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A kind of peramivir solution type inhalation agent 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, uniform distribution, and reduce the production of irrelevant substances

Active Publication Date: 2019-09-20
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; Peramivir has good stability under certain conditions; 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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  • A kind of peramivir solution type inhalation agent and preparation method thereof
  • A kind of peramivir solution type inhalation agent and preparation method thereof
  • A kind of peramivir solution type inhalation agent and preparation method thereof

Examples

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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 aseptically filled to obtain the product.

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

[0034] Determination method of related substances: HPLC: Agilent 1260 Infinity 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

...

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 showed that the equilibrium solubility of peramivir was pH-dependent, and its equilibrium solubility increased as the pH decreased. Combined with the requirements of preparation pH (3-8) and factors such as physiological stimulation, the pH of...

Embodiment 3

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

[0050] Regulate the solution pH value at 4.5, 4.5, 5.0, 5.5 with dilute hydrochloric acid (5% v / v) with prescription 1, 6 respectively, and the solution that is not adjusted with dilute hydrochloric acid, then the peramivir solution is placed in airtight 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]

[0054] 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 inhalation and a preparation method thereof, wherein the solution inhalation is made of peramivir, an osmotic pressure regulator, a pH regulator and water, wherein the concentration of peramivir Greater than 15 mg / ml, the concentration of the osmotic pressure regulator is less than 8 mg / ml, the pH value of the solution-type inhalation is 5.0-6.0, and no heat sterilization is used, and the osmotic pressure regulator is selected from sodium chloride or glucose . The solution-type inhalation has better stability and excellent lung-targeting effect, which significantly improves the effectiveness and safety of the drug.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a peramivir solution type inhalation agent 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. Peramivir is a cyclopentane derivative. The groups connected to the ring include hydrophilic carboxyl and guanidinium groups, as well as hydrophobic isopentyl and acetamido groups. Four groups with different polarities act on influenza virus NA respectively. Different active site regions in the structure. The carboxyl part forms a strong intermolecular interaction with the three arginine residues Arg118, Arg292, and Arg371 in the NA active site, the methyl part of the acetamido interacts with Trp 178 and Ile 222 in the hydrophobic pocket of NA, and the carbonyl oxygen in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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