Use of zoledronic acid, powder aerosol and preparation method

A technology of zoledronic acid micropowder and zoledronic acid is applied in the directions of aerosol delivery, pharmaceutical formulations, respiratory system diseases, etc., and can solve the problems of no inhalation dosage form, and zoledronic acid has no therapeutic application of respiratory system diseases, etc. Achieve the effect of low systemic side effects, good safety, and rapid metabolism into the blood

Inactive Publication Date: 2018-01-09
HANGZHOU DC PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there are no research reports on the application of zoledronic acid in the treatment of respiratory diseases not related to bone mass, and there are no research reports on the application of zoledronic acid in inhalation forms such as powder aerosol or atomized liquid droplets

Method used

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  • Use of zoledronic acid, powder aerosol and preparation method
  • Use of zoledronic acid, powder aerosol and preparation method
  • Use of zoledronic acid, powder aerosol and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] one step pulverization

[0088] Get 1000g of zoledronic acid crude drug, and load it into the QS100 pulverizer. The pulverization condition is 0.7 MPa pulverization pressure, 2 hours, pulverization once, to obtain zoledronic acid fine powder. Preliminary observation shows that the micropowder has no adhesion, no agglomerates, and is well dispersed.

[0089] About 1g of the micropowder sample was taken, and the particle size of the micropowder powder was measured using a laser particle size analyzer from Malvern Instruments Ltd. in the United Kingdom. As a result, the particle size of the above sample was 8.54 μm for d90, 3.40 μm for d50, and 1.09 μm for d10.

[0090] In order to investigate whether the preparation process caused the destruction and degradation of zoledronic acid, the molybdenum blue colorimetric method was used to measure the raw material drug of zoledronic acid before pulverization and the powder after pulverization. The method is to take 8 mg each o...

Embodiment 2

[0092] two-step pulverization

[0093] Get 1000g of zoledronic acid crude drug, and load it into the QS100 pulverizer. The crushing condition is 0.7MPa crushing pressure, crushing twice. The first crushing time is 1.5 hours, and the second crushing time is 2 hours. Obtain zoledronic acid micropowder. Preliminary observation shows that the micropowder has no adhesion, no agglomerates, and is well dispersed.

[0094] About 1g of the micropowder sample was taken, and the particle size of the micropowder powder was measured using a laser particle size analyzer from Malvern Instruments Ltd. in the United Kingdom. As a result, the particle size of the above sample was 2.73 μm for d90, 1.61 μm for d50, and 0.58 μm for d10.

[0095]In order to investigate whether the preparation process caused the destruction and degradation of zoledronic acid, the molybdenum blue colorimetric method was used to measure the raw material drug of zoledronic acid before pulverization and the powder af...

Embodiment 3

[0097] spray drying

[0098] Dissolve 0.5g of zoledronic acid in 200ml of water, 2.5g of ammonium bicarbonate in 100ml of water, mix the two solutions, then add 200ml of ethanol and mix to form a 40% ethanol aqueous solution for spraying. Ammonium bicarbonate completely degrades and volatilizes during the spray drying process, so that small holes are produced in the finally formed zoledronic acid solid micropowder.

[0099] B-290 spray dryer, equipped with 0.7mm 2-liquid nozzle. The conditions are: inlet temperature 160°C, 100% suction, feed rate 15ml / min, spray rate 500L / h. Dry powder samples were stored in a desiccator at room temperature. The outlet temperature is about 70°C.

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Abstract

The invention provides new use of zoledronic acid and a novel dosage form for inhalation administration. The zoledronic acid for inhalation administration can be in the form of powder aerosol and atomized droplets, and is characterized in that the granularity is less than or equal to 7mu m; the zoledronic acid can include or not include any auxiliary material. The zoledronic acid for inhalation administration can directly promote airway relaxation, resisting inflammation and improving pathology on the respiratory tract, can be used for treating chronic obstructive pulmonary diseases and/or asthma, and can significantly improve the pulmonary function of mice suffering from chronic obstructive pulmonary diseases, reduce the airway resistance by about 50 percent, and enhance the pulmonary dynamic compliance by about 50 percent.

Description

technical field [0001] The invention belongs to the field of pharmacy and preparation, and relates to zoledronic acid for inhalation administration, its preparation method and application. Background technique [0002] Zoledronic acid (zoledronic acid, ZOL), its chemical name is 1-hydroxy-2-(imidazol-1-yl)-ethylene-1,1-diphosphoric acid, and its molecular formula is C 5 h 10 N 2 o 7 P 2 , the molecular weight is 272.09; the hydrate containing 1 molecule of water is commonly used, and the molecular formula is C 5 h 10 N 2 o 7 P 2 ·H 2 O, with a molecular weight of 290.10, is a third-generation bisphosphonate drug bone resorption inhibitor. In 2007, it was approved by the US FDA for the treatment of osteoporosis, women's postmenopausal osteoporosis, and Paget's disease. It can also be used for the treatment of fractures or pain caused by hypercalcemia and tumor bone metastasis. In the United States The trade names in the market are RECLAST and ZOMETA, and there are ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61K9/12A61K9/72A61P11/06A61P11/00
CPCA61K9/12A61K31/675A61P11/00A61P11/06
Inventor 陈燃陆泉栗波兰海侠
Owner HANGZHOU DC PHARM CO LTD
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