Formulation and in vivo evaluation of ondansetron orally disintegrating tablets using different superdisintegrants

Abstract

The aim of this study was to formulate cost effective taste-masked orally disintegrating tablets of ondansetron, a bitter drug using different superdisintegrants by a wet granulation technique. Microcrystalline cellulose (Avicel) as a diluent and disintegrant in addition to aspartame as a sweetener were used in all formulations. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. The tablets' hardness was maintained in the range of 2-3 kg and friability was <1% for all batches. All tablet formulations disintegrated rapidly in vitro within 5.83 to 33.0 sec. The optimized formulation containing 15% Polyplasdone XL-10 released more than 90% of drug within 5 min and the release was comparable to that of a commercial product. In human volunteers, optimized formulation was found to have a pleasant taste and mouth feel and they disintegrated in the oral cavity within 12 sec. The stability results were also satisfactory. A pharmacokinetic study with the optimized formulation was performed in comparison with a reference (Zofer MD 8®) and they were found to be bioequivalent. In conclusion, a cost effective ondansetron orally disintegrating tablet was successfully prepared with acceptable hardness, desirable taste and rapid disintegration in the oral cavity.

Oral transmucosal drug delivery for pediatric use

“…Depending on the formulation, the tablet generally disintegrates and dissolves rapidly, usually within 15 to 30 min, to allow immediate drug release, or adheres to the mucosa to allow prolonged drug release. In the case of disintegrating tablets, rapid disintegration can be achieved by incorporating superdisintegrants such as polyplasdone, croscarmellose sodium and sodium starch glycolate into the formulation [90,91]. At the same time, these tablets must be sufficiently robust to withstand the physical forces experienced during handling and transportation.…”

A Review of Disintegration Mechanisms and Measurement Techniques

“…Such formulations are particularly important where a rapid onset of action is desired, e.g. for analgesics [4] or to enable enhanced bioavailability of a poorly soluble drug substance [5]. In contrast, in modified - release tablets the API release may be designed to be gradual in order to achieve slow and sustained dissolution in, or selective absorption across, the gastrointestinal (GI) tract, and/or resulting in a delayed onset time.…”

Palatability and Preference of Gummi Formulations with Various Pharmaceutical Characteristics

“…Various efforts have been made to improve medication adherence, [1][2][3] because it is a complex, multi-determined behavior that is often influenced by the cost of treatment, drug regimen complexity, and patient-related factors. Optimized dosage forms for each patient, such as orally disintegrating tablets, 4,5) oral jelly formulations, 6) chewable tablets, 7,8) and gummi formulations, [9][10][11] have important roles in medication adherence. Gummi drugs are dried jelly drugs prepared by adding gelatin as a gelling agent to syrup, consisting of carbohydrates such as sugar and starch syrup that have been boiled down.…”