Formulation Design and Optimization of Novel Taste Masked Mouth-Dissolving Tablets of Tramadol Having Adequate Mechanical Strength

Abstract

Abstract. The purpose of this work was to develop novel taste masked mouth-dissolving tablets of tramadol that overcomes principle drawback of such formulation which is inadequate mechanical strength. Tramadol is an opioid analgesic used for the treatment of moderate to severe pain. Mouthdissolving tablets offer substantial advantages like rapid onset of action, beneficial for patients having difficulties in swallowing and in conditions where access to water is difficult. The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time while maintaining a good mechanical strength of the tablet. Mouth-dissolving tablets of tramadol are not yet reported in the literature because of its extreme bitter taste. In this work, the bitter taste of Tramadol HCl was masked by forming a complex with an ion exchange resin Tulsion335. The novel combination of a superdisintegrant and a binder that melts near the body temperature was used to formulate mechanically strong tablets that showed fast disintegration. A 3 2 full factorial design and statistical models were applied to optimize the effect of two factors, i.e., superdisintegrant (crospovidone) and a mouth-melting binder (Gelucire 39/01). It was observed that the responses, i.e., disintegration time and percent friability were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste masked mouth-dissolving tablets of Tramadol HCl with adequate mechanical strength and rapid disintegration.

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.…”

Formulation and development of orodispersible sustained release tablet of domperidone

“…As ODT-SR was formulated as compressed tablet ODT, crospovidone was used as superdisintegrant to provide quick disintegration of the tablet 52 . The time for disintegration for ODT is usually considered less than a minute 53 54,55 .…”

Fabrication and Evaluation of Rosuvastatin Calcium Fast- Disintegrating Tablets Using β-Cyclodextrin and Superdisintegrants

“…Improved dissolution rate can be ascribed to (i) an increased solubility of the drug because of its amorphous state or small particle size (Kelvin's law) [8] (ii) an increasing surface area available for drug dissolution because of the small size of the drug particles [9] and (iii) an improved wetting of the drug caused by the hydrophilic carrier [10].…”