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Lopinavir inhalation aerosol and preparation method thereof

The technology of lopinavir and aerosol is applied in the field of lopinavir inhalation aerosol and its preparation, and can solve the problems of poor systemic bioavailability, large dose of lopinavir, low self-solubility and the like, To achieve the effect of accurate dose, high local concentration and good lung deposition

Active Publication Date: 2020-06-12
JIANGSU ALICORN PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Lopinavir is easily soluble in methanol and ethanol, soluble in isopropanol, almost insoluble in water, poor in water solubility, good in fat solubility, high first-pass effect, and extremely poor systemic bioavailability. The high dosage (recommended daily dosage is 800mg), low self-solubility, and large side effects have become technical bottlenecks in the development of oral and injection routes of administration.

Method used

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  • Lopinavir inhalation aerosol and preparation method thereof
  • Lopinavir inhalation aerosol and preparation method thereof
  • Lopinavir inhalation aerosol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Micronization of lopinavir

[0031] Lopinavir is micronized in a jet mill, the pulverization pressure is 0.4~1.2Mpa, and the particle size of the obtained product is D 50 ≤3μm, D 90 ≤5μm.

Embodiment 2

[0033]

[0034] Preparation method: Slowly add the micronized active drug obtained in Example 1 to absolute ethanol and stir until a clear and transparent solution is formed, then add it into a pressure-resistant container; insert the valve in the pressure-resistant container, seal the valve, and fill it with propellant, that is, have to.

Embodiment 3

[0036]

[0037] Preparation method: Add the indicated active agent into absolute ethanol, slowly add the micronized active drug obtained in Example 1 and stir until a clear and transparent solution is formed, then add it into a pressure-resistant container; insert the valve in the pressure-resistant container, seal the valve, Propellant filling, that is.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and discloses a lopinavir inhalation aerosol and a preparation method thereof. The lopinavir inhalation aerosol is composed of lopinavir serving as an active ingredient, a propellant, a cosolvent, a surfactant and the like according to a certain ratio . The aerosol inhalant is administrated through the oral cavity and directly acts on thelung to achieve targeted administration. The inhalation preparation disclosed by the invention can target a focus, is accurate in dosage, takes effect rapidly, can quickly improve the pulmonary infection condition, is beneficial to improve the adaptability of an infected person, and avoids gastrointestinal tract absorption so as to reduce side effects on the gastrointestinal tracts.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to a lopinavir inhalation aerosol and a preparation method thereof. Background technique [0002] For 2019-nCoV, there is currently no specific antiviral drug in the world. It is mainly for symptomatic treatment of patients. There is no effective antiviral drug. In view of the current epidemic situation, it is necessary to quickly find suitable antiviral drugs and use them rationally. Timing is of great significance for treating infected people, controlling the spread of the epidemic, and reducing the fatality rate. [0003] The receptor binding pathway of 2019-nCoV virus and SARS coronavirus is similar, through the molecular mechanism of S-protein binding and interaction with human ACE2 receptor, and ACE2 exists in alveolar and small intestinal epithelial cells, and in arteriovenous epithelial cells of all organs It is expressed on the surface of arterial smooth m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/513A61K47/10A61K47/12A61K47/26A61P31/14A61P11/00
CPCA61K9/124A61K9/0073A61K31/513A61K47/10A61K47/12A61K47/26A61P31/14A61P11/00
Inventor 宋敏舒欣高超李莉周影
Owner JIANGSU ALICORN PHARMATECH CO LTD
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