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Nintedanib lyophilized liposome preparation for aerosol inhalation and preparing method thereof

A liposome preparation, nintedanib technology, applied in the field of pharmaceutical preparations, can solve problems such as low solubility in water, and achieve the effects of reducing microbial pollution and waste, good biocompatibility, and convenient use process

Inactive Publication Date: 2019-05-17
BEIJING INCREASE INNOVATIVE DRUG RESEARCH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention develops the drug into a freeze-dried liposome preparation to solve the problem of its low solubility in water. After freeze-drying, the liposome also increases the stability of the drug, and makes up for the gap in the current domestic market. A new safe and effective drug delivery preparation and drug delivery method of nintedanib

Method used

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  • Nintedanib lyophilized liposome preparation for aerosol inhalation and preparing method thereof
  • Nintedanib lyophilized liposome preparation for aerosol inhalation and preparing method thereof
  • Nintedanib lyophilized liposome preparation for aerosol inhalation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: Preparation of 200 nintedanib freeze-dried liposome preparations for nebulization inhalation

[0035]

[0036] Preparation:

[0037] (1) Add the prescribed amount of soybean lecithin and glyceryl monostearate into an appropriate amount of ethyl acetate and stir to dissolve under nitrogen gas, then add the prescribed amount of nintedanib and stir to dissolve. Dry under reduced pressure at °C for about 2 hours to remove ethyl acetate to obtain a film-like solid;

[0038] (2) Add 80% water for injection at 50°C to the film-like solid obtained in step (1), hydrate it with ultrasonic waves, add the prescribed amount of isotonic agent to it and stir to dissolve, and then adjust the system with a pH regulator pH value and dilute to 1L with water for injection;

[0039] (3) After the obtained sample is circulated twice under the homogenization pressure of 8000bar using a micro-fluidic homogenizer, it is filtered with a 0.22 μm polycarbonate membrane, aseptica...

Embodiment 2

[0040] Embodiment 2: Preparation of 200 nintedanib freeze-dried liposome preparations for nebulization inhalation

[0041]

[0042] Preparation:

[0043] (1) Add the prescribed amount of soybean lecithin and glyceryl monostearate into an appropriate amount of ethyl acetate and stir to dissolve under nitrogen gas, then add the prescribed amount of nintedanib and stir to dissolve. Dry under reduced pressure at °C for about 2 hours to remove ethyl acetate to obtain a film-like solid;

[0044] (2) Add 70% purified water at 60°C to the film-like solid obtained in step (1), hydrate it with ultrasound, then add the prescribed amount of isotonic agent to it and stir to dissolve, then adjust the system with a pH regulator pH value and dilute to 1L with purified water;

[0045] (3) After the obtained sample is circulated twice under the homogenization pressure of 8000bar using a micro-fluidic homogenizer, it is filtered with a 0.22 μm polycarbonate membrane, aseptically dispensed, ...

Embodiment 3

[0046] Embodiment 3: Preparation of 200 nintedanib freeze-dried liposome preparations for nebulization inhalation

[0047]

[0048] Preparation:

[0049] (1) Add the prescribed amount of soybean lecithin and glyceryl monostearate into an appropriate amount of ethyl acetate and stir to dissolve under nitrogen gas, then add the prescribed amount of nintedanib and stir to dissolve. Dry under reduced pressure at °C for about 2 hours to remove ethyl acetate to obtain a film-like solid;

[0050] (2) Add 60% water for injection at 35°C to the film-like solid obtained in step (1), hydrate it with ultrasound, then add the prescribed amount of isotonic agent to it and stir to dissolve, then adjust the system with a pH regulator pH value and dilute to 1L with water for injection;

[0051] (3) After the obtained sample is circulated twice under the homogenization pressure of 8000bar using a micro-fluidic homogenizer, it is filtered with a 0.22 μm polycarbonate membrane, aseptically d...

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Abstract

The invention discloses a nintedanib lyophilized liposome preparation for aerosol inhalation and for treating pulmonary fibrosis and a preparing method thereof. The single dosage of the lyophilized liposome preparation contains 10-80 mg of nintedanib or a salt thereof (according to the amount of free nintedanib), 25-250 mg of lipid, 100-1000 mg of phospholipid, and 20-150 mg of an osmotic agent. The prepared preparation has good stability and small particle size, and is suitable for aerosol administration. At the same time, the lyophilized liposome preparation has the advantages of high efficiency, low toxicity and high safety, and greatly reduces the hepatic and renal toxicity of medication of patients.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a nintedanib freeze-dried liposome preparation for nebulization inhalation and a preparation method thereof. Background technique [0002] Pulmonary fibrosis is a final severe pathological feature shared by a clinical class commonly referred to as interstitial lung disease. Interstitial lung diseases can include those that are primary in the lungs, those that occur with systemic rheumatism, those that are caused by treatment such as drugs or radiation, those that are associated with the environment or occupation, those that are associated with pulmonary angiogenesis, alveolar stasis diseases, and genetic diseases, etc. seven categories. The specific mechanism of pulmonary fibrosis caused by different etiologies is unclear, but the common feature is that the normal alveolar structure is damaged by inflammation caused by various reasons, that is, alveolitis; instead, col...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K9/19A61K9/127A61K47/02A61K31/496A61P11/00
Inventor 张保献胡杰
Owner BEIJING INCREASE INNOVATIVE DRUG RESEARCH CO LTD
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