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Bioavailability Enhancement of Rizatriptan Benzoate by Oral Disintegrating Strip: In vitro and In vivo Evaluation

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Oral disintegrating strips containing rizatriptan benzoate, a selective 5-hydroxy tryptamine receptor agonist with anti migraine property, was developed using polyvinyl alcohol, sodium alginate and hydroxyl propyl methylcellulose as the base materials. The analytical and bioanalytical methods were developed and validated using HPLC (PDA and flouroscence detectors). The dissolution study performed on the strips revealed that all the five formulations, release the drug within eight minutes. Under ICH accelerated stability conditions, strips were stable at 40°C and 75% humidity for eight weeks. Furthermore, pharmacokinetic properties of oral strip were compared with rizatriptan benzoate marketed tablet. Oral disintegrating strip and tablet showed significantly higher bioavailability. Oral strip exhibited better pharmacokinetic parameters than rizatriptan marketed tablet. The Tmax, Cmax, AUC and t1/2 for oral strip were found to be 1.00 h, 64.13±19.46 ng/mL, 352.00±71.57 ng/mL/h and 3.09±1.03 h respectively, whereas, tablet showed 1.5 h, 38.00±13.43 ng/mL, 210.38± 40.37ng/mL/h and 1.66±0.31 h respectively. These findings confirm that the rizatriptan benzoate oral disintegrating strip is potentially a useful tool for an effective treatment of migraine with improved bioavailability, rapid onset of action and with increased patient compliance.
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Keywords: Bioavailability; HPLC; Oral disintegrating strips; Rizatriptan benzoate; Stability

Document Type: Research Article

Publication date: May 1, 2016

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  • The aim of Current Drug Delivery is to publish peer-reviewed articles, short communications, short and in-depth reviews in the rapidly developing field of drug delivery. Modern drug research aims to build in delivery properties of a drug at the design phase, however in many cases this ideal cannot be met and the development of delivery systems becomes as important as the development as the drugs themselves.

    The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance.

    The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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