Formulation and In Vitro Evaluation of Extended Release Tablets of Paliperidone Using Natural Gums

Document Type: Original Article

Author

Pharmaceutics,Phd,India

Abstract

Paliperidone is a well known dopamine antagonist of the atypical antipsychotic class. In the present study Paliperidone was formulated as ER release tablets using natural and synthetic polymers separately or in combination. The aim of ER release formulation is to reduce the frequency of dosing. Tablets are prepared by direct compression method. The optimized formulations contain Paliperidone as active ingredient and Hydroxy propyl methyl cellulose (HPMC K100M), Ethyl cellulose, Albizia gum, Moi gum, Karaya gum and Copal gums are used as polymers. The reason for combination of natural and synthetic is to check its compatability and know the impact of each polymer on drug release. The quantity of gums that is used in the formulation is maximum of 60 mg per tablet and the synthetic polymers that are used are also 60mg per tablet. The evaluation parameters include the thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The prepared formulations are F1-F9 and among the formulation F2 follows non-Fickian Transport, with Zero order, Higuchi mechanism and F3, F5 and F8 following First order. The gum Moi (F2), Albizia gum (F3) and Copal gum (F5) in combination with HPMC K100M and Copal gum with Karaya gum (F8) were successful to achieve the extended drug release for 20 hours. Based on the results it was concluded that the natural polymers can be used as an efficient matrix former to provide extended release of Paliperidone. This indicates the usefulness of the formulations for once daily dosage forms. Thus the reducing frequency of dosing increases patient compliance.

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