1.Compatibility study of quetiapine fumarate with widely used sustained release excipients
M. C. Gohel • T. M. Patel. J Therm Anal Calorim (2013) 111:2103–2108
Quetiapine fumarate is a novel antipsychotic drug of dibenzothiazepine class. The chemical name of quetiapine fuma rate is 2-[2-(4-(dibenzo[b,f][1,4]thiazepin-11-yl-1-piperaziny-1)- ethoxy]ethanol fumarate (2:1) (salt). The chemical structure of quetiapine fumarate is shown in Fig. 1. Quetiapine and the active human plasma metabolite nor-quetiapine exhibit affinity
for brain serotonin (5-HT2) and dopamine D1 and D2 receptors. It is effective in treatment of schizophrenia, bipolar disorder, and major depressive disorder. As the expense of new drug development are very high and new invention is all-time low, the development of sustained release formulation is an interesting area in pharmaceutical research.
2.Quality by design approach for development and optimization of Quetiapine Fumarate effervescent floating matrix tablets for improved oral bioavailability
D. Narendar • N. Arjun • K. Someshwar • Y. Madhusudan Rao. Journal of Pharmaceutical Investigation (2016) 46:253–263
Quetiapine Fumarate (QF) is atypical anti-psychotic agent, widely used for bipolar disorder as well as schizophrenia management (Bui et al. 2013). QF is an appropriate initial treatment for psychotic disturbances in patients with schizophrenia of any stage and for those in whom a therapeutic switch is indicated for clinical reasons, such as inability to tolerate the side effects of treatment. QF shows pH dependent solubility i.e. highly soluble in acidic pH and slightly soluble in basic pH. As its solubility decreases with increase in pH, it would be more beneficial to retain the drug in stomach (acidic environment) for prolonged duration so as to achieve maximum absorption and bioavailability (Basak et al. 2007). Hence, gastroretentive drug delivery system is desirable to prolong the residence time of the dosage form in the stomach or upper gastrointestinal tract until the drug is completely released from the system (Baumgartner et al. 2000).
3.Design, optimization and pharmacokinetics of novel prolonged gastroretentive drug delivery system of quetiapine fumarate
Dharmik M. Mehta • Punit B. Parejiya • Hetal K. Patel. Journal of Pharmaceutical Investigation (2016) 46:453–465
Quetiapine fumarate (QF) is an atypical antipsychotic drug indicated for the treatment of schizophrenia and acute manic episodes associated with bipolar I disorder, either as monotherapy or as an adjunct to lithium. It is having mean terminal half-life of about 6 h. During long term treatment, it faces problems of lack of convenience and patient non-compliance due to frequent dosing. Besides, it belongs to BCS class II and exhibits pH dependent aqueous solubility and extensively absorbed from the upper part of GI tract. These characteristics make it a suitable candidate for GRDDs (Mehta et al. 2013; Velhal et al. 2011).