Acyclovir 10-20% oral bioavailability; less bioavailability at higher doses; plasma peak about 2hrs after dosing; no food effect on absorption; plasma elimination t1/2 of about 2.5hrs (in adults), 4hrs (in neonates), 20hrs (in anuric patients); non-metabolized drug elimination by renal excretion; 9-33% protein binding [5,6]
Cefuroxime Axetil The t1/2 of 1.7hrs; 30-50% oral absorption; drug is hydrolyzed to cefuroxime with variable plasma concentration [5,7]
Celecoxib Unknown absolute bioavailability; peak plasma 2-4hrs after dosing; extensive protein binding; mostly metabolized to carboxylic acid and glucoronide in the urine and feces; elimination t1/2 of 11 hrs; plasma concentration of 40% (in patients with mild hepatic impairment, and 180% (in patients with moderate hepatic impairment which requires 50% reduced dose in such patients); predominantly metabolized by CYP2C9 [5]
Clarithromycin Rapid oral absorption; 50-55% bioavailability (due to first-pass metabolism); plasma peak about 2hrs after administration; 40-70% protein binding (concentration dependent); renal and non-renal elimination; several liver metabolites; oxidative N-demethylation and hydroxylation as primary metabolic pathway; elimination t1/2 of 3-7hrs (for the drug) and 5-9 hrs (for the primary metabolite, 14-hydroxylcalrithromycin); non-linear pharmacokinetics with longer t1/2 for larger dosesĀ  [5]
Diltiazem HCl Rapid oral absorption followed by reduced bioavailability due to first pass metabolism; the t1/2 of 4hrs [5] with 70-80% plasma protein binding [8]
Furosemide With 60% oral bioavailability and elimination t1/2 of 1.5hrs; about 65% of the drug excreted unchanged in urine with the rest conjugated to glucuronic acid in the kidney [5]
Gabapentin Oral absorption with no appreciable metabolism and no plasma protein binding; excreted unchanged mainly in the urine; the t1/2 of about 6hrs [5]
Ibuprofen Rapid oral absorption with high protein binding; undergoes hepatic metabolism with 90% of the drug metabolized to hydroxylate and carboxylate derivatives excreted by kidney; the t1/2 of 2hrs [5]
Levodopa Rapid absorption from the small bowel; plasma peak of 0.5-2 hrs after oral dosing; short plasma t1/2 of 1-3hrs; rate of gastric emptying, gastric pH, and the exposure to enzymes of the gastric and intestinal mucosa determine rate and extent of levodopa absorption [5]
Metformin HCl Primarily absorbed from small intestines; stable with no plasma protein binding; excreted unchanged in the urine; the t1/2 of about 2hrs; 50-60% bioavailability in fasted state; reduced and delayed absorption with food intake; plasma peak of 3hrs after oral administration [5,9]
Metoclopramide HCl Rapid oral absorption; liver metabolism via sulfation and glucuronide conjugation; primary renal excretion; the t1/2 of 4-6hrs; plasma peak within 1hr after oral dosing [5]
Metoprolol Tartrate Complete oral absorption with 40-50% oral bioavailability; the t1/2 of 3-7hrs with 12% plasma protein binding [5]
Metronidazole Rapid and complete oral absorption; the t1/2 of 8hrs with <20% binding to plasma proteins [5]
Tetracycline Variable and incomplete oral absorption; plasma peak at 2-4hrs with t1/2 of 6-12hrs; administered 2-4 times a day [5]
Verapamil HCl With 90% oral absorption; about 70% of the dose excreted as metabolites in urine and >16% in the feces with 3-4% of unchanged excreted drug; the t1/2 of 2.8-7.4hrs [10]
Table 1: Pharmacokinetic Parameters of Gastric Retention Drug Candidates.