Abstract
Purpose: An orally disintegrating tablet (ODT) of amlodipine has been developed for the benefit of patients who have difficulty swallowing solid dosage forms. Methods: Two pivotal bioequivalence studies of amlodipine ODT given with and without water, versus either amlodipine tablets or capsules, were conducted in 36 subjects each. Both studies were randomized, open-label, crossover, single-dose (10 mg) studies in healthy subjects ages 18 to 55 years. Plasma samples were collected for 168 hours post dose and pharmacokinetics were determined by non-compartmental analyses. Results: Amlodipine ODT with or without water was bioequivalent to amlodipine tablets as the ratio (90% CI) of Cmax, AUC∞, and AUClast were contained within 80–125%. Amlodipine ODT with or without water was also bioequivalent to amlodipine capsules as the ratio (90% CI) of Cmax, AUC∞, and AUClast were contained within 80–125%. Conclusion: Amlodipine ODT, given with or without water, provides equivalent systemic exposure compared to amlodipine tablets or capsules.
Highlights
Amlodipine is a calcium ion influx inhibitor of the dihydropyridine group which inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle [1]
Time Curve to the Last Quantifiable Time Point; AUC∞: Area Under the Concentration Versus Time Curve from Time 0 Extrapolated to Infinite; adverse events (AEs): Adverse Event; body mass index (BMI): Body Mass Index; confidence intervals (CIs): Confidence Interval; Cmax: Maximum Plasma Concentration; ECG: Electrocardiogram; K2-EDTA: Dipotassium Ethylene Diamine Tetraacetic Acid; λz: Elimination Rate Constant; orally disintegrating tablet (ODT): Orally Disintegrating Tablet; time for Cmax (Tmax): Time for Cmax; K2-EDTA: Dipotassium Ethylene Diamine Tetraacetic Acid
This paper describes the two pivotal bioequivalence studies – one comparing the ODT to the commercial tablet formulation, the other comparing the ODT to the commercial capsule formulation – conducted to support the registration of the amlodipine ODT formulation
Summary
Amlodipine is a calcium ion influx inhibitor of the dihydropyridine group (slow channel blocker or calcium ion antagonist) which inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle [1]. Amlodipine has several indications including first-line treatment of hypertension, to reduce the risk of coronary revascularization and the need for hospitalization due to angina pectoris, and first-line treatment of myocardial ischemia. Amlodipine tablets and capsules are available in strengths of 5 and 10 mg. For both hypertension and angina, the usual initial dose is amlodipine 5 mg once daily which may be increased to a maximum of 10 mg depending on the individual patient’s response. Absorption of amlodipine is unaffected by consumption of food [2,3,4]. In vitro studies have shown that approximately 97.5% of circulating amlodipine is bound to plasma proteins [2]
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