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Jasminoidin or gardenia total iridoid glycoside liposome preparation

A technology for total iridoid glycosides and liposome preparations, applied in the field of pharmaceutical preparations, can solve problems such as poor ability to penetrate mucous membranes

Active Publication Date: 2012-01-11
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, geniposide and total iridoid glycosides of Gardenia jasminoides are easily soluble in water, and their ability to penetrate the mucosa is poor; if they are directly dropped or sprayed into the nasal cavity in the form of a solution, they are easily degraded by enzymes in the nasal cavity and Nasal cilia are cleared, therefore, it is necessary to develop a nasal administration preparation that can prolong the contact time of geniposide and total iridoid glycosides of geniposide and nasal mucosa, and improve the ability of drugs to penetrate the mucosa, thereby improving the geniposide and total iridoid glycosides. The concentration of total iridoid glycosides of Gardenia glycosides in the brain tissue, reducing the loss of geniposide and total iridoid glycosides of Gardenia

Method used

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  • Jasminoidin or gardenia total iridoid glycoside liposome preparation
  • Jasminoidin or gardenia total iridoid glycoside liposome preparation
  • Jasminoidin or gardenia total iridoid glycoside liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] The preparation of embodiment 1 gardenia total iridoid glycosides

[0078]Take 1 kg of gardenia coarse powder, add 6 times of water to decoct 3 times, each time for 30 minutes, filter, combine the decoction, concentrate to 1000 ml of thick paste (each 1 ml is equivalent to 1 g of medicinal materials), add 730 ml of 95% ethanol to contain Alcohol content 40%, stand for 24 hours, take the supernatant, recycle ethanol, concentrate to 500ml of thick cream with no alcohol smell (each 1ml is equivalent to 2g of medicinal materials), add 2700ml of 95% ethanol to alcohol content of 80%, stand for 24 hours, Filter, the filtrate is concentrated to a relative density of 1.05 to 1.10 (60° C.), and dried to obtain 130 g of dry cream. The content of total iridoid glycosides of geniposide is determined to be 55% by ultraviolet spectrophotometry, and the content of total iridoid glycosides of geniposide is determined by high-performance liquid phase. The glycoside content is 27.4%.

Embodiment 2

[0079] Embodiment 2 reverse evaporation method prepares geniposide liposome

[0080] Dissolve 50 mg of geniposide and 9 mg of sodium chloride in 10 ml of PBS (PH=7.0) buffer solution, and dissolve 160 mg of egg yolk phospholipid (EPC) and 40 mg of cholesterol in 30 ml of organic phase (chloroform:isopropanol=14:1 ), the two were mixed, and the water bath was sonicated for 8 minutes until a stable water / oil (W / O) emulsion was formed (the temperature of the water bath was controlled at 20 ° C), and then the organic solvent was evaporated in a rotary evaporator under reduced pressure, and the colloidal state was dropped Add 1-2ml of PBS (PH=7.0) buffer solution, hydrate, and continue to evaporate under reduced pressure for a short time to make a white liposome suspension. Add preservatives and fill in nasal cavity drug delivery devices.

Embodiment 3

[0081] Example 3 Preparation of total iridoid glycoside liposomes of Gardenia jasminoides by reverse evaporation method

[0082] Take total iridoid glycosides of gardenia jasmine glycosides 50mg and sodium chloride 9mg prepared in Example 1 and dissolve them in 10ml of PBS (PH=7.0) buffer solution, and take soybean lecithin (SPC) 100mg and cholesterol 50mg and dissolve them in 30ml of organic phase (Chloroform: isopropanol = 14:1), mix the two, and ultrasonicate in a water bath for 8 minutes to obtain a white emulsion. Evaporate the organic solvent in a water bath on a rotary evaporator (to make it into a gel), and add a small amount of PBS (PH=7.0) to buffer Solution, hydration, and continue to evaporate under reduced pressure for a short time to make a liposomal suspension. Add preservatives and fill in nasal cavity drug delivery devices.

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Abstract

The invention discloses a jasminoidin or gardenia total iridoid glycoside liposome preparation which comprises liposome formed by phospholipid and cholesterol, and asminoidin or gardenia total iridoid glycoside wrapped and loaded in the liposome, wherein the weight ratio of phospholipid to cholesterol is (3:1)-(7:1), preferably 5:1; the weight ratio of asminoidin or gardenia total iridoid glycoside to phospholipid is (1:2)-(1:8), preferably 1:4; and the phospholipid is selected from lecithin, soya lecithin, yolk phospholipid or phosphatidylcholine, preferably soya lecithin or yolk phospholipid. The preparation provided by the invention has the advantages that the contact time of the asminoidin or gardenia total iridoid glycoside and mucosa is prolonged. The liposome preparation can be prepared into a spraying agent after being loaded into a nasal suction apparatus, and is applied in a nasal delivery mode, so that the distribution of the asminoidin or gardenia total iridoid glycoside in brain tissues is effectively improved. The invention also discloses the application of the liposome preparation in preparation of medicaments for treating hypoxic ischemic brain damage diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to liposome preparations loaded with geniposide or gardenia total iridoid glycosides. Background technique [0002] Ischemic brain injury accounts for about 80% of cerebrovascular diseases, and refers to the degeneration, necrosis or loss of function of local brain tissue, including nerve cells, glial cells and contact fibers due to blood supply disorders. Once the cerebral artery is occluded, the brain tissue will not get enough blood perfusion, and ischemia and hypoxia will occur, and the physiological and pathological evolution process of ischemic cerebrovascular disease will begin, which will eventually lead to neuronal death and neurological dysfunction. defect. It is a clinical common disease, frequently-occurring disease, high mortality and disability rate, has become one of the three major fatal diseases recognized in the world. [0003] In recent years, studies ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61K36/744A61K9/12A61K9/72A61P9/10
Inventor 杨明张海燕汪建民刘昊赵成城郑琴岳鹏飞芦乾
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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