Drug Excipient Compatibility, Development and Preliminary Clinical Studies of Tizanidine Hydrochloride Floating Drug Delivery System

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The objective of this investigation was to develop formulation of floating matrix tablets of tizanidine HCl to prolong the gastric residence time by using hydroxy propyl methyl cellulose (HPMC K15M) or xanthan gum as sole release retardant and to check the clinical response. The drug-excipients compatibility studies were conducted using DSC and also by visual observation. Incorporation of NaHCO3 in the formulation resulted incompatibility with drug and therefore, the composition was modified by replacing NaHCO3 with CaCO3 in remaining formulations. Floating matrix tablets of tizanidine were developed by direct compression method and the developed ten formulations exhibited satisfactory physicochemical characteristics and in-vitro buoyancy. Formulation (F9) was selected as optimized formulation based on physicochemical characters, in-vitro buoyancy and drug release, and was used in in-vivo radiographic studies in human volunteers by incorporating BaSO4. In radiographic studies, the gastric retention time of floating tablets was found to be 4 ± 0.86 h (n=3). Optimized floating tablets (F9) were used to know the clinical effects in patients suffering from spasticity under the observation of clinician. The optimized tizanidine HCl floating matrix tablets were developed and found to have gastric retention behaviour in stomach and further were found to have good clinical effects in patients suffering from spasticity during preliminary clinical studies.