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Paeoniflorin ethosome, preparation method and applications thereof

A technology of paeoniflorin alcohol and plastids, which is applied in the field of medicine, can solve the problems of low bioavailability of oral paeoniflorin, and achieve the effects of improving low bioavailability, prolonging drug efficacy, and enhancing penetration

Inactive Publication Date: 2018-07-06
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The present invention aims to solve the technical problem of low bioavailability of oral paeoniflorin at present, and provides a paeoniflorin ethosome, which uses the ethosome as a transdermal drug delivery carrier, which can promote the percutaneous absorption of paeoniflorin, and can be absorbed in the deep layer of the skin. The formation of paeoniflorin drug storage can play a slow-release effect, significantly increase the retention of paeoniflorin in the treatment area, and has good stability and safety

Method used

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  • Paeoniflorin ethosome, preparation method and applications thereof
  • Paeoniflorin ethosome, preparation method and applications thereof
  • Paeoniflorin ethosome, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of paeoniflorin alcohol plastids

[0032] A paeoniflorin alcohol plastid, comprising the following raw materials: 0.05-0.3% (w / v) paeoniflorin, 2-6% (w / v) soybean lecithin S80, 0.05-1% (w / v) cholesterol, 5 ~40% (v / v) glycerol.

[0033] The preparation of the paeoniflorin alcohol plastid comprises the following steps:

[0034] Soybean lecithin S80 and cholesterol are dissolved in a certain amount of methanol:chloroform (3:1) mixed solvent as the oil phase, paeoniflorin is dissolved in a certain amount of glycerol aqueous solution to be the water phase, and the oil phase:water phase is 3:1. Proportional mixing, ultrasonication for 30min to form an emulsion, the solvent was removed under reduced pressure in a constant temperature water bath at 37°C to make the lipid form a uniform film on the bottle wall, the glycerol aqueous solution of the above recipe was added, the hydration was rotated for 1h, the probe was ultrasonicated for 2min (380w, interva...

Embodiment 2

[0035] Example 2 Preparation of paeoniflorin alcohol plastids containing volatile oil

[0036] A kind of paeoniflorin alcohol plastid body containing volatile oil of Coleus vulgaris, comprising the following raw materials: 0.3% (w / v) paeoniflorin, 2% (w / v) soybean lecithin S80, 0.05% (w / v) cholesterol, 40% % (v / v) glycerol, 3% (v / v) volatile oil of Thornweed.

[0037] The preparation of the paeoniflorin alcohol plastid body containing the volatile oil of Radix vulgaris comprises the following steps:

[0038] (1) First, mix the whole dried Radix vulgaris with water in a mass ratio of 1:12, soak for 12 hours, conduct steam distillation at 200°C, and extract the volatile oil from Radix Radix et Rhizoma after 10 hours.

[0039] (2) Soybean lecithin S80 and cholesterol are dissolved in a certain amount of methanol: chloroform (3:1) mixed solvent as oil phase, paeoniflorin is dissolved in a certain amount of glycerol aqueous solution to be water phase, oil phase: water phase is 3 ...

Embodiment 3

[0041] Example 3 Preparation of paeoniflorin alcohol plastids containing volatile oil

[0042] A kind of paeoniflorin alcohol plastid body containing volatile oil of Coleus vulgaris, comprising the following raw materials: 0.05% (w / v) paeoniflorin, 6% (w / v) soybean lecithin S80, 1% (w / v) cholesterol, 5% (w / v) % (v / v) glycerol, 0.5% (v / v) volatile oil of Thornweed.

[0043] The preparation of the paeoniflorin alcohol plastid body containing the volatile oil of Radix vulgaris comprises the following steps:

[0044] (1) First, mix the whole dried Radix vulgaris with water in a mass ratio of 1:12, soak for 12 hours, conduct steam distillation at 200°C, and extract the volatile oil from Radix Radix et Rhizoma after 10 hours.

[0045] (2) Soybean lecithin S80 and cholesterol are dissolved in a certain amount of methanol: chloroform (3:1) mixed solvent as oil phase, paeoniflorin is dissolved in a certain amount of glycerol aqueous solution to be water phase, oil phase: water phase is ...

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Abstract

The invention discloses a paeoniflorin ethosome, which contains 0.05-0.3% (w / v) of paeoniflorin, 2-6% (w / v) of soybean lecithin, 0.05-1% (w / v) of cholesterol, 5-40% (w / v) of low chain alcohol, and thebalance of water. The invention further discloses a paeoniflorin ethosome-containing pharmaceutical preparation for treating rheumatoid arthritis. According to the present invention, the paeoniflorinethosome can significantly increase the transdermal absorption of paeoniflorin, promote the retention of paeoniflorin at the treatment site, and control the transdermal absorption of paeoniflorin ata relatively constant rate so as to prolong the effect of the drug and provide good social and economic benefits.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a paeoniflorin alcohol plastid and a preparation method and application thereof. Background technique [0002] Rheumatoid arthritis is a chronic systemic autoimmune disease. It is mainly characterized by joint synovitis, symmetrical and destructive joint lesions. The disease progresses gradually, eventually leading to joint dysfunction. Currently, antirheumatic drugs that improve symptoms and slow disease progression are the main treatments for rheumatoid arthritis. However, its toxic and side effects are relatively large, and the biological preparations for certain cytokines are expensive, resulting in poor patient compliance with long-term use, which is not conducive to disease control. Therefore, it is imperative to design an anti-rheumatic drug with a good cost-effectiveness. [0003] Paeoniflorin is an effective part extracted from the traditional Chinese medicine Radix ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/7048A61K47/28A61K47/44A61K47/10A61P19/02A61P29/00A61P17/02
CPCA61K31/7048A61K9/1271A61K47/10A61K47/28A61K47/44
Inventor 冯年平张恺张永太黎哲
Owner SHANGHAI UNIV OF T C M
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