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. 2010 Mar;11(1):294-303.
doi: 10.1208/s12249-010-9380-5. Epub 2010 Feb 25.

In vitro release kinetics and bioavailability of gastroretentive cinnarizine hydrochloride tablet

Ramesh C Nagarwal  1 , Devendra N Ridhurkar, J K Pandit
Affiliations

In vitro release kinetics and bioavailability of gastroretentive cinnarizine hydrochloride tablet

Ramesh C Nagarwal et al. AAPS PharmSciTech. 2010 Mar.

Abstract

An oral sustained release dosage form of cinnarizine HCl (CNZ) based on gastric floating matrix tablets was studied. The release of CNZ from different floating matrix formulations containing four viscosity grades of hydroxypropyl methylcellulose, sodium alginate or polyethylene oxide, and gas-forming agent (sodium bicarbonate or calcium carbonate) was studied in simulated gastric fluid (pH 1.2). CNZ release data from the matrix tablets were analyzed kinetically using Higuchi, Peppas, Weibull, and Vergnaud models. From water uptake, matrix erosion studies, and drug release data, the overall release mechanism can be explained as a result of rapid hydration of polymer on the surface of the floating tablet and formation of a gel layer surrounding the matrix that controls water penetration into its center. On the basis of in vitro release data, batch HP1 (CNZ, HPMC-K100LV, SBC, LTS, and MgS) was subjected to bioavailability studies in rabbits and was compared with CNZ suspension. It was concluded that the greater bioavailability of HP1 was due to its longer retention in the gastric environment of the test animal. Batch no. HP1 of floating tablet in rabbits demonstrated that the floating tablet CNZ could be a 24-h sustained release formulation.

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Figures

Fig. 1
Fig. 1
Effect of viscosity grade of HPMC on drug release from floating matrix tablet
Fig. 2
Fig. 2
Effect of CO2 forming agent on drug release from floating matrix tablet
Fig. 3
Fig. 3
Effect of CA and TA combination with SBC and CC on drug release from floating matrix tablet
Fig. 4
Fig. 4
Effect of different polymers on drug release from floating matrix tablet
Fig. 5
Fig. 5
Percentage swelling profile of CNZ floating matrix tablet containing different polymers
Fig. 6
Fig. 6
Percentage erosion profile of CNZ floating matrix tablet containing different polymers
Fig. 7
Fig. 7
Plasma concentration profiles of CNZ from floating controlled release tablets (HP1) and reference (oral suspension) in healthy rabbits
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