Formulation and evaluation of paliperidone HCL oral disintegrating tablets

Abstract

Paliperidone HCL is atypical antipsychotic agent which blocks D2, 5HT2, α2, α1 and H1 receptor. It is derivative of Resperidone having better efficacy in treatment of Schizophrenia. When compared with other atypical antipsychotics (eg. Chlorpromazine), it having broad spectrum activity and reduces both positive and negative symptoms  of  Schizophrenia.  It  undergoes  an  extensive  hepatic  first  pass  metabolism  leads  to  low  oral bioavailability (28%). ODT can overcome this problem through improving its bioavailability with an immediate drug release.In  the  present  work,  Oral disintegrating tablets  of  Paliperidone HCL were prepared  by  direct compression method using superdisintegrants such as Crosspovidone lycoat, and Tulsion. Paliperidone HCL has very long half hife and less bioavailability, so for enhancing the bioavailability of the drug it was formulated as a oral disintegrating tablet. The dispersion    time of    tablets were reduced w i t h increase in the concentration of superdisintegrants like Crosspovidone, lycoat, and Tulsion . From the results obtained, it was concluded that Tulsion was found to be the best among the superdisintegrants, the highest drug release of F9 is 99.45% of the drug in 30 min.