Design and evaluation of taste masked dextromethorphan hydrobromide oral disintegrating tablets

Abstract

Oral disintegrating tablets (ODTs) have advantages of solid dosage forms such as good stability, accurate dosing, small packaging size, and easy handling, as well as those of liquid formulations such as easy administration and minimal risk of suffocation. Therefore, they are beneficial for children, elderly and schizophrenic patients who have difficulty in swallowing conventional solid dosage forms (1). The success of ODT depends on patient acceptance, palatability and the challenging aspect in the formulation of orally disintegrating tablets is to mask the bitterness of active pharmaceutical ingredients, since most drugs have bitter taste. The distasteful sensation of a drug can be masked either by the addition of flavors, sweeteners and effervescent agents or by reducing direct contact with the patient's taste buds through coating or granulation (2, 3). Flavor is often overpowered by the taste of the medicine and the use of effervescent agents is not always convenient. Moreover, coating and granulation of the active ingredient may The present study is aimed to develop dextromethorphan hydrobromide (DXM) oral disintegrating tablets (ODT) with acceptable palatability to help patients of all age groups. The bitter taste of the drug was masked by binding the drug to ion exchange resin. The effect of the particle size of resin on drug loading was studied. In vitro and in vivo disintegration time and in vitro drug release studies were performed. Drug loading increased significantly with a decrease in the particle size of the resin. DSC and XRPD studies reveal that the molecular state of the drug changed from crystalline to amorphous form. The dissolution efficiency calculated for optimized ODT and conventional directly compressed tablet were almost comparable, indicating free dissociation of the drug from the resinate. The bitter taste of DXM can be masked by binding with ion exchange resin and the resinate can be successfully formulated into oral disintegrating tablets.

Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100

“…2) showed characteristic absorption bands, which occurred at 3297 cm -1 corresponding to (NH + stretching vibration in the tertiary amine group of the drug), 2933 cm -1 corresponding to (C-H stretching), 1615 cm -1 corresponding to (C=C stretching), 1600-1450 cm -1 corresponding to (C-C aryl stretching) and 1300-900 cm -1 corresponding to (C-N and C-O stretching) (24). This is in agreement with the previously recorded spectra of the pure drug (21). The IR region from 1400 to 600 cm -1 , termed the fingerprint region, usually contains a large number of unassigned vibrations.…”

“…This indicates the crystallinity of the drug. The recorded melting point value is in accord with literature values (21). Pure Eudragit S 100 showed a broad endotherm between 32.2 and 94.6°C, which can be attributed to the moisture content of the sample (22).…”

“…Hence, these findings can imply that dextromethorphan in the solid dispersion exists in the positively charged form (NH + group of drug in solid dispersion), which interacts with the carbonyl group of the carboxylic group of Eudragit S 100 in the solid dispersion. This kind of ionic association is referred to as a salt bridge and it significantly reduces the NH + stretching (21). This emphasized the occurrence of interaction between the drug and the polymer.…”

Physical Approaches to Masking Bitter Taste: Lessons from Food and Pharmaceuticals

“…They have been used as food processing aids to extract bitter compounds from fruit juices or directly consumed as drug delivery systems. Drug-resin conjugates have been formed into orodispersible tablets that have been shown to eliminate the bitterness of a number of drugs including chloroquine phosphate (74) donepezil hydrochloride (75), Risperidon (76), dextromethorphan hydrobromide (77), and tramadol (78). However, it should be noted that in many of these studies the bitterness suppression is claimed on the basis of reduced release into simulated saliva rather than direct sensory analysis.…”

Effect of Methyl-Β-Cyclodextrin Complexation on the Hypoglycemic and Hypolipidemic Effects of Khellin: Experimental Study

“…The withdrawn samples were filtered through 0.45 μm millipore filter and analyzed for drug content spectrophotometrically at 278 nm after appropriate dilution. Dissolution profiles were plotted and cumulative amount of drug dissolved as well as dissolution efficiency was calculated by the following equation [42]:…”