Pharmaceutical composition for inhalation

A technology of composition and monohydrate, which is applied in the pharmaceutical composition for inhalation of remdesivir and the field of pharmaceutical composition for inhalation, can solve problems such as difficult process, increased production cost, and unfavorable drug production enterprises, and achieve particle Good stability and good powder fluidity

Pending Publication Date: 2022-03-04
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The 2020 edition of the Pharmacopoeia defines both acetonitrile and dioxyethane as the first class of solvents, the solvent residue limit of acetonitrile is 0.041%, and the solvent residue of dioxane is 0.038% (see "The Pharmacopoeia of the People's Republic of China" (2020 Edition) four volumes Page 0861); In addition, the film freeze-drying technology also requires a harsh freeze-drying condition of -100°C, which is very unfavorable to pharmaceutical manufacturers. Not only is the process difficult to achieve, but it also increases production costs
The above-mentioned technical defects have led to the fact that the remdesivir freeze-dried powder prepared by the film freeze-drying technology is not suitable for the remdesivir inhalation prepared by pharmaceutical manufacturers.
In addition, when the University of Texas at Austin studied the stability of the formulation, it only studied the stability of Redcivir in the formulation, and did not study the overall stability of the Redcivir dry powder formulation, and the overall stability of the formulation has a great impact on the stability of the formulation. It is very important for pharmaceutical preparations

Method used

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  • Pharmaceutical composition for inhalation
  • Pharmaceutical composition for inhalation
  • Pharmaceutical composition for inhalation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～16

[0118] Examples 1-16: Preparation of remdesivir dry powder inhalation.

[0119] First, weigh each material according to the prescription amount in Table 3; secondly, add magnesium stearate, calcium stearate or stearic acid to remdesivir and mix, jet mill (for example, the shear flow is nitrogen or RH% is lower than 20% of the air, the central ring pressure is 0.5-12bar, the Venturi pressure is 1-14bar, and the feed rate is 0.1-3g / min), and the drug-containing micropowder of different particle sizes (as a flow aid) is obtained. The magnesium stearate and other ingredients in the product have almost no effect on the particle size measurement results of remdesivir, so the particle size measurement results of the drug-containing micropowder can still reflect the particle size of the active ingredient remdesivir to a certain extent) (preferably Subsequently, the micropowder is subjected to aging treatment, for example, at a temperature of 5 to 88°C and an environment of 10% to 95% ...

Embodiment 17～20

[0127] Examples 17-20: Preparation of remdesivir dry powder inhalation.

[0128] First, weigh each material according to the prescription quantity in Table 5; second, refer to the process conditions in Examples 1-16, add magnesium stearate to remdesivir and mix, and after jet milling, obtain different particle sizes Drug-containing micropowder; finally, the pre-screened lactose and drug-containing micropowder are placed in a solid mixing device for physical mixing to obtain the pharmaceutical compositions for inhalation of Examples 17 to 20.

[0129] Table 4 lists the D of the drug-containing micropowder of each embodiment through particle size analysis-laser diffraction method measurement. 10 、D 50 and D 90 Particle size, the prescription composition of the pharmaceutical composition of each embodiment is listed in table 5.

[0130] Table 4. Particle size distribution of the medicinal ingredients of Examples 17 to 20

[0131]

[0132] Table 5. The prescription composit...

Embodiment 21～22

[0134] Examples 21-22: Preparation of remdesivir dry powder inhalation.

[0135] First, weigh each material according to the prescription quantity in Table 7; second, refer to the process conditions in Examples 1-16, add magnesium stearate to remdesivir and mix, and after jet milling, obtain different particle sizes Drug-containing micropowder; finally, the pre-screened lactose and drug-containing micropowder are placed in a solid mixing device for physical mixing to obtain the pharmaceutical compositions for inhalation of Examples 21 to 22.

[0136] Table 6 lists the D of the drug-containing micropowder of each embodiment through particle size analysis-laser diffraction method measurement. 10 、D 50 and D 90 Particle size, the prescription composition of the pharmaceutical composition of each embodiment is listed in table 7.

[0137] Table 6. Particle size distribution of the medicinal ingredients of Examples 21 to 22

[0138]

[0139] Table 7. The prescription composit...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition for inhalation. Specifically, the pharmaceutical composition for inhalation comprises 1 wt%-70 wt% of a pharmaceutical active ingredient and 30 wt%-99 wt% of a pharmaceutically acceptable carrier, the pharmaceutical active ingredient is ridecevir or a pharmaceutically acceptable salt thereof, and the carrier is selected from one or more of sugars and sugar alcohols, amino acids, lipids, inorganic salts and polymers. The pharmaceutical composition for inhalation disclosed by the invention has the characteristics of good particle stability, good powder fluidity, no agglomeration and the like, has remarkable advantages compared with an existing ridecevir preparation, and is suitable for clinical use.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a pharmaceutical composition for inhalation, in particular to a drug against Marburg virus, Ebola virus, Nipah virus, respiratory syncytial virus, hepatitis C virus, human immunodeficiency virus, 2019 novel A pharmaceutical composition for inhalation containing remdesivir as an active ingredient for infections such as coronaviruses. Background technique [0002] Remdesivir is a nucleoside analog with a broad-spectrum antiviral mechanism of action. In particular, it has been reported that it can target Marburg virus (Marburg virus, MV), Ebola virus (Ebola virus, EV) , Nipah virus (Nipah virus, NV), respiratory syncytial virus (Respiratory syncytial virus, RSV), hepatitis C virus (Hepatitis C virus, HCV), human immunodeficiency virus (Human immunodeficiency virus, HIV), new coronavirus (SARS -CoV-2) and other infections have certain medicinal effects. However, u...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/685A61K47/26A61P31/14
CPCA61K9/0075A61K31/685A61K47/26A61P31/14
Inventor 袁建栋余佳琪李明孙娟刘承阮晓颖缪浩黄仰青
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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