Application of sodium ibandronate, powder inhalation and preparation method

A technology of sodium ibandronate and powder spray, applied in the field of sodium ibandronate, can solve the problems of no inhalation dosage form and no respiratory system of sodium ibandronate, and achieve low systemic side effects, good safety, The effect of rapid metabolism in the blood

Inactive Publication Date: 2017-12-08
HANGZHOU DC PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no research report on the application of ibandronate sodium in the treatment of respiratory diseases not related to bone mass, and there is no research report on the application of ibandronate sodium in inhaled dosage forms such as powder aerosol or atomized liquid droplets

Method used

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  • Application of sodium ibandronate, powder inhalation and preparation method
  • Application of sodium ibandronate, powder inhalation and preparation method
  • Application of sodium ibandronate, powder inhalation and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] one step pulverization

[0088] Get 1000g of ibandronate sodium bulk drug, and load it into the QS100 pulverizer. The pulverization condition is 0.7MPa pulverization pressure, 2 hours, pulverization once, to obtain ibandronate sodium 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 5.55 μm for d90, 2.73 μm for d50, and 0.90 μm for d10.

[0090] In order to investigate whether the preparation process caused the destruction and degradation of sodium ibandronate, the raw material drug of sodium ibandronate before pulverization and the powder after pulverization were determined by molybdenum blue colorimetry. The method is to take 8 mg each of t...

Embodiment 2

[0092] two-step pulverization

[0093] Get 1000g of ibandronate sodium bulk 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 ibandronate sodium 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 sodium ibandronate, the raw material drug of sodium ibandronate before pulverization and the powder after pulverization were determined by molybdenum ...

Embodiment 3

[0097] spray drying

[0098] Dissolve 0.5g of ibandronate sodium in 200ml of water, 2.5g of ammonium bicarbonate in 100ml of water, mix the 2 solutions, then add 200ml of ethanol and mix to form a 40% ethanol aqueous solution for spraying. Ammonium bicarbonate is completely degraded and volatilized during the spray drying process, so that small pores are formed in the finally formed ibandronate sodium 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 application of sodium ibandronate and a new formulation for inhalation administration. The sodium ibandronate for inhalation administration exists in two forms of powder inhalation and atomized droplets, and is characterized in that the granularity is smaller than or equal to 7mum, and the sodium ibandronate can contain accessories or no accessory. According to the sodium ibandronate for the inhalation administration, provided by the invention, the functions of directly promoting airpassage relaxation in a respiratory passage, resisting inflammation and improving pathology can be obtained, the application of treating a chronic obstructive pulmonary disease and / or asthma can be obtained, the pulmonary function of mice suffering from the chronic obstructive pulmonary disease can be remarkably improved, the air passage resistance of the mice is reduced by about 40 percent, and the pulmonary dynamic compliance of the mice is increased by about 90 percent.

Description

technical field [0001] The invention belongs to the field of pharmacy and pharmacy, and relates to ibandronate sodium for inhalation administration, its preparation method and application. Background technique [0002] Ibandronate sodium (Ibandronate sodium, IBA), its chemical name is 1-hydroxy-3-(methylpentylamine)-propane-1,1-sodium bisphosphonate, its molecular formula is C9H22NO7P2 Na, its molecular weight is 341.21 ; Commonly used to contain 1 molecule of water, the molecular formula is C9H22NNaO7P2 · H2O, the molecular weight is 359.23, is a third-generation bisphosphonate drug bone resorption inhibitor. In 2003, the U.S. FDA approved it for the prevention and treatment of postmenopausal osteoporosis in women. The product name in the U.S. market is BONIVA, and the Chinese name is Bangluoli. There are two dosage forms of oral tablet and intravenous injection. The clinical dose is about 150mg / tablet / month orally, and 3mg / 3 months for intravenous injection. The average ...

Claims

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Application Information

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IPC IPC(8): A61K31/663A61K9/72A61K47/26A61P11/00A61P11/06
CPCA61K9/0073A61K31/663A61K47/26
Inventor 陈燃陆泉栗波褚梦思
Owner HANGZHOU DC PHARM CO LTD
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