Vol.103 No.1 contentsPRACTICA OTO-RHINO-LARYNGOLOGICA
Vol. 103 No. 1 January 2010
Phase I Clinical Study of Dexamethasone Cipecilate (NS-126C), a Steroid
Nasal Spray, in Single- and Repeated-dose Administration
Minoru Okuda
(Japan Allergy and Asthma Clinic)
Dexamethasone cipecilate (NS-126C), a new steroid nasal spray in powder form, is effective in once-a-day administration. We conducted a placebo-controlled, double-blind phase I clinical study in single administration at 50 mg, 100 mg, 200 mg, or 400 mg and repeated administration at 200 mg or 400 mg once a day for 14 days in healthy adults to determine NS-126C safety and pharmacokinetics.
An analysis of subjective symptoms, objective findings, anterior rhinoscopy, laboratory tests, adrenal function tests, physical examination, throat or nasal fungal tests, and nasal ciliary function tests showed only 1 adverse event for which a causal relationship to the study drug could not be ruled out, i.e. 1 case of mild throat discomfort in 1 subject given the drug at 100 mg in the single-dose study. No adverse effect on adrenal function was observed.
In pharmacokinetic examination, plasma levels of the unchanged drug and its principal metabolite, DX-17-CPC, and the level of unchanged drug in urine were less than the quantitation limit of ＜16 pg/ml in all subjects. DX-17-CPC was detected in urine at and after 120 hours from initial administration in the repeated-dose study, but was low in concentration at less than 3 times the quantitation limit.
These findings confirmed the safety of NS-126C at 400 mg, once a day, for 14 days, with only extremely low levels of systemic exposure demonstrated.
Key words :phase I, dexamethasone cipecilate, NS-126C, nasal spray, safety, pharmacokinetic