Effect of Time Interval between Food and Drug Ingestion on the Absorption of Oxybutynin from a Controlled‐Release Tablet

Abstract

Abstracl:The effect of time interval between food and drug ingestion on the bioavailability of oxybutynin was investigated in a randomized, three-phase cross-over study in 3 1 healthy volunteers. The serum concentrations of oxybutynin and the metabolite, N-desethyloxybutynin were measured up to 48 hr after ingestion of a controlled-release 10 mg oxybutynin tablet either in fasting state, 2 hr after breakfast or I hr before. The C , , , of both oxybutynin (P<O.OOOI) and Ndesethyloxybutynin (P<0.0001) and the AUC,-, of N-desethyloxybutynin (P<0.05) were significantly larger when oxybutynin was ingested 2 hr after breakfast. than during the fasting, but the AUCw, of oxybutynin remained unchanged. Breakfast ingested I hr after oxybutynin did not affect the pharmacokinetic parameters of oxybutynin or N-desethyloxybutynin. The saliva secretion rate decreased slightly more (P<0.05), when oxybutynin was administered 2 hr after breakfast than during fasting. The effect of food ingestion on the serum concentrations of oxybutynin and N-desethyloxybutynin is expected to have minor clinical significance only. However, ingestion of the controlled-release tablet 1 hr before meal increases the likelihood of obtaining constant drug levels with lower peak concentrations during the dosage interval, and thus ingestion of the controlled-release tablet 0.5-1 hr before food may well improve tolerability and compliance in patients who suffer from adverse reactions.

A short review of drug–food interactions of medicines treating overactive bladder syndrome

“…Lukkari et al [19] investigated the effect of food on the prevalence of drug related adverse effects. The authors confirmed that a meal resulted in a significant increase in C max both for the drug and its metabolite, and increased AUC for N-deethyloxybutynin.…”

Medication and food issues for overactive bladder/lower urinary tract symptoms: When do we eat?

“…To alleviate these effects by maintaining a more constant level of oxybutynin, an ER formulation is commonly used [11]. Studies have shown that although there are alterations in oxybutynin ER pharmacokinetics when it is taken in a fasting state versus a fed state, the differences are not clinically signifi cant and should not affect the therapeutic response [4,12,13]. However, it also has been shown that the presence of food may increase the initial release of oxybutynin from its ER formulation, producing a slightly higher concentration peak and the possibility for increased nonbladder effects such as dry mouth.…”

“…However, it also has been shown that the presence of food may increase the initial release of oxybutynin from its ER formulation, producing a slightly higher concentration peak and the possibility for increased nonbladder effects such as dry mouth. Therefore, it may be recommended to take oxybutynin ER 1 hour before meals to maintain more consistent and level oxybutynin concentrations, especially in individuals prone to systemic side effects [4,12].…”

Rapid and selective UV spectrophotometric and RP-HPLC methods for dissolution studies of oxybutynin immediate-release and controlled-release formulations

“…OXB and/or its formulation(s) are official in USP, EP and BP. Being the drug of first choice in treating UI, OXB has been studied extensively for its pharmacodynamic properties [5,6] and pharmacokinetic parameters [7][8][9].…”