Abstract

FORMULATION AND EVALUATION OF CLOPIDOGREL ORODISPERSIBLE TABLETS

Mahmoud Mahyoob Alburyhi*, Abdalwali Ahmed Saif, Maged Alwan Noman and Mohammed Abbas Hamidaddin

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Abstract

In the present quality assurance research work pharmaceutical manufacturing has largely grown in recent years. This and many other factors have led to the ability of manipulating pharmaceutical dosage forms and routes of administration. One example of such unique dosage forms is Orodispersible tablets ODTs, which are solid dosage forms intended to be dissolved in mouth in a relatively short time, ranging from a few seconds to up to 3minutes. In this research, Clopidogrel bisulfate was chosen to be the active pharmaceutical ingredient (API) in Orodispersible tablets ODTs formulations. Clopidogrel bisulfate is thieno pyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease and cerebrovascular disease, its solubility is very low and has very low bioavailability. A total of nine formulations of Orodispersible tablets ODTs of Clopidogrel bisulfate with Superdisintegrants like; croscarmellose sodium, and/or crospovidone in different ratios were prepared with a view to increase its effect by decreasing the time required for the drug to be released. The ingredients of the formulation were tested for compatibility study; all ingredients were compatible. Clopidogrel bisulfate and the excipients were mixed together in different ratio in nine formulation and submitted to pre-formulation tests. The powders were then compressed into tablets by direct compression method. The prepared batches of tablets were evaluated for thickness, wight variation, hardness, friability, disintegration time, wetting time, in-vitro dispersion time and in vitro dissolution studies which tested in comparing with innovator product (PLAVIX®). Clopidogrel bisulfate ODTs showed better results than PLAVIX® depending on dissolution test. Among the nine formulations the drug release of F2 and F3 formulations were found to be 92.34% and 91.8% at 2 minutes in 0.1NHCl medium while the drug release of F9 formulation were found to be 69.7% at 5minutes in phosphate buffer. The formulations F2 and F9 were the best formulations as it showed a drug release percentage 92.34% and 69.7% at 5minutes and the assay of Clopidogrel was within the acceptable limit.

Keywords: Clopidogrel bisulfate, Orodispersible tablets, Superdisintegrants, Antiplatelet therapy.