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Riluzole Oral Suspension: Bioavailability Following Percutaneous Gastrostomy Tube-modeled Administration Versus Direct Oral Administration.

Abstract：

PURPOSE:During amyotrophic lateral sclerosis progression, up to 85% of patients develop dysphagia. Riluzole oral suspension 50 mg/10 mL is bioequivalent to riluzole 50-mg film-coated tablets administered orally under fasting conditions. Here, we compare the bioavailability of a single 50-mg dose of riluzole oral suspension via intragastric tube, a proxy for percutaneous endoscopic gastrostomy administration, with that of oral administration in healthy volunteers under fasting conditions. Secondary objectives included the plasma pharmacokinetic and safety profiles of each administration route. METHODS:This was a single-center, single-dose, open-label, randomized, 2-period, 2-sequence, crossover bioequivalence/bioavailability study. Healthy volunteers were randomized to riluzole oral suspension 50 mg/10 mL either via nasogastric tube or orally, with a 5-day washout before crossover. FINDINGS:A total of 32 subjects were randomized (safety population); 30 were eligible for pharmacokinetic analysis. The ratios (nasogastric tube/oral) of the geometric least squares means and the geometric 90% CIs of AUC0-t, AUC0-inf, and Cmax were calculated to be 90.60% (85.66%-95.82%), 90.43% (85.47%-95.67%), and 96.99% (89.40%-105.23%), respectively, indicating bioequivalence. No significant differences in Cmax, Tmax, Kel, and t1/2el between treatments were found. Overall, riluzole oral suspension was well tolerated. No deaths or other serious adverse events were reported. IMPLICATIONS:In this study, riluzole oral suspension was bioequivalent when administered intragastrically and orally in healthy subjects under fasting conditions. Both administration methods were well tolerated. These results show that intragastric administration of riluzole oral suspension may provide an important formulation option in people with amyotrophic lateral sclerosis who have a percutaneous endoscopic gastrostomy tube.

journal_name

Clin Ther

journal_title

Clinical therapeutics

authors

Brooks BR,Bettica P,Cazzaniga S

doi

10.1016/j.clinthera.2019.09.016

subject

Has Abstract

pub_date

2019-12-01 00:00:00

pages

2490-2499

issue

eissn

0149-2918

issn

1879-114X

pii

S0149-2918(19)30495-3

journal_volume

pub_type

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Riluzole Oral Suspension: Bioavailability Following Percutaneous Gastrostomy Tube-modeled Administration Versus Direct Oral Administration.