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Artemisia rupestris L. nasal spray with antiviral activity

An antiviral activity and spray technology, which can be applied to antiviral agents, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of low absorption and utilization, and achieve accurate dosage, The effect of improving bioavailability and good spray characteristics

Pending Publication Date: 2020-06-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is based on the current state of the prior art, in order to overcome the problem of low oral absorption and availability of the antiviral active ingredients of Artemisia annua in the prior art, and provide a nasal spray with high bioavailability for the effective part of Artemisia annua agent

Method used

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  • Artemisia rupestris L. nasal spray with antiviral activity
  • Artemisia rupestris L. nasal spray with antiviral activity
  • Artemisia rupestris L. nasal spray with antiviral activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Weigh 0.2g of Artemisia annua extract in each portion, and use different concentrations of ethanol and NaHCO 3 solution, Tween-80 solution and the combined use of mixed solvents, prepare a Artemisia nasal spray solution according to the proportion shown in Table 3 respectively, and observe the drug dissolution situation;

[0037] Table 3 The prescription composition of different solubilization methods of Artemisia nasal spray

[0038]

[0039]

[0040] Continued Table 3

[0041]

[0042] The dissolution observation results of prescriptions 1-14 shown in the above table 3 show that the Artemisia annua extract is dissolved in a certain concentration range of NaHCO 3 It can be completely dissolved in the dissolution of Tween 80, and the solubility of the Artemisia annua extract can also be increased by using a joint method.

Embodiment 2

[0044] Prepare 0.1%, 0.2%, 0.3%, 0.5% w / w Carbomer 940 Nasal Spray and 0.15%, 0.2%, 0.25%, 0.5% w / w Carbomer 971P nasal spray, inspect its pH and viscosity, and spray out droplets with a nebulizer, inspect the particle size and adhesion degree, and evaluate the possibility of forming preparations; the results show that each Carbomer 940 preparation is a yellow solution, and the Carbomer 971P preparation is yellow solution. It is a yellow clear solution. 0.3%, 0.5% w / w Carbomer 940 preparations and 0.25%, 0.5% Carbomer 971P preparations have high viscosity and low pH. When the mist is sprayed by the nebulizer, it will be clogged, and the ideal nasal cavity cannot be formed. Preparations: 0.1%, 0.2% Carbomer 940 preparations and 0.15%, 0.2% Carbomer 971P preparations have moderate viscosity, pH is more suitable for nasal administration, and can be sprayed out by sprayer.

Embodiment 3

[0046] According to the prescription shown in Table 4, prepare different models of an Artemisia nasal spray containing poloxamer;

[0047] A Artemisia nasal spray prescription (w / w%) of different adhesive pharmaceutical excipients of table 4

[0048]

[0049] Dissolve the hydrophilic material in the prescription 15-19 in an appropriate amount of deionized water, heat to 100°C under magnetic stirring to disperse evenly, and then place it in a refrigerator at 4°C to completely cool (more than 24h) to obtain a clear solution. In addition, the drug solution and the rest of the excipients were dissolved in deionized water, the two liquids were mixed and dissolved to the full amount, and the temperature sensitivity and spray characteristics of each preparation were investigated. The results showed that with the increase of the amount of poloxamer, the nebulized solution It has certain temperature sensitivity characteristics, but it also affects the size of atomized droplets and t...

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, and in particular relates to a traditional Chinese medicine nasal spray preparation containing an extract of Artemisia rupestris L. and a preparation method thereof. The nasal spray preparation containing the extract of Artemisia rupestris L. is a new traditional Chinese medicine spray preparation administered through thenasal cavity prepared by taking 50% ethanol extract of Xinjiang Artemisia annua L. as an antiviral active component, adopting a unique solubilization method, and adding a hydrophilic medicinal polymer adjuvant with mucous membrane adhesion ability. After animal experiments, the results confirmed that the nasal spray preparation has high bioavailability, convenient administration and strong antiviral treatment effect; and the nasal spray preparation is non-irritating to the administration site, has good compliance, has good clinical transformation potential and broad market prospects, and hastheoretical, economic and social significance for the development of antiviral traditional Chinese medicine preparations.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and specifically relates to a new dosage form of a nasal drug-an Artemisia nasal spray with antiviral activity, and the nasal spray is an Artemisia annua with mucoadhesive ability The aqueous solution of the extract is in a liquid state under normal conditions, and can be quickly distributed and adhered to the surface of the nasal mucosa after nasal administration, thereby delaying drug elimination and improving bioavailability. Background technique [0002] According to reports, viral infectious diseases are still one of the dangerous diseases affecting human health. Virus infection can cause various diseases and seriously endanger human health and life. According to incomplete statistics, about 60% of epidemic infectious diseases are caused by virus infection. So far, more than 3,000 kinds of viruses have been discovered in the world, and new viruses are still being discov...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K47/32A61K47/10A61K36/282A61P31/12
CPCA61K9/0043A61K47/32A61K47/10A61K36/282A61P31/12
Inventor 沙先谊韩小利何文秀
Owner FUDAN UNIV
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