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Huperzine A binary ethosome thermosensitive gel nasal delivery preparation and preparation method thereof

A temperature sensitive gel nasal cavity, Huperzine A technology, applied in the directions of pharmaceutical formulation, liquid delivery, drug combination, etc. High bioavailability, avoids first-pass effect, overcomes the effect of greater mobility

Inactive Publication Date: 2021-02-26
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although glycolosomes are excellent carriers for nasal administration, their viscosity is low. Due to the mechanism of nasal cilia swinging, the retention time of glycolosomes in the nasal cavity is short, which is not conducive to the transport of drugs from the nose to the brain.

Method used

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  • Huperzine A binary ethosome thermosensitive gel nasal delivery preparation and preparation method thereof
  • Huperzine A binary ethosome thermosensitive gel nasal delivery preparation and preparation method thereof
  • Huperzine A binary ethosome thermosensitive gel nasal delivery preparation and preparation method thereof

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Effect test

Embodiment 1

[0021]1. Formulation composition:

[0022]Huperzine A glycol plastids:

[0023]Huperzine A: 15mg

[0024]Lecithin: 540mg

[0025]Tween-80: 45mg

[0026]Absolute ethanol: 3.375mL

[0027]Propylene glycol: 3.375mL

[0028]Purified water: 8.250mL

[0029]The total solution is 15 mL.

[0030]Huperzine A Glycol Body Temperature Sensitive Gel:

[0031]P-407: 1380mg

[0032]P-188: 300mg

[0033]Purified water: 3mL

[0034]Huperzine A glycol plastid: 3mL

[0035]The total solution is 6mL.

[0036]2. Preparation method:

[0037](1) Preparation method of huperzine methyl glycol plastids:

[0038]Injection method: accurately weigh the formula amount of Huperzine A, soybean lecithin, Tween-80, measure a certain proportion of the glycol phase (ethanol: propylene glycol), place it in an Erlenmeyer flask, and stir until it is closed. completely dissolved. Under the condition of 30℃±0.5 and stirring speed of 700r / min, use a constant flow pump to slowly add purified water to the above-mentioned drug-containing glycol system solution at a rate of 1 m...

Embodiment 2

[0047]Huperzine A glycol plastids:

[0048]Huperzine A: 20mg

[0049]Lecithin: 600mg

[0050]Tween-80: 50mg

[0051]Absolute ethanol: 4.0mL

[0052]Propylene glycol: 3.0mL

[0053]Purified water: 8.0mL

[0054]A total of 15mL.

[0055]Huperzine A Glycol Body Temperature Sensitive Gel:

[0056]P-407: 1300mg

[0057]P-188: 320mg

[0058]Purified water: 3.0mL

[0059]Huperzine A glycol plastid: 3.0mL

[0060]A total of 6mL.

[0061]The preparation method is the same as in Example 1.

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Abstract

The invention relates to the field of medicinal preparations, and especially relates to a huperzine A binary ethosome thermosensitive gel nasal delivery preparation and a preparation method thereof. The preparation is formed by dispersing huperzine A binary ethosome into a thermosensitive gel matrix. An injection method is adopted to prepare the huperzine A binary ethosome; and then a cold dissolving method is adopted to prepare the huperzine A binary ethosome thermosensitive gel nasal delivery preparation. The preparation can achieve treatment effects through nasal delivery. The preparation is fast in absorption through nasal delivery, so that first pass effect can be avoided; and the preparation is high in bioavailability, small in body injury and convenient in using. The huperzine A binary ethosome is high in encapsulation efficiency, small in particle size and good in stability; and the huperzine A binary ethosome thermosensitive gel can overcome the disadvantages of inconvenient administration due to large mobility of the huperzine A binary ethosome, is higher in bioavailability and has a certain sustained release function.

Description

Technical field[0001]The invention relates to the field of pharmaceutical preparations, in particular to a nasal cavity administration preparation of a huperzine methyl glycol body temperature sensitive gel and a preparation method thereof.Background technique[0002]Huperzine A (Huperzine A, HupA) is a new type of effective monomer of lycopodium alkaloids isolated from the Chinese folk herbal medicine Melaleuca, its molecular formula is C15H18N2O, with a molecular weight of 242.3, is a white or off-white crystalline powder with high fat solubility and an oil-water partition coefficient logP=0.696. Huperzine A has a small molecular weight and strong blood-brain barrier permeability. As a highly effective and reversible acetylcholinesterase (AChE) inhibitor, it is useful for the treatment of Alzheimer's disease (Alzheimer's disease, AD) has a significant curative effect. The clinical data shows that the overall clinical safety of Huperzine A is good, there is no dose-limiting hepatotox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/4748A61K36/11A61K47/10A61K47/24A61P25/28
CPCA61K9/0043A61K9/06A61K31/4748A61K36/11A61K47/10A61K47/24A61P25/28
Inventor 黄庆德冯连晶
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE