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Aerosol compositions

A composition and aerosol technology, applied in the field of medicinal aerosol compositions and their preparation, can solve the problems of small proportion of active components, impossible to ensure uniformity of content, complexity and the like

Inactive Publication Date: 2004-02-11
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method is not only complicated, but also has disadvantages, since the proportion of the active ingredient is rather small, it is almost impossible to ensure uniformity of its content for each dispersant at the stage of distributing the propellant for dispersing the active ingredient in batches sex

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] FK506 was pulverized to a particle size of 2-3 μm by using a jet mill and the resulting powder was kneaded together with Miglyol 812. After distributing the kneaded body, fill the HFA-227 pre-cooled to -20°C into each dispersing mixer and install a valve to obtain an aerosol product (cold filling method) containing the following components per unit (5ml) ).

[0090] FK506 10mg (0.2(w / v)%)

[0091] Miglyol 812 25mg (0.5(w / v)%)

[0092] HFA-227 5ml

Embodiment 2

[0094] Fill the kneader with the following components per unit (5 ml) obtained in a similar manner to Example 1 into a dispersing mixer, and, after installing the valve, pressurize to 20 atmospheres at room temperature HFA-227 was filled into each dispersing mixer to obtain a pharmaceutical aerosol composition with the same components as in Example 1 (pressure filling method).

[0095] FK506 5mg (0.1(w / v)%)

[0096] Miglyol 812 10mg (0.2(w / v)%)

[0097] HFA-227 5ml

Embodiment 3-11

[0100] In a similar manner to Example 2, an aerosol composition containing the following components per unit (5 ml) can also be prepared.

[0101] FK506 10mg

[0102] Miglyol 812 25mg

[0103] Polyvinylpyrrolidone 0.25mg

[0104] HFA-227 5ml

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PUM

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Abstract

The use of a medium-chain fatty acid triglyceride as the dispersant in the preparation of a medicinal aerosol composition comprising tricyclic compound (I) dispersed in a liquefied hydrofluoroalkane propellant is described. When a liquefied hydrofluoroalkane is added to a kneaded premix of the tricyclic compound (I) and a medium-chain fatty acid triglyceride, the active ingredient is evenly dispersed in the liquefied hydrofluoroalkane. Therefore, by distributing a dispenser first with the kneaded premix and, then, with a liquefied hydrofluoroalkane under cooling or elevated pressure, there can be provided a medicinal aerosol composition an improved uniformity of content of the active ingredient.

Description

Technical field: [0001] The invention relates to a pharmaceutical aerosol composition and a preparation method thereof, and finds the application of the composition in the field of pharmacy. Background technique: [0002] It is known that the tricyclic compound (I) used in the present invention and its pharmaceutically acceptable salts have excellent pharmacological activities, such as immunosuppressive activity and antibacterial activity, so they can be used for the treatment and / or prevention of organ transplantation or tissue transplantation, Graft-host disease, rejection by various anti-immune diseases and infectious diseases (see eg EP-A-0184162 and WO 89 / 05304). [0003] In particular, compounds belonging to the tricyclic compound (I) and referred to as FR900506 (=FK506), FR900520, FR900523 and FR900525 were produced by Streptomyces, particularly Streptomyces tsukubaensis No. 9993 (Depository: 1-3, Higashi 1 chome , Yatabe-machi, Tsukuba-gun, Ibaraki-ken, Japan, F...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K9/00A61K31/135A61K31/137A61K31/35A61K31/407A61K31/425A61K31/436A61K31/4433A61K31/4525A61K31/46A61K31/47A61K31/57A61K31/573A61K38/00A61K45/00A61K47/06A61K47/14A61P11/00A61P11/08A61P31/04A61P37/06A61P43/00C07D498/18
CPCA61K9/12A61K9/008A61K31/4433A61P11/00A61P11/08A61P31/04A61P37/06A61P43/00
Inventor 村田三郎下条文男德永雄二秦武久
Owner ASTELLAS PHARMA INC