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Title: Ultrafine particle power for inhalation and method for
production thereof
United States Patent: 5,972,388
Inventors: Sakon; Kiyoyuki (Hino, JP); Sakagami;
Masahiro (Hino, JP); Makino; Yuji (Hino, JP); Suzuki; Yoshiki (Hino, JP);
Kobayashi; Hideki (Hino, JP)
Assignee: Teijin Limited (Osaka, JP)
Appl. No.: 779614
Filed: January 7, 1997
Abstract
An ultrafine particle powder for inhalation to be delivered mainly to a
lower airway, containing specific cellulose lower alkyl ethers and a
medicament, at least 80% of the powder having a particle size in the range
of 0.5 to 10 .mu.m.
DISCLOSURE OF INVENTION
In accordance with the present invention, there is
provided an ultrafine particle powder for inhalation comprising
hydroxypropyl cellulose, and/or hydroxypropyl methyl cellulose, and a
medicament, at least 80% of the powder having a particle size of 0.5 to 10
.mu.m.
It will be understood from the above description that the ultrafine
particle powder for inhalation of the present inventors comprising
hydroxypropyl cellulose and/or hydroxypropyl methyl cellulose and a
medicament and containing particles having a particle size of 0.5 to 10 .mu.m
in an amount of at least 80% is a novel technical conception which cannot
be obtained even from the analogy to the conventional technical idea.
As a result of intensively carrying out research, the present inventors
have discovered that when an ultrafine particle powder comprising
hydroxypropyl cellulose and/or hydroxypropyl methyl cellulose, and a
medicament, at least 80% of the powder having a particle size of 0.5 to 10
.mu.m, is used as an inhalant, the powder becomes an inhalant exhibiting
good delivery to and good deposition at a lower airway such as a trachea
and bronchi, being excellent in retaining properties and sustained
releasing properties of the medicament at deposition sites, and having
excellent properties such as efficient productivity, stability, safety and
uniformity. The present invention has been achieved on the basis of the
discovery.
Furthermore, in accordance with the present invention, there is provide a
method for the production, by spray drying, of an ultrafine particle
powder for inhalation comprising hydroxypropyl cellulose and/or
hydroxypropyl methyl cellulose and a medicament, at least 80% of the
powder having a particle size of 0.5 to 10 .mu.m.
Furthermore, in accordance with the present invention, there is provide a
powder preparation for inhalation comprising such an ultrafine particle
powder for inhalation. Since such an ultrafine particle powder for
inhalation of the present invention has a particle size in a specific
numerical range, it is capable of being delivered principally to a lower
airway.
Claim 1 of 8 Claims
1. An ultrafine particle powder for administering a medicament to the
lower airways by oral inhalation comprising cellulose lower alkyl ether
wherein said cellulose lower alkyl ether is hydroxypropyl cellulose,
wherein at least 80% of said powder has a particle size of from 0.5 to 10
.mu.m and the particle powder is capable of being delivered principally to
lower airways and is obtained by spray drying, wherein said cellulose
lower alkyl ether is present in an amount effective to achieve sustained
release of said medicament.
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