Development of Nanocrystal Ziprasidone Orally Disintegrating Tablets: Optimization by Using Design of Experiment and In
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Research Article Development of Nanocrystal Ziprasidone Orally Disintegrating Tablets: Optimization by Using Design of Experiment and In Vitro Evaluation Emine Tashan,1,2 Alptug Karakucuk,1 and Nevin Celebi1,3
Received 25 November 2019; accepted 7 March 2020 Abstract.
The objective of the current study was to develop ziprasidone hydrochloride monohydrate (ZHM) nanocrystal–based orally dispersible tablet (ODT) formulations. Design of experiment approach was used to develop ODTs. The tablets were compressed using direct compression method and characterized with quality control tests. In vitro dissolution studies and Caco-2 cell permeability tests were executed. The hardness and friability values of nanocrystal-based ODTs were found 31.2 N and 1.05%, respectively. The disintegration time was below 10 s. Dissolution profile in pH 7.4 phosphate buffer showed that nanocrystal-based ODTs and commercial product were dissolved in 120 min 58.98% and 16%, respectively. In pH 7.4 phosphate buffer with SLS, sample groups dissolved above 85% at the end of the study. Permeability value and cumulative ZHM amount on the cells were improved with nanocrystals. In conclusion, the novel formulation of ZHM nanocrystal–based ODTs was successfully developed for alternative dosage form.
KEY WORDS: nanocrystal(s); oral drug delivery; factorial design; dissolution; physical characterization.
INTRODUCTION Schizophrenia is a type of chronic mental disorder involving a breakdown in the relation between thought, emotion, and behavior, leading to faulty perception, inappropriate actions and feelings, withdrawal from reality and personal relationships by having fantasy and delusion, and a sense of mental fragmentation (1). It affects approximately 1% of population all over the world (2). It may arise at any age and affect women and men coequally (3,4). Patients who are schizophrenic have to use antipsychotic drug treatment. However, 40% of patients do not show compliance to treatment because of irreversible adverse effects of antipsychotics which are classified first and second generation (5–7). Moreover, long-term maintenance on the medication causes non-adherence of the drug treatment which is related with relapse and hospitalization (8). Besides, the conventional dosage forms, such as tablets and capsules, new formulation approaches of the schizophrenia treatment are needed to improve reliability of deliver medications (9). Orally disintegrating tablet (ODT) technology has gained success in recent years in pharmaceutical industry with its many advantages, such as easy swallowing and increasing patient compliance comparing with conventional tablet or liquid
1
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, Turkey. 2 Zoleant Pharmaceuticals International, Istanbul, Turkey. 3 To whom correspondence should be addressed. (e–mail: [email protected])
dosage forms (10). Intake of ODTs does not require the use of water and this is an advantage for especially old people, children, those who suffer from schizop
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