Preparation and Characterization of Sustained Release Matrix Tablets of Tizanidine Hydrochloride for Spinal Injuries

Purpose: To formulate matrix type sustained-release (SR) tablets of tizanidine hydrochloride (TH) for prolonged drug release and improvement in motor activity after spinal injuries. Methods: Matrix tablets were prepared by the wet granulation method using four polymers (hydroxyl propyl methyl cellulose [HPMC] K 100, ethyl cellulose [EC], guar gum, and polyvinylpyrrolidone (PVP K30) and characterized for hardness, friability, drug content, swelling, weight variation, in vitro drug release, and in vivo motor function activity using the spinal injury rat model. Results: All tablets showed good drug content, hardness, and other physicochemical properties. The tablet formulations showed a percent drug release ranging from 92.54 ± 1.02 to 98.56 ± 1.26 % at the end of 12 h. Using the spinal injury rat model, negative control had a motor activity of only 12.75 %, while F4 (containing HPMC, EC, and PVP) and F5 (containing EC, guar gum, and PVP) had motor activities of 62.25% and 57.5%, respectively, compared with 68.0 % for normal controls. Conclusion: SR matrix tablets of TH showed significant improvement in motor activity in post-traumatic spinal injury rat model.