Diclofenac potassium 12.5 mg liquid capsules: earlier and higher exposure to diclofenac. A fasted, single-dose, comparative, bioavailability study versus diclofenac potassium 12.5 mg tablets.
BACKGROUND
A fast-release liquid capsule formulation of low-dose diclofenac- K is available, which aims to improve patient convenience and compliance. The new formulation is a soft gelatin capsule designed to facilitate faster absorption of diclofenac versus the tablet form with anticipated overall comparable bioavailability.


OBJECTIVE
To compare the bioavailability of diclofenac-K 2 × 12.5 mg liquid capsules versus diclofenac- K 2 × 12.5 mg tablets.


METHODS
This randomized, open-label crossover, single-dose study was conducted in 42 healthy subjects (mean age 23.5 years) given diclofenac-K 2 × 12.5 mg liquid capsules or tablets over two 1-day treatment periods separated by a 14-day washout period.


RESULTS
Diclofenac-K 12.5 mg liquid capsules were equivalent to the tablets in terms of total systemic exposure (mean AUCt ratio = 112%, 2-sided 90% CI = (107%, 116%)). However, the mean Cmax for the liquid capsules (1,090 ng/ml) was almost double that of the tablets (583 ng/ml) (mean Cmax ratio = 196%, 2-sided 90% CI = (169%, 227%)). Median tmax was ~ 10 min faster with the liquid capsules (0.42 h) compared with the tablets (0.58 h) and AUCtmax ref for the liquid capsules (294 ng×h/ml) was almost double the value for the tablets (158 ng×h/ml). This indicated a faster absorption of diclofenac from the liquid capsules compared to the tablet. There were no differences between the two treatments regarding safety, and both drugs were well tolerated.


CONCLUSIONS
This study demonstrated equivalent overall systemic exposure to diclofenac but a faster absorption and substantially greater early exposure to diclofenac from diclofenac-K liquid capsules compared with the tablets, which may lead to a more rapid analgesic effect in patients.
Clinical Pharmacology Consultancy, Ornex, France. jean-luc.kienzler@orange.fr
Jean-Luc
JL
Kienzler
Morris
M
Gold
D000293:Adolescent; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002214:Capsules; D018592:Cross-Over Studies; D004008:Diclofenac / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D008297:Male; D013607:Tablets
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D013607:Tablets; D004008:Diclofenac