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Preparation method of pharmaceutical composition for inhalation and product thereof

A composition and drug technology, applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as difficult process implementation, increased production costs, and unfavorable drug manufacturers, and achieve Good particle stability, avoiding solvent residue problems, 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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  • Preparation method of pharmaceutical composition for inhalation and product thereof
  • Preparation method of pharmaceutical composition for inhalation and product thereof
  • Preparation method of pharmaceutical composition for inhalation and product thereof

Examples

Experimental program
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preparation example Construction

[0123] In the preparation method of the present invention, the equipment used in the solid mixing step can be either a low-shear mixer or a high-shear mixer.

[0124] In one embodiment of the invention, the low shear mixer may be mixer.

[0125] In another embodiment of the invention, the high shear mixer may be mixer.

[0126] In yet another embodiment of the invention, the high shear mixer may be mixer.

[0127] In some cases, the preparation method of the present invention may further include a jet pulverization step, which is used to pulverize the mixture of the pharmaceutically active ingredient and part of the pharmaceutically acceptable carrier (such as a glidant) to obtain a co-gas powder (or a powder containing medicine powder).

[0128] For example, when the pharmaceutically acceptable carrier is a combination of sugar and sugar alcohols (such as lactose monohydrate) and lipids (such as magnesium stearate), the jet milling step can make the pharmaceutical act...

Embodiment 1-16

[0154] Example 1-16: Preparation of remdesivir dry powder inhaler.

[0155] 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 Air with RH% below 20%, center ring pressure 0.5-12bar, eg 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 9.0, 10.0 or 12.0bar , the Venturi pressure is 1-14bar, such as 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 12.5, 13, 13.5 or 14bar, and the feed rate is 0.1-3g / min, such as 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, 1.1, 1.3, 1.5, 2.0, 2.5 or 3.0g / min), obtain drug-containing micropowders of different particle sizes (as The magnesium stearate and other components of the glidant have little effect on the particle size measurement of remdesivir, so the particle size measurement results of the drug-containing micropowder can still reflect the particle size of the ...

Embodiment 17-20

[0163] Example 17-20: Preparation of remdesivir dry powder inhaler.

[0164] First, weigh each material according to the prescription amount 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.

[0165] 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.

[0166] Table 4. Particle size distribution of the medicinal ingredients of Examples 17 to 20

[0167]

[0168] Table 5. The prescription composition of...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of a pharmaceutical composition for inhalation and a product thereof. Specifically, the preparation method provided by the invention comprises a solid mixing step for mixing the ridecevir or the pharmaceutical salt thereof with a pharmaceutically acceptable carrier. Preferably, the preparation method disclosed by the invention further comprises an air jet pulverization step, an aging step, a transportation and / or preservation step and the like. The pharmaceutical composition for inhalation prepared by the preparation method provided by the invention has the characteristics of good particle stability, good powder fluidity, no agglomeration and the like, has significant advantages compared with the existing ridecevir preparation, and is suitable for clinical use. In addition, the preparation method disclosed by the invention avoids the problem of solvent residue existing in a film freeze-drying method, and does not need ultralow-temperature harsh conditions in process.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a preparation method of a pharmaceutical composition for inhalation and a product thereof, in particular to a method for treating Marburg virus, Ebola virus, Nipah virus, respiratory syncytial virus, hepatitis C virus, human A preparation method and a product thereof for an inhalation pharmaceutical composition infected with immunodeficiency virus, 2019 novel coronavirus, etc., and containing remdesivir as a pharmaceutical active ingredient. 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 immunodeficien...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/14A61K47/26A61K47/12A61K31/685A61P31/14A61P31/18A61P31/20
CPCA61K9/0075A61K9/145A61K31/685A61P31/14A61P31/18A61P31/20
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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