FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF
RAPID DISINTEGRATING AND MUCOADHESIVE SUBLINGUAL
TABLETS OF LORAZEPAM
JALEH VARSHOSAZ*, FARZIN FIROZIAN, ERFANEH GHASSAMI
Department of Pharmaceutics, School of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of
Medical Sciences, Isfahan, Iran
*corresponding author: varshosaz@pharm.mui.ac.ir
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Abstract:
Lorazepam a benzodiazepine drug is used as an antianxiety, sedative, hypnotic, and anticonvulsant drug. Bypassing the
enterohepatic recirculation and first-pass metabolism of lorazepam by sublingual delivery of this drug may accelerate the
onset of its action. The objective of this study was the formulation, optimization and in vitro characterization of
mucoadhesive sublingual tablets of lorazepam. To optimize the formulation of the mucoadhesive sublingual tablets of
lorazepam seven variables including: disintegrating agent type (Primojel or Kollidone), filler [Silicified microcrystalline
cellulose (SMCC) or Avicel PH 101], carrier powder (mannitol or lactose), disintegrating agent content (5 or 10%), lubricant
type (Mg-stearate or Aerosil), drug content (1 or 2 mg) and mixing time (12 or 24 h) were studied by the Taghuchi design
and nine different formulations were prepared. The tablets were tested for their thickness, hardness, weight variation, drug
content uniformity, assay, porosity, disintegration time, bioadhesion tensile strength and dissolution efficiency and the effect
of different studied formulation parameters were studied on their properties. The formulation of tablets was optimized
considering their dissolution efficiency within 10 minutes (DE10%). The optimum formulation obtained from 2 mg of the
drug, 1.2 mg Mg-stearate, 6 mg of Primojel, 20.8 mg of Avicel, 90 mg of mannitol which was mixed for 12 hours with the
drug. This tablet with the DE10% of 81.30±2.50%, bioadhesion of 34.15±0.15%, and disintegration time of about 14 sec
seems promising as a rapid disintegrating and mucoadhesive sublingual tablet for lorazepam.






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