Author: David Beer ; Gillian M. Spooner ; Deborah Hynx ; Katharine L. Turner ; Simon J. Watson ; Morris F. Tweed ; Sarah Craig ; Bernard M. Cuenoud ; Paul A. Kirkham ; Lazzaro Mazzoni ; Pamela Tranter ; Sandra Haberthuer ; David Bentley ; Keith D. Butler ; Christoph Walker ; Lucy Barker ; Elisabeth Schaebulin ; David A. Sandham ; Thomas H. Keller ; Claire Ffoulkes-Jones ; Gaynor E. Pilgrim ; Sarah Jeffers ; David Farr ; Rowan Stringer ; Andrew Nicholls ; Janet C. Maas ; John R. Fozard ; David Beattie ; Louise Bidlake ; Colin Howes

A series of novel corticosteroid derivatives featuring C-17 furoate ester functionality have been synthesised. Profiling in vitro and in vivo has resulted in the identification of a compound with a longer duration of action and a lower oral side effect profile in rodents compared to budesonide.

01 Feb 2003·Journal of Controlled ReleaseQ1 · MEDICINE

A new agglomerated KSR-592 β-form crystal system for dry powder inhalation formulation to improve inhalation performance in vitro and in vivo

Q1 · MEDICINE

Article

Author: Yoshiaki Kawashima ; Kazuki Mimura ; Den-ichi Momose ; Kiyohisa Ouchi ; Hiromitsu Yamamoto ; Hirofumi Takeuchi ; Kazuhiko Ikegami

A new agglomerated KSR-592 (steroid) beta-form needle-like crystals with lactose system for dry powder inhalation (DPI) was developed to improve inhalation performance with Jethaler. The drug agglomerates were prepared by the method of spherical agglomeration in liquid so as to control the particle size and the mechanical strength of agglomerates by changing the agitation speed of the agglomeration system. The agglomerates mixed with lactose particles for the DPI formulation were effectively disintegrated into respirable fine particle in the milling chamber of the device (Jethaler) when inhaled. The DPI formulation with these agglomerates exhibited ideal fluidity and provided a larger fine particle fraction (FPF: 29.7%) than the formulation with agglomerates consisting of alpha-form (plate-like) crystals (24.5%). The air-flow rate of inhalation had no effect on the disintegration properties of these agglomerates, suggesting a reliable inhalation performance in vivo. Further, an in vivo test of the aerosolized KSR-592 (beta-form) crystals having the same particle size distribution as those in the aerosol produced by Jethaler was conducted by means of a dry powder inhalation testing system using Brown Norway rats. Inhaled KSR-592 (beta-form) crystals were found to be uniformly deposited in the lungs of Brown Norway rat sensitized by ovalbumin (OA) and suppressed the increase in eosinophil number in the lungs after OA challenge.

01 Feb 2003·Powder Technology

Simultaneous particulate design of primary and agglomerated crystals of steroid by spherical agglomeration in liquid for dry powder inhalation

Author: Yoshiaki Kawashima ; Den-ichi Momose ; Kiyohisa Ouchi ; Nobuyuki Isshiki ; Hiromitsu Yamamoto ; Hirofumi Takeuchi ; Kazuhiko Ikegami

Spherical agglomerates of steroid KSR-592, consisting of fine primary drug crystals suitable for dry powder inhalation (DPI), were prepared by the spherical agglomeration method in liquid with a bridging liquidIt was found that the particle size of primary crystals increased until the dispersing medium was saturated with the bridging liquid, whereas the spherical agglomeration of primary crystals was continued even after the saturation of medium with the bridging liquidThe growth rates of primary crystals and agglomerates increased with an increase in the temperature and/or a reduction in the agitation speed of the system.The agglomerates were easily disintegrated into the primary crystals depositing ideally on carrier lactose particles for DPI by mixing.The in vitro efficiency of the mixed system of lactose and disintegrated primary crystals of drug was 2 to 3 times higher than that of crystals prepared conventionally.Furthermore, the soft agglomerates disintegrated easily into respirable particles in air stream when emitted from the inhalation device were prepared by reducing the agitation speed after the dispersing medium was saturated with the bridging liquid

100 Deals associated with CGP-13774

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 1	-	Kissei Pharmaceutical Co., Ltd.	-
Asthma	Phase 1	-	Novartis Pharma AG	-
Rhinitis, Allergic	Phase 1	-	Novartis Pharma AG	-
Rhinitis, Allergic	Phase 1	-	Kissei Pharmaceutical Co., Ltd.	-

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