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H102 peptide nasal liposome-type spray

A nasal spray and spray technology, which is applied in the direction of non-active ingredients of polymer compounds, nervous system diseases, pharmaceutical formulations, etc., can solve the problems of poor mucous membrane penetration and unstable H102 peptide, and achieve less irritation and increase in vivo Stability, favorable therapeutic effect

Inactive Publication Date: 2015-03-18
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The H102 peptide nasal cavity liposome spray of the present invention can solve the problems that the H102 peptide is unstable in the body, easily cleared by nasal cilia, and poor in mucous membrane penetration

Method used

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  • H102 peptide nasal liposome-type spray
  • H102 peptide nasal liposome-type spray
  • H102 peptide nasal liposome-type spray

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Accurately weigh 30 g of hydrogenated soybean phosphatidylcholine (HSPC), 6 g of dipalmitoylphosphatidylcholine (DSPC), and 1 g of mPEG5000-DSPE in a 1000 mL round-bottomed flask, add 100 mL of chloroform to fully dissolve the phospholipid material, and then evaporate to A thin film of phospholipids formed on the bottom of the flask. In addition, accurately weigh 6g of H102 peptide, dissolve it in 50mL of phosphate buffer (pH 6.0) containing 0.2% human serum albumin, add it into the flask to fully dissolve the phospholipid film, continue to add phosphate buffer to 200mL, hydrate, shake , ultrasonication, and membrane passage to obtain the H102 peptide liposome suspension. Add 10% glucose as a freeze-dried scaffold, dissolve, filter, and subpackage into sterilized nasal spray bottles for freeze-drying; after freeze-drying, take out and add bottle caps with quantitative spray pumps, and store in airtight low temperature. Before use, add sterilized three-distilled water t...

Embodiment 2

[0037] Accurately weigh 25g of egg yolk lecithin, 6.25g of cholesterol, and 2.5g of mPEG2000-DSPE in a 1000mL round bottom flask, add chloroform to dissolve, and rotary evaporate to form a film. In addition, 2 g of H102 peptide was precisely weighed, dissolved in 50 mL of phosphate buffer solution (pH 6.5) containing 0.5% human serum albumin, added to the flask to fully dissolve the phospholipid film, continued to add 100 mL of phosphate buffer solution, hydrated, shaken, Ultrasound and membrane passage to obtain H102 peptide liposome suspension. Add 5% trehalose as a freeze-dried scaffold agent, dissolve, filter through a 0.22 μm microporous membrane, pack into sterilized nasal spray bottles and freeze-dry to obtain H102 peptide nasal cavity liposome freeze-dried powder, which is sealed and stored at low temperature . Before use, add sterilized three-distilled water to dissolve, and then administer by spraying.

[0038] The H102 peptide nasal cavity liposome prepared in thi...

Embodiment 3

[0041]Accurately weigh 40 g of egg yolk lecithin, 10 g of cholesterol, and 2 g of mPEG2000-DSPE in a round bottom flask, add chloroform to dissolve, and rotary evaporate to form a film. In addition, 1 g of H102 peptide was accurately weighed, dissolved in 100 mL of phosphate buffer (pH 6.5) containing 0.1% human serum albumin, added to the flask to fully dissolve the phospholipid film, continued to add an appropriate amount of phosphate buffer, hydrated, oscillated, and ultrasonicated. 1. After being treated by a high-pressure homogenizer, pass through a membrane to obtain the H102 peptide liposome suspension. Add 10% trehalose to dissolve, filter, freeze-dry, take out, cover, and store in airtight low temperature. Before use, add sterilized three-distilled water to dissolve, and then administer by spraying.

[0042] The H102 peptide nasal cavity liposomes prepared in this example had an average particle size of 147.9 nm and an encapsulation efficiency of 71%; after freeze-dr...

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Abstract

The invention relates to the field of medicine preparations, and particularly relates to a nasal liposome-type spray taking H102 peptide as a main medicine, and a preparation method thereof. The preparation disclosed by the invention is composed of H102 peptide, phospholipid auxiliary materials, an anti-adsorbent and a freeze-drying stent. A preparation process for the preparation comprises the steps of preparing liposomes by a film dispersion method, adjusting a particle size and carrying out freeze drying. The preparation disclosed by the invention is in the form of solid powder, and administrated in the form of spray after being dissolved by adding sterilization tri-distilled water before application. The preparation disclosed by the invention is mainly used for treating Alzheimer disease, improving the dysmnesia of patients with Alzheimer disease, and alleviating pathological symptoms.

Description

technical field [0001] The invention belongs to the field of preparations and relates to an H102 peptide nasal cavity liposome spray. In particular, it relates to an H102 peptide nasal cavity liposome spray for treating Alzheimer's disease and a preparation method thereof. Background technique [0002] H102 peptide is a synthetic β-sheet blocking peptide. In vitro studies have confirmed that H102 peptide has the ability to stabilize the spatial structure of β-amyloid peptide (Aβ), inhibit the formation of β-sheets, and decompose the formed Aβ fibers. It can significantly improve the survival rate of nerve cells. After intracerebroventricular injection of H102 peptide drug solution, it can significantly improve the spatial memory impairment of APP transgenic mice and prevent the formation of Aβ amyloid plaques in the brain, showing the potential to treat Alzheimer's disease (Alzheimer's disease, AD). The research has applied for a Chinese invention patent (application numbe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/72A61K9/107A61K47/34A61K47/42A61P25/28
Inventor 张奇志邵夏炎谭远贞郑晓瑶蒋新国徐淑梅
Owner FUDAN UNIV
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