Development of Sublingual tablets of Bisoprolol Hemifumarate / Hydroxypropyl -β-Cyclodextrin Complex for Potential treatment of Angina Pectoris

Rasha Mohamed Kharshoum, Adel A Ali


Fast-disintegrating tablet drug delivery is gaining an importance for drug delivery technology especially for geriatric and pediatric patient because of swallowing difficulties.   In certain diseases such as hypertension and angina pectoris therapy, taking a fast pharmacological response is of important criteria. Thus, the aim of the present work was to prepare a novel fast disintegrating Bisoprolol Hemifumarate (BH) tablet formulation for sublingual administration based on the use of 2-hydroxypropyl-βcyclodextrin (HP-βCD) which forms an inclusion complex with (BH) to improve the permeability of the drug to sublingual membrane, in addition to mask the taste of the drug through the inclusion complex.  Attempt has been made to prepare fast disintegrating tablets of (BH) using superdistintegrants like crosscarmellose sodium and crospovidone in concentration of (5%). Eight different formulae (B1-B8) with variation in tablet excipients were prepared by direct compression method using different mucoadhesive polymers such as chitosan and polyethylene glycol 6000 at different concentration (3% and 6%) for reduction the flushing action of saliva and to provide enough contact time for drug to be absorbed. The tablets were evaluated for the weight variation, hardness, friability, wetting time, disintegration time and dissolution study. The formulae B2 and B7 possessed the lowest disintegration time due to the presence of the high concentration of chitosan, which has some disintegration action, thus were subjected to a pharmacokinetic study using human volunteers. The bioavailability of B2 was significantly higher than that of the reference (Concor®) (p > 0.05).  Thus, the present investigations suggest that (BH) sublingual tablets allowed the rapid tablet disintegration, improved bioavailability and effective in emergency treatment of anginal pain and hypertension.


Sublingual tablets, Bisoprolol Hemifumarate, 2-hydroxypropyl-ß-cyclodextrin, inclusion complex, Bioavailability

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