Nasal administration preparation and application thereof

A nasal administration preparation and preparation technology, which is applied in the field of chemical pharmacy, can solve the problems of low oral effect, achieve the effects of accurate dosage, easy use, and increased transport speed

Inactive Publication Date: 2011-08-31
杭州天龙药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, it provides a non-injection route for oligonucleotide drugs, because the oral effect of oligonucleotide drugs is low, and they are only l

Method used

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  • Nasal administration preparation and application thereof
  • Nasal administration preparation and application thereof
  • Nasal administration preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Embodiment 1 (nasal drops / nasal spray)

[0070] FT 2.0g, paraben complex ester (respectively weigh an appropriate amount of paraben ethyl and propyl paraben, and mix the two at a ratio of 1:1 to obtain a paraben complex ester, the same below) 0.15g, Propylene glycol 3.5g, PBS (pH7.4) buffer (that is, phosphate buffer (pH7.4): take 1.36g of potassium dihydrogen phosphate, add 0.1mol / L sodium hydroxide solution 79ml, dilute to 200ml with water, that is obtained. The same below) was added to 100ml.

[0071] Preparation method: Weigh 2.0g FT and dissolve it with 1.7ml PBS (pH7.4) buffer solution, pour it into the preparation tank, add 3.5g propylene glycol, stir, let it stand, filter, and then use buffer solution PBS (pH7.4) in the filtrate ) buffer solution to a final volume of 100ml, and finally add paraben complex ester, stir evenly, let stand, filter, potting, and sterilize to obtain.

Embodiment 2

[0072] Embodiment 2 (nasal drops / nasal spray)

[0073] Add 2.0 g of FT, 0.2 g of ethylparaben, 2.0 g of propylene glycol, 2.50 g of hydroxypropyl β-cyclodextrin, and add PBS (pH7.4) buffer solution to 100 ml.

[0074] Weigh 2.0g of FT and 2.5g of hydroxypropyl β-cyclodextrin, dissolve them with 1.7ml and 4.17ml of PBS (pH7.4) buffer solution respectively, inject them into the preparation tank, add 2.0g of propylene glycol, stir, stand still, and filter. Then add PBS (pH7.4) buffer solution to the filtrate to a final volume of 100ml, and finally add ethylparaben, stir well, let stand, filter, pot, and sterilize to obtain.

Embodiment 3

[0075] Embodiment 3 (nasal drops / nasal spray)

[0076] Add FT 2.0g, methyl paraben 0.25g, glycerin 4.2g, and normal saline to 100ml.

[0077]Weigh 2.0g of FT and dissolve it with 1.85ml of normal saline, inject it into the preparation tank, then add 4.2g of glycerin, stir, let stand, filter, add the filtrate to the final volume of 100ml with normal saline, finally add methylparaben, stir Mix evenly, let stand, filter, pot, sterilize, and you get it.

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PUM

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Abstract

The invention provides a nasal administration preparation which takes an antisense oligonucleotide medicament flutide (of which the sequence is 5'-CCTTGTTTCTACT-3') as a main component and is used for preventing and treating H1N1, H3N2 and H5N1 influenza virus infection, belonging to the field of chemical pharmacy. The nasal administration preparation takes the flutide as an effective component and also contains a proper amount of preservatives, buffer solution and medicinal auxiliary materials, and the pH value of the preparation is 7-8. The preservatives are reagents which can not influencethe physicochemical properties of medicaments and have no harm to human bodies, no irritation and no special odor under the inhibitory concentration. Common preservatives comprise methyl paraben, ethyl paraben, propyl paraben, butyl paraben, ethyl hydroxy benzoate, potassium sorbate, benzoic acid, benzalkonium bromide, chlorhexidine acetate, o-phenyl phenol, eucalyptus oil, cassia oil, peppermintoil and the like. The flutide nasal administration preparation has no irritation and very low toxicity, and is a medicament which has a high action speed and a lung targeting function when used for treating influenza.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and is a nasal administration preparation mainly composed of an antisense oligonucleotide drug influenza Tide (its sequence is: 5'-CCTTGTTTCTACT-3'), which is used for H1N1, H3N2 and H5N1 Prevention and treatment of influenza virus infection. Background technique [0002] Influenza is an acute, viral respiratory infectious disease that seriously endangers human life and health. There are large-scale outbreaks and epidemics in winter and spring every year, and each epidemic will cause 3 to 5 million severe influenza cases worldwide. Influenza virus has the characteristics of fast transmission, rapid mutation, and great harm. It is difficult to prevent vaccines. There are few types of anti-influenza drugs available, and they are particularly prone to drug resistance. According to WHO reports, for the main anti-influenza drug oseltamivir ( Drug-resistant mutant strains have appeared in many countri...

Claims

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Application Information

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IPC IPC(8): A61K31/711A61P31/16
Inventor 朱德领王升启郭锰金义光李淼鲁丹丹张玉林仲婕张金钟李剑波高婵
Owner 杭州天龙药业有限公司
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