H102 peptide nasal solution type spray for treatment of Alzheimer's disease

A nasal spray and Alzheimer's disease technology, applied in the field of H102 peptide nasal solution spray and its preparation, can solve the problems of poor mucous membrane penetration and instability of polypeptide drugs, so as to increase the dosage and benefit the prevention and treatment , the effect of convenient administration

Inactive Publication Date: 2015-01-14
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The H102 peptide nasal cavity solution spray of the present invention can solve the problems that current polypeptide drugs are unstable in the nasal cavity, easily cleared by nasal cilia, and poor in mucous membrane penetration;

Method used

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  • H102 peptide nasal solution type spray for treatment of Alzheimer's disease
  • H102 peptide nasal solution type spray for treatment of Alzheimer's disease
  • H102 peptide nasal solution type spray for treatment of Alzheimer's disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] According to Table 1, the H102 peptide nasal solution spray with chitosan as an absorption enhancer was prepared.

[0062] Table 1 Prescription of H102 peptide nasal solution spray (w / v %)

[0063]

[0064] ;

[0065] (1) The preparation process is as follows: take a buffer solution with about 70% of the prescription amount, add chitosan to make it fully swell until it is completely dissolved; then add antibacterial agent, stabilizer, osmotic pressure regulator, freeze-dried scaffold agent, Stir the anti-adsorbent and H102 peptide to fully dissolve, add buffer to the full amount; the liquid is sterilized by filtration through a 0.22 μm microporous membrane, and then packed into sterilized nasal spray bottles for freeze-drying; after freeze-drying, take out , Add a bottle cap with a quantitative spray pump, and store in an airtight low temperature. Before use, add sterilized three-distilled water to dissolve and then spray it for administration;

[0066] (2) Stab...

Embodiment 2

[0073] According to Table 3, the H102 peptide nasal cavity solution spray with cyclodextrin and Tween as absorption accelerators was prepared.

[0074] Table 3 bFGF nasal spray prescription (w / v %)

[0075]

[0076] ;

[0077] (1) The preparation process is as follows: take a buffer solution of about 70% of the prescription amount, add a bioadhesive agent to make it fully swell until it is completely dissolved; then add an absorption enhancer, a bacteriostat, a stabilizer, an osmotic pressure regulator, Dry the scaffolding agent, anti-adsorbent and H102 peptide, stir to fully dissolve, add buffer to the full amount; the drug solution is sterilized by filtering through a 0.22 μm microporous membrane, and then packed into sterilized nasal spray bottles to freeze-dry; freeze-dry After completion, take out and add the bottle cap with a quantitative spray pump, and store in airtight low temperature; before use, add sterilized three-distilled water to dissolve and then spray i...

Embodiment 3

[0080] SD rats were anesthetized, respectively nasal administration of H102 peptide solution, prescriptions 2, 3, 5 in the above-mentioned embodiment 1 and 7, 9, 10, 13 in the above-mentioned embodiment 2, and tail vein injection of the H102 peptide solution (the medicine was directly dissolved in buffer), wherein the nasal administration dose is 10 times that of intravenous injection; blood is taken from the tail vein at a predetermined time point, and plasma is obtained by centrifugation; after treatment, the concentration of H102 peptide is determined by LC-MS method, and the drug-time curve is calculated by trapezoidal method The area AUC 0-t , the results are shown in Table 4 (AUC values ​​in blood after nasal cavity and intravenous injection), the H102 peptide itself has poor ability to penetrate the mucosa, and the drug concentration in the blood was not measured after nasal cavity administration; however, after adding an absorption enhancer, it increased significantly ...

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Abstract

Belonging to the field of pharmaceutical preparations, the invention relates to an H102 peptide nasal solution type spray for treatment of Alzheimer's disease and a preparation method thereof. The nasal solution type spray contains H102 peptide, an absorption promoter, a stabilizer and other pharmaceutically effective excipients. The nasal solution type spray provided by the invention is made into freeze-dried powder form, can be dissolved into a solution before use and is then administrated by means of spray. Test results show that, the nasal solution type spray can obviously prolong the in vivo action time of H102 peptide and significantly increase the brain entry amount of the drug, and also can be used for treating Alzheimer's disease, improving the dysmnesia of patients with Alzheimer's disease, and relieving pathological symptoms.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an H102 peptide nasal cavity solution spray for treating Alzheimer's disease and a preparation method thereof. Background technique [0002] Alzheimer's disease (AD) is a progressive and fatal neurodegenerative disease, and it has become the fourth cause of death in the elderly after cardiovascular disease, cancer and stroke. With the aging of the population, the incidence of AD is increasing. It is estimated that by 2025, the number of AD patients will reach 34 million. AD has become a serious threat to human health and quality of life, and is an increasingly serious public health problem. [0003] It is now known that the β-sheet structure is one of the recurring secondary structures commonly found in proteins; studies have found that in the secondary structure of β-amyloid peptide (Aβ), the β-sheet The formation of layer structure is a necessary condition for the agg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K9/19A61K9/12A61K47/42A61K47/18A61K47/38A61K47/32A61P25/28
Inventor 张奇志邵夏炎谭远贞蒋新国徐淑梅
Owner FUDAN UNIV
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