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Acta Pharmaceutica, Vol. 61 No. 2, 2011.

Short communication, Note

https://doi.org/10.2478/v10007-011-0015-5

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

KOMURAVELLY SOMESHWAR ; Vishnu College of Pharmacy, Bhimavaram (A.P.), India
KALYANI CHITHALURU ; Chalapathi Institute of Pharmaceutical Sciences, Guntur-522034 (A.P.), India
TADIKONDA RAMARAO ; Blue Birds College of Pharmacy, Warangal (A.P.), India
K. K. KALYAN KUMAR ; Chalapathi Institute of Pharmaceutical Sciences, Guntur-522034 (A.P.), India

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Abstract

Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility throughout 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.

Keywords

tizanidine hydrochloride; gastroretentive drug delivery system; floating tablets; release kinetics

Hrčak ID:

66186

URI

https://hrcak.srce.hr/66186

Publication date:

1.6.2011.

Article data in other languages: croatian

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