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Novel aerosol formulations of granisetron and uses thereof

A technology of granisetron hydrochloride and its composition, which is applied in the field of granisetron aerosol composition, can solve the problems of inconvenient administration and invasiveness, and achieve the effect of avoiding gastrointestinal intolerance

Inactive Publication Date: 2015-01-14
浙江悉娜医药有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injectable granisetron, while effective in reducing or preventing nausea and vomiting, is invasive, painful, and inconvenient to administer

Method used

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  • Novel aerosol formulations of granisetron and uses thereof
  • Novel aerosol formulations of granisetron and uses thereof
  • Novel aerosol formulations of granisetron and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0483] The preparation method of granisetron includes a spray drying method;

[0484] Granisetron has a mass median aerodynamic diameter (MMAD) of less than 5 microns;

[0485] The composition enters the pulmonary airway by inhalation;

[0486] The user is a cancer patient with symptoms of nausea or vomiting caused by chemotherapy, radiotherapy or surgery.

[0487] In a specific embodiment, regarding the composition or method of the present invention, the fine powder of granisetron is prepared by spray drying, and the process includes:

[0488] Dissolve granisetron coarse powder in distilled water to form a solution;

[0489] Obtain the fine powder of granisetron with spray-drying method;

[0490] Use cyclone separation / filtering of granisetron fine powder according to particle size;

[0491] The resulting fine granisetron powder was collected and analyzed.

[0492] In a specific embodiment, regarding the composition or method described in the present invention, the fine ...

example 1

[0561] Example 1: Preparation of granisetron fine powder - spray drying method

[0562] In a specific embodiment, the fine granisetron powder is obtained by spray drying. The spray drying system used is the SD-Micro spray drying system produced by the German GEA Group. The experiment was completed at GEA Process Engineering, Inc., Columbia, MD, USA, Columbia, Maryland, USA.

[0563] Table 1 is the parameter setting of three typical spray drying processes for preparing granisetron fine powder.

[0564]

example 2

[0565] Example 2: the measurement of the particle size distribution of granisetron fine powder obtained by spray drying method

[0566]After obtaining granisetron fine powder through the above-mentioned preparation method and parameters, the inventors analyzed the particle size distribution of the obtained product using a particle size analyzer Malvern Mastersizer produced by Malvern Instruments (Malvern Instruments, UK). The experiment was completed at GEA Process Engineering, Inc., Columbia, MD, USA, Columbia, Maryland, USA.

[0567] The typical dimensions of typical granisetron prepared by the above method are: D10: 1.01 microns; D50: 2.33 microns; D90: 5.34 microns; proportion less than 9 microns: 98.0% by weight.

[0568] For a typical particle size distribution see figure 2 .

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Abstract

Aerosol formulations of granisetron useful for pulmonary delivery are provided. The formulations are useful in the reduction, elimination or prevention of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Also provided are novel methods to treat chemotherapy-induced nausea and vomiting (CINV), radiation-induced nausea and vomiting (RINV), and post-operative nausea and vomiting (PONV) using the inhalation formulations.

Description

technical field [0001] The present invention relates to a granisetron (Granisetron) aerosol composition and use thereof. Background technique [0002] Cancer is one of the leading causes of human death in the modern world. Chemotherapy, radiation therapy and surgery are the main cancer treatments. Nausea and vomiting are common side effects of these treatments. Emetogenic effects may cause patients to delay, or even refuse, potentially effective treatments. The increase of serotonin in the blood and the activation of 5-HT3 receptors in the Chemoreceptor Trigger Zone (CTZ) in the brain are considered to be related to the emetic effect induced by anticancer treatment [Hornby, 2001]. [0003] Granisetron is a 5-HT3 receptor (5-hydroxytryptamine receptors, family3) antagonist that is commonly used as an antiemetic after chemotherapy, radiotherapy, or surgery [Aapro, 2004]. 5-HT3 receptor antagonists are thought to block 5-HT3 receptors in the chemoreceptor trigger zone and a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/00A61K31/439A61P1/08
CPCA61K47/06A61K47/26A61K9/0075A61K9/008A61K31/46A61K31/439A61P1/08A61K9/1623
Inventor 陆乔治李晓东
Owner 浙江悉娜医药有限责任公司