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Darunavir inhaled dry powder pharmaceutical composition and preparation method thereof

A technology of darunavir and its composition, which is applied in the field of preparation of inhalation dry powder pharmaceutical composition, which can solve the problems of increasing the risk of powder agglomeration or agglomeration, low solubility of darunavir, and large amount of dissolving solvent used

Pending Publication Date: 2020-05-29
JIANGSU ALICORN PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Darunavir itself has low solubility and severe side effects. The original oral formulation was made into glycolate, which greatly improved its solubility and improved bioavailability. However, the daily dosage of the oral formulation was 800 mg, which still Become a technical bottleneck in the development of other routes of drug delivery, especially through the respiratory tract
Chinese patent CN103509031 (applicant: Shanghai Desano, publication date: 2014-1-15) discloses the process of preparing darunavir with water as the anti-solvent. In order to lower the temperature, the use of the dissolving solvent in Example 2 The amount is very large, resulting in a large energy consumption in solvent recovery, which is not economical and environmentally friendly
Patent CN101820865A (applicant: Taibotek, publication date: 2010-1-25) provides an anti-HIV tablet formulation containing darunavir, which mentions that the available particle size can be obtained by rolling drying instead of static drying Smaller darunavir, Dv10 (Dv10 refers to 10% of particles) decreased from 85 microns to about 35 microns, but this will reduce the fluidity of dry particles and increase the risk of powder agglomeration or caking

Method used

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  • Darunavir inhaled dry powder pharmaceutical composition and preparation method thereof
  • Darunavir inhaled dry powder pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Preparation of amorphous darunavir

[0037] Dissolve darunavir in 50% ethanol solution, the solid content of the solution is 3% (w / v), spray dry according to the following process parameters, collect the obtained particles, and calculate the yield,

[0038] Inlet temperature: 120°C;

[0039] Spray flow: 6ml / min;

[0040] Atomization pressure: 180KPa;

[0041] Spray gas flow rate: 0.6 m 3 / min.

Embodiment 2

[0042] Example 2: Preparation of amorphous darunavir granules

[0043] Weigh Darunavir: Mannitol: Leucine in a ratio of 7:2:1 (w / w / w) and dissolve in 50% ethanol solution, the solid content of the solution is 3% (w / v), according to the implementation The process parameters in Example 1 were spray-dried, and the resulting particles were collected.

Embodiment 3

[0044] Example 3: Preparation of amorphous darunavir granules

[0045] According to the ratio of 7:2:1 (w / w / w), darunavir: lactose: leucine was dissolved in 50% ethanol solution, and the solid content of the solution was 3% (w / v), according to the example The process parameters in 1 are spray-dried, and the resulting particles are collected.

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Abstract

The present invention belongs to the technical field of medicines and discloses a darunavir inhaled dry powder pharmaceutical composition, and a preparation method and medical uses of the composition.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a method for preparing a dry powder pharmaceutical composition for inhalation. The dry powder pharmaceutical composition contains darunavir as an active ingredient and is shear-mixed with pharmaceutically acceptable excipients to form a pharmaceutical composition. Targeted pulmonary administration can be via a dry powder inhalation device. 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 SA...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/34A61K47/10A61K47/18A61K47/26A61K47/40A61P31/14A61P31/16A61P31/18A61P31/22
CPCA61K9/0075A61K31/34A61K47/10A61K47/26A61K47/183A61K47/40A61P31/18A61P31/16A61P31/14A61P31/22
Inventor 宋敏舒欣高超陈磊陆平波陶觉泉
Owner JIANGSU ALICORN PHARMATECH CO LTD
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