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Peramivir dry powder inhalant and preparation method thereof

A dry powder inhaler and dry powder inhalation technology, applied in the field of medicine, can solve the problems of influence, influence on prescription, production and use, etc., and achieve the effects of reducing mortality, ensuring drug effectiveness, and excellent drug effect

Active Publication Date: 2020-07-03
GUANGZHOU NUCIEN PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2. Electrostatic force: The static electricity generated by the friction between particles in the production process of dry powder inhaler will affect its powder properties such as fluidity, dispersion and adhesion, thus affecting its formulation, production and use
4. Shear force between irregular particles
[0014] At present, carriers and / or excipients are usually added to dry powder inhalers to improve particle performance, but the inhalation effect of dry powder inhalers is affected by a variety of factors, and various factors affect each other, resulting in the change of one factor, the other Factor variables affect the reversal of outcomes, therefore, the development of a pharmaceutically acceptable dry powder inhaler still faces multiple technical challenges

Method used

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  • Peramivir dry powder inhalant and preparation method thereof
  • Peramivir dry powder inhalant and preparation method thereof
  • Peramivir dry powder inhalant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] 1. The prescription of peramivir spray-dried powder is as follows

[0045] Table 1 Peramivir spray-dried prescription

[0046]

[0047] Process conditions: The spray drying process parameters are the inlet air temperature 200°C, the outlet air temperature 100°C, and the speed: 400ml / h. The obtained powder was passed through a 180-mesh sieve. The experimental results are as follows:

[0048] Table 2 Peramivir spray-dried powder experimental results (n=3)

[0049]

[0050] The experimental results showed that after adding phospholipids and amino acids, the density and particle size of the spray-dried powder were reduced, but the fluidity became worse.

[0051] 2. Mix dry powder of spray-dried powder and mannitol, fully mix the peramivir spray-dried powder of the above composition 1 and mannitol (w / w): 1:1; 1:2; 1:5. The experimental results are as follows:

[0052] Table 3 Peramivir spray powder mixed with mannitol experimental results (n=3)

[0053]

[005...

Embodiment 2

[0061] 1. Prescription 1: peramivir micropowder dry powder, the peramivir raw material drug is pulverized by airflow, and the dry powder is prepared under the conditions of feed speed 130V, feed pressure 0.45MPa, and pulverization pressure 0.45MPa.

[0062] 2. Prescription 2: Mix the dry powder prepared above with lactose Inhalac 120 to make a mixed powder, and mix at a mass ratio of 1:1.

[0063] 3. Prescription 3: Mix the dry powder prepared above with lactose Inhalac 400 to make a mixed powder, and mix at a mass ratio of 1:1.

[0064] Lung deposition rate test

[0065] The powders of the above-mentioned prescriptions 1-3 are respectively packed into capsules, 20 mg per capsule. Cover the NGI instrument, put it on the throat, seal it tightly with a sealing film, turn on the pump first, then turn on the flow meter, turn on the TPK instrument, then connect the flow meter to the throat, and use the pen test device to install the empty capsule and make a hole. Connect to a flo...

Embodiment 3

[0081] The peramivir trihydrate raw material of 1.3kg is pulverized with a jet mill, and at a feed rate of 130V, a feed pressure of 0.45MPa, and a pulverization pressure of 0.40MPa to obtain a dry powder, and then the dry powder is packed into hypromellose Vegetarian capsules, each capsule filled with 20mg dry powder. The dry powder particle size D10 is 1.934um; D50 is 4.415um; D90 is 8.858um. Angle of repose 34.8 degrees, bulk density 0.25g / cm 3 , tap density 0.41g / cm 3 , Carr flow index 59.0.

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Abstract

The invention relates to a Peramivir dry powder inhalant, which is prepared from Peramivir or an acceptable salt or a hydrate thereof. A single-dosage preparation is 5-30 mg, the particle size D10 ofthe dry powder is 1.3-2.2 um, D50 is 3-6 um, and D90 is 6-13 um. The valence of influenza A viruses in the lungs of a mouse can be effectively lowered, the Peramivir dry powder inhalant has an obviousanti-virus function, can obviously prolong survival time and lowers a death rate, and the medicine effect function of the Peramivir dry powder inhalant is superior to the medicine effect function ofa Peramivir sodium chloride injection and Oseltamivir phosphate. The Peramivir dry powder inhalant has a specific lung targeting function, and the effectiveness and the safety of the medicine can be obviously improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a peramivir dry powder inhaler and a preparation method thereof. Background technique [0002] Peramivir, chemical name (-)-(1S,2S,3R,4R)-2-hydroxy-3-[(1S)-1-acetamido-2-ethyl]butyl-4-guanidine Cyclopentane-1-carboxylic acid is a cyclopentane derivative influenza virus neuraminidase (NA) inhibitor. [0003] Due to the low oral availability of peramivir, it is mainly made into parenteral preparations such as injections. Peramivir can play an anti-influenza effect by staying in the patient's respiratory organ tissue. Therefore, peramivir is made into The inhalant directly reaches the tissue lesions of the respiratory organs through the non-oral route, reducing potential adverse reactions to other tissues in the body. There are many dosage forms of inhalants, including dry powder inhalers, sprays, solution inhalers, etc. The applicant protected a peramivir solution inhaler in CN...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/14A61K31/196A61P31/16
CPCA61K9/14A61K9/0075A61K31/196A61P31/16A61M15/003A61M2202/064
Inventor 缪栋胡双华
Owner GUANGZHOU NUCIEN PHARM CO LTD
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