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Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.
Acta Pharm. 2011 Jun; 61(2):217-26.AP

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+Show Affiliations

Vishnu College of Pharmacy, Bhimavaram (A.P.), India.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Clinical Trial
Comparative Study
Journal Article

Language

eng

PubMed ID

21684848

Citation

Someshwar, Komuravelly, et al. "Formulation and Evaluation of Effervescent Floating Tablets of Tizanidine Hydrochloride." Acta Pharmaceutica (Zagreb, Croatia), vol. 61, no. 2, 2011, pp. 217-26.
Someshwar K, Chithaluru K, Ramarao T, et al. Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride. Acta Pharm. 2011;61(2):217-26.
Someshwar, K., Chithaluru, K., Ramarao, T., & Kumar, K. K. (2011). Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride. Acta Pharmaceutica (Zagreb, Croatia), 61(2), 217-26. https://doi.org/10.2478/v10007-011-0015-5
Someshwar K, et al. Formulation and Evaluation of Effervescent Floating Tablets of Tizanidine Hydrochloride. Acta Pharm. 2011;61(2):217-26. PubMed PMID: 21684848.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride. AU - Someshwar,Komuravelly, AU - Chithaluru,Kalyani, AU - Ramarao,Tadikonda, AU - Kumar,K K Kalyan, PY - 2011/6/21/entrez PY - 2011/6/21/pubmed PY - 2011/10/15/medline SP - 217 EP - 26 JF - Acta pharmaceutica (Zagreb, Croatia) JO - Acta Pharm VL - 61 IS - 2 N2 - 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. SN - 1846-9558 UR - https://www.unboundmedicine.com/medline/citation/21684848/Formulation_and_evaluation_of_effervescent_floating_tablets_of_tizanidine_hydrochloride_ DB - PRIME DP - Unbound Medicine ER -