically used to treat enteritis, leucorrhea, chronic bronchitis, bacillary dysentery, psoriasis, etc. The main chemical constituents of quincetin are coumarins, and cereolone is the main coumarin monomer. [0004] Frucetin is a natural coumarin compound named 7,8-dihydroxy-6-methoxycoumarin. It is a flaky crystal that is normally light yellow in color. Afracetin is very solub...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/37A61K47/24A61K47/28A61P1/00A61P1/04
CPCA61K9/1271A61K9/1277A61K31/37A61K47/24A61K47/28A61P1/00A61P1/04
Inventor 缪志伟顾鸣佳肖龙王利兵徐艳
Owner ZHANGJIAGANG HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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