Nasal spray with cholinesterase inhibitors XQ528

A nasal spray, cholinesterase technology, applied in aerosol delivery, non-active components of polymer compounds, nervous system diseases, etc., can solve problems such as instability of XQ528, improve spatial memory impairment, and achieve good nasal absorption. , the effect of raising the level

Inactive Publication Date: 2016-02-10
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, practice shows that the XQ528 is unstable, and it is easily hydrolyzed into mebutamol and aniline under conditions of pH>6, heating or the presence of enzymes, and is ineffective when taken orally.

Method used

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  • Nasal spray with cholinesterase inhibitors XQ528
  • Nasal spray with cholinesterase inhibitors XQ528
  • Nasal spray with cholinesterase inhibitors XQ528

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Prepare the XQ528 nasal cavity solution with cyclodextrin as a stabilizer according to Table 1, and fill it in a nasal spray device, with a volume of 3-5 ml per bottle.

[0040] Table 1XQ528 Nasal Solution Spray Prescription (w / v%)

[0041]

[0042]

[0043] Table 1 (continued table) XQ528 nasal cavity solution type spray prescription (w / v%)

[0044]

[0045] (1) The preparation process is as follows: take about 60% of the buffer solution of the prescription amount in the preparation container, add bioadhesive agent to make it fully swell until completely dissolved; add bacteriostatic agent, isotonic regulator, metal ion chelating agent and stir Dissolve; add cyclodextrin in stages, stir to dissolve, then add XQ528, stir for 1-2 hours, add buffer to the full amount after complete dissolution, and mix well. After the pH and content are qualified, the liquid medicine is filtered through a 0.45 μm microporous membrane until it is clear, and then sterilized by fil...

Embodiment 2

[0049] Prepare XQ528 nasal cavity solution with polyethylene glycol (PEG) as a stabilizer according to Table 2, and fill it in a nasal spray device, and the amount of each bottle is 3-5 ml.

[0050] Table 2XQ528 nasal cavity solution type spray prescription (w / v%)

[0051]

[0052] (1) The preparation process is as follows: same as Example 1, except that cyclodextrin is replaced with PEG.

[0053] (2) Thermal stability investigation: The thermal stability of the formulation obtained in Example 2 was investigated by the same method as in Example 1. As a result, after the pure XQ528 solution was placed at 60°C for 6 days, the remaining dose was only 30.79±3.05% of the initial dose. After adding PEG as a stabilizer, the stability of the solution was significantly improved, and the remaining dose of XQ528 after 6 days was the initial dose. 40% to 64% of that. Figure 4 is the percentage-time curve of the remaining drug dose of prescriptions 14, 16 and 18.

Embodiment 3

[0055] Prepare the ion-sensitive nasal cavity instant gel according to Table 3, and fill it in a nasal spray device, and the volume of each bottle is 3-5ml.

[0056] Table 3 Prescription (w / v%) of ion-sensitive nasal cavity instant gel spray

[0057]

[0058] Table 3 (continued table) prescription (w / v%) of ion-sensitive nasal cavity instant gel spray

[0059]

[0060]

[0061] (1) The preparation process is as follows: take triple-distilled water with about 60% of the prescription amount, adjust the pH to about 5.5 with 0.1N HCl, add a hydrophilic gel material, and leave it at room temperature or heat (depending on the nature of the material) to make it Fully swell until completely dissolved; add bacteriostatic agent and isotonic regulator and stir to dissolve; add cyclodextrin and XQ528, stir until a clear solution is obtained, adjust the pH to 3.8-5.5 with 0.1N HCl, and finally add triple distilled water to the full amount, Mix well. After the pH and content are ...

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Abstract

The invention relates to the field of medicine preparations, in particular to novel nasal spray with cholinesterase inhibitors XQ528. The novel nasal spray which is a preparation comprises the cholinesterase inhibitors XQ528, stabilizers and other pharmaceutically effective excipients, can be in an aqueous solution form or an in-situ gel form and can be administered in a spray mode. The novel nasal spray has the advantages that the stability of the cholinesterase inhibitors XQ528 can be improved, hydrolysis of the cholinesterase inhibitors XQ528 can be reduced, the nasal retention time of medicines can be prolonged, and nasal absorption of the medicines can be promoted; the novel nasal spray is mainly used for treating Alzheimer's diseases, improving memory impairment of patients suffering from the Alzheimer's diseases and relieving pathogenic symptoms.

Description

technical field [0001] The invention belongs to the field of western medicine preparations and relates to a nasal spray of a novel cholinesterase inhibitor XQ528 for treating Alzheimer's disease. Background technique [0002] Alzheimer's disease (AD), the most common type of senile dementia, is a progressive and fatal neurodegenerative disease. The clinical manifestations are deteriorating cognitive and memory functions, progressive decline in the ability of daily living, accompanied by various neuropsychiatric symptoms and behavioral disturbances. With the intensification of population aging process, the incidence of such diseases is increasing day by day. According to incomplete statistics, the number of AD patients in my country has exceeded 5 million at present, and it is estimated that by 2050, AD patients will reach 25 million. AD has become a serious threat to human health and quality of life, and is an increasingly serious public health problem. [0003] The patho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K9/06A61K31/55A61K47/40A61K47/34A61K47/18A61P25/28
Inventor 张奇志查媛万旭钱勇仇缀百谢琼蒋新国
Owner FUDAN UNIV
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