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Peramivir solution type inhalant and preparation method thereof

An inhalant and solution-type technology, applied in the field of medicine, can solve problems such as poor stability, achieve good stability, reduce the production of irrelevant substances, and evenly distribute the effect

Active Publication Date: 2019-05-21
GUANGZHOU NUCIEN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Another document (“Study on the Stability of Peramivir API”, Gan Wei et al., Modern Drugs and Clinics, 2018) reported that the Peramivir API was stable within 48 hours at 100°C; In the case of peramivir, the stability of peramivir is good; peramivir has good stability in alkaline and neutral environments, but is unstable in acidic conditions, and the stability is worse as the pH value decreases

Method used

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  • Peramivir solution type inhalant and preparation method thereof
  • Peramivir solution type inhalant and preparation method thereof
  • Peramivir solution type inhalant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Inhalant Prescription

[0032] According to the prescription in Table 1, mix the peramivir raw material and auxiliary materials in the liquid preparation tank, add water for injection at 70-80°C to 1000ml, stir and dissolve, then cool the solution, and dilute the solution with dilute hydrochloric acid (5% v / v) The pH value is adjusted between 5.0 and 6.0, and then the peramivir solution is pre-filtered and then aseptically filtered, and it is obtained after aseptic filling.

[0033] Prescriptions 1-9 in Table 1 were respectively placed under airtight high temperature (60°C) and light (4500lx ± 500lx) conditions for 0 days, 5 days, 10 days, and 30 days to investigate the situation of related substances.

[0034] Determination method of related substances: HPLC: Agilent 1260Infinity USA; Chromatographic column: EclipsePlus C 18 (5μm, 4.6×250mm, Agilent, USA); mobile phase: gradient elution is as follows:

[0035] Table 1 Mobile phase gradient elution

[0036...

Embodiment 2

[0044] Embodiment 2: Experiment on the influence of different pH on the solubility of peramivir

[0045] Take by weighing excessive peramivir crude drug and add in the 25ml volumetric flask, be settled to scale with 0.7% saline, be placed in shaker shaking (25 ℃, 75rpm) after 24h, with dilute hydrochloric acid (5%, V / V) adjust the pH to 4, 4.5, 5.0, 5.5 respectively, continue to stand for 48h, filter with a 0.45 μm filter membrane, and the filtrate is diluted 250 times with deionized water, and the sample adopts the HPLC method in the peramivir standard to measure the peramivir content .

[0046] Table 4 The equilibrium solubility of peramivir in different pH physiological saline solutions

[0047]

[0048] The experimental results show that the equilibrium solubility of peramivir is pH-dependent, and its equilibrium solubility increases as the pH decreases. Combined with factors such as the requirement (3-8) of preparation pH and physiological stimulation, the pH of per...

Embodiment 3

[0049] Embodiment 3: Stability experiment of peramivir inhalation solution under different pH conditions

[0050] Adjust the pH value of the solution to 4.5, 4.5, 5.0, 5.5 with dilute hydrochloric acid (5% v / v) for prescription 1 and 6 respectively, and the solution that was not adjusted with dilute hydrochloric acid, and then place the peramivir solution in an airtight container Place it under the conditions of high temperature (60°C) and light (4500lx±500lx) for 0 day and 30 days to investigate the situation of related substances.

[0051] Related substance content (%) under different pH conditions of table 5

[0052]

[0053] The experimental results show that the peramivir inhalation solution is the most stable at a pH value of 5.5, and can still maintain good stability under high temperature conditions.

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Abstract

The invention relates to a peramivir solution type inhalant and a preparation method thereof. The solution type inhalant is prepared from peramivir, an osmotic pressure adjusting agent, a pH adjustingagent and water, the concentration of the peramivir is more than 15 mg / ml, the concentration of the osmotic pressure adjusting agent is less than 8 mg / ml, the pH of the solution type inhalant is 5.0-6.0, heating sterilizing is not adopted, and the osmotic pressure adjusting agent is selected from chlorine, sodium or glucose. The solution type inhalant has better stability and excellent lung targeting, which significantly improves the effectiveness and safety of medicines.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a peramivir solution type inhalation 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, a cyclopentane derivative, is a neuraminidase (NA) inhibitor of influenza-like viruses. Peramivir is Cyclopentane Derivatives, the group attached to the ring has a hydrophilic carboxyl and Guanidine , and hydrophobic Isopentyl and Acetamide base , 4 groups with different polarity act on flu virus Different in NA structure active site area. The carboxyl part forms a strong intermolecular interaction with the three arginine residues Arg118, Arg292, and Arg371 in the NA active site, and the methyl part of the acetamido interacts with Trp 178 and Ile 222 in the hydrophobic pocket of NA. Carbonyl Oxygen interacts with Arg152; the guanidin...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/08A61K47/26A61K47/02A61K31/196A61P31/16
CPCA61K47/02A61P31/16A61K31/196A61K9/08A61K9/0078A61K47/26
Inventor 张世喜冯玉欢缪栋
Owner GUANGZHOU NUCIEN PHARM CO LTD
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