Efficacy, Safety, and Palatability of RACTAB® Formulation Amlodipine Orally Disintegrating Tablets

Abstract

Objective: The aim of this study was to confirm the efficacy, safety, and expected palatability of amlodipine orally disintegrating tablets (ODT) [RACTAB® formulation (Towa, Osaka, Japan)]. We report the re-analyzed results of 1687 cases in clinical settings obtained through postmarketing surveillance in Japan.Method: Study subjects were patients receiving treatment for the first time with amlodipine ODT for hypertension under routine care. A multicenter central registration system was used for this prospective survey. The survey was conducted from October 2008 to October 2010. The observational period was 12 weeks, during which time surveys on outpatient blood pressure, adverse events, palatability, etc. were conducted.Results: Blood pressure stabilized following treatment, and both systolic and diastolic blood pressures were favorably controlled. Adverse events observed were not significantly different from those observed during drug use trials of amlodipine formulations reported in 2003. Moreover, palatability of amlodipine ODT showed a 99.6% (227 of 228 cases) favorable patient acceptance, which is consistent with the initial design concept of RACTAB® formulation.Conclusions: The results of this postmarketing surveillance study indicated that the efficacy, safety, and palatability of amlodipine ODT met our expectations (dissolves quickly in the mouth, tastes good, and is not rough on the tongue). Accordingly, amlodipine ODT are believed to be an easy-to-use formulation for prescribing doctors, dispensing pharmacists, and patients receiving treatment.

Formulations of Amlodipine: A Review

“…It is a convenient and modest method of administration without the need of water [13, 14] with good palatability [15, 16]. The dispersible tablets of ADB are comparatively bioequivalent to conventional tablets [17].…”

“…The dispersible tablets of ADB are comparatively bioequivalent to conventional tablets [17]. The main drawback of using orally disintegrating or crushed tablets of AD is their bitter taste [16, 18, 19] and, therefore, taste masking of such dosage forms is very important to increase palatability [15]. …”

Coated dextrin microcapsules of amlodipine incorporable into orally disintegrating tablets for geriatric patients

“…Each sample containing an amount equivalent to 10.0 mg amlodipine was placed into 900 mL of pH 1.2 HCl solution or pH 6.8 phosphate-buffered saline (PBS) as dissolution media. One mL of each dissolution medium was collected at predetermined time intervals (10,20,30,60,90, and 120 min) and filtered using a 0.45 mm membrane filter. The concentration of dissolved amlodipine was determined using the HPLC method above.…”

“…Amlodipine, a long-acting dihydropyridine-type calcium channel blocker, is considered to be one of the most effective and tolerable agents in the elderly for reducing blood pressure and vascular morbidity and mortality [4][5][6][7]. Like other antihypertensive drugs used for chronic conditions in the geriatric population [8,9], amlodipine has been developed into orally disintegrating tablets (ODT's) that can enhance geriatric patient compliance and acceptance for long-term daily administration [10,11].…”

“…In the formulation of amlodipine ODT's, the besylate salt form used in marketed conventional tablets has primarily been used because of its increased aqueous solubility compared to the free base [10,11]. When, instead of salt forms, amlodipine free base is intentionally employed as an alternative active ingredient, its limited oral absorption and bioavailability as a result of the lower dissolution rate and permeability characteristics in the gastrointestinal tract are challenges that must be overcome for ODT development [12,13].…”