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Preparation formula of methacholine chloride freeze-dried powder for inhalation and preparation method of preparation formula

A methacholine chloride and freeze-drying technology, applied in the field of medicine, can solve problems such as not easy to absorb moisture and agglomerate, unsolved preparation production and sterility assurance, and high microbial level

Pending Publication Date: 2021-09-10
上海轩耘生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Products that have been marketed abroad are non-sterile products due to their earlier launch time. In the process of clinical use, they must be reconstituted, sterilized and filtered with a filter membrane before being used. Clinical use is inconvenient and there is a risk of high microbial levels.
[0003] Chinese patent CN110950767A provides a new crystal form of methacholine chloride crude drug, which is not easy to absorb moisture and agglomerate, has uniform particle size and improved stability, which is beneficial to the production of preparations, but it is still produced by powder packaging, without Solve the problems of sterility assurance and long reconstitution time
[0004] Chinese patent CN111635327A provides a kind of amorphous crystal form of methacholine chloride raw material drug, also in order to improve the humidity stability of raw material drug, it does not solve the problem of preparation production and sterility assurance
Through systematic literature research, there is no publication of relevant research on the production of methacholine chloride preparations by freeze-drying process

Method used

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  • Preparation formula of methacholine chloride freeze-dried powder for inhalation and preparation method of preparation formula
  • Preparation formula of methacholine chloride freeze-dried powder for inhalation and preparation method of preparation formula

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1, inhalation methacholine chloride powder

[0026] Weigh 1 g of homemade methacholine chloride crude drug, add 150 mL of ethanol, and stir until completely dissolved (the mass percentage of methacholine chloride is about 0.8%). The liquid medicine is sterilized and filtered through a 0.22 μm microporous membrane, filled in 20 mL vials, each bottle has a filling volume of 15 mL, half-filled with a rubber stopper, and placed in a lyophilizer for lyophilization. The medicinal solution is sterilized and filtered through a 0.22 μm microporous membrane, filled in vials, half-plugged with rubber stoppers, and placed in a freeze dryer for freeze-drying. The lyophilizer rapidly cools down to -40~-45°C and keeps warm for 120 minutes. After the cold trap cools down to -40~-45°C, start vacuuming, slowly raise the shelf temperature to -20~-30°C, keep warm for 9 hours, and slowly increase Shelf temperature to -10~10°C, keep warm for 4 hours, increase shelf temperature ag...

Embodiment 2

[0027] Embodiment 2, inhalation methacholine chloride powder

[0028] Weigh 1g of homemade methacholine chloride crude drug, add 1mL of water for injection, stir evenly, add propylene glycol to 50ml, stir until completely dissolved (mass percentage of methacholine chloride is about 2%). The medicinal solution is sterilized and filtered through a 0.22 μm microporous membrane, filled in 20 mL vials, each bottle filled with a volume of 5 mL, half-filled with a rubber stopper, and placed in a lyophilizer for lyophilization. The lyophilizer rapidly cools down to -40~-45°C and keeps warm for 240 minutes. After the cold trap cools down to -40~-45°C, start vacuuming, slowly raise the shelf temperature to -20~-30°C, keep warm for 9 hours, and slowly increase Shelf temperature to -10~10°C, keep warm for 3 hours, increase the shelf temperature again to 25~30°C, keep warm for 4 hours, keep the vacuum at 20~30Pa, and make the methacholine chloride product for inhalation; After the determi...

Embodiment 3

[0029] Embodiment 3, inhalation methacholine chloride powder

[0030] Weigh 1g of homemade methacholine chloride crude drug, add 0.2mL water for injection, stir evenly, add tert-butanol to 10ml, stir until completely dissolved (mass percentage of methacholine chloride is about 11.2%) . The medicinal solution was sterilized and filtered through a 0.1 μm microporous membrane, filled in 20 mL vials, each bottle filled with a volume of 1 mL, half-filled with a rubber stopper, and placed in a lyophilizer for lyophilization. The lyophilizer rapidly cools down to -45°C and keeps warm for 4 hours. After the cold trap cools down to -40~-45°C, start vacuuming, slowly (1 hour) raise the temperature of the shelf to -25°C, and keep warm for 9 hours; slowly (half an hour) ) raise the temperature of the shelf to -10°C and keep it warm for 1 hour; slowly (half an hour) raise the temperature of the shelf to 0°C and keep it warm for 1 hour; slowly (half an hour) raise the temperature of the sh...

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Abstract

The invention relates to a preparation formula of methacholine chloride freeze-dried powder for inhalation. The preparation formula is characterized by comprising the following components: 0.5-40wt% of methacholine chloride and the balance of a solvent, wherein the ratio of water in the solvent (the volume of water / the total volume of the mixed solvent) is 0-30% (v / v), and the balance is an organic solvent. According to the methacholine chloride freeze-dried powder for inhalation provided by the invention, by virtue of a freeze-drying process, filtration sterilization is adopted, so that the sterile level of the product is guaranteed, the product quality meets the requirements of Chinese pharmacopoeia on an inhalation solution, and the risk in the aspect of microorganisms is remarkably reduced in comparison with non-sterile products which are sold in the market abroad; meanwhile, the product is in a solution state during perfusion, so that the accurate control of the product loading amount is facilitated; and in addition, the product is in a low-temperature state in the production process, so that the stability can be fully guaranteed.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation formula of methacholine chloride freeze-dried powder for inhalation and a preparation method thereof. Background technique [0002] Methacholine Chloride is a bronchoconstrictor and should only be used in airway hypersensitivity testing. product name It was developed by Methapharm Inc and approved by FDA in 1986. After investigation, the existing marketed product methacholine chloride powder for inhalation is prepared by raw material drug powder packaging process. Attached equipment, so there are quality defects such as prolonged reconstitution time and inaccurate loading, and the humidity control of the production environment is very strict (usually the relative humidity of the control environment is less than 30%), which is difficult to achieve in conventional production workshops. In addition, this product needs to be reconstituted into a solution for clinic...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/72A61K31/22A61P11/00
CPCA61K31/22A61K9/19A61K9/0073A61P11/00
Inventor 苏敏宋晓丽景天水翁志洁魏农农
Owner 上海轩耘生物医药科技有限公司
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