title: Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.
abstract: Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.
authors.affiliation: Vishnu College of Pharmacy, Bhimavaram (A.P.), India.
authors.forename: Komuravelly
authors.initials: K
authors.lastname: Someshwar
authors.forename: Kalyani
authors.initials: K
authors.lastname: Chithaluru
authors.forename: Tadikonda
authors.initials: T
authors.lastname: Ramarao
authors.forename: K K Kalyan
authors.initials: KK
authors.lastname: Kumar
mesh_terms: D000328:Adult; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D003000:Clonidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D005765:Gastrointestinal Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D005772:Gastrointestinal Transit; D006801:Humans; D065347:Hypromellose Derivatives; D007700:Kinetics; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D010276:Parasympatholytics / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D017693:Sodium Bicarbonate / Q000737:chemistry; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry; D013607:Tablets; D055815:Young Adult
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D005765:Gastrointestinal Agents; D010276:Parasympatholytics; D013229:Stearic Acids; D013607:Tablets; D065347:Hypromellose Derivatives; C031183:stearic acid; C023754:tizanidine; D017693:Sodium Bicarbonate; D008747:Methylcellulose; D003000:Clonidine