Abstract:
Aim of the present study was to prepare and evaluate mouth dissolving tablets of antiemetic
drug like Buclizine HCl. Buclizine HCl is antihistamine drug mainly used for
emesis. Solubility of this drug is low in biological fluids which result in poor solubility
after oral administration. Therefore solid dispersion of Buclizine HCl with β Cyclodextrin
in different weight ratio (1:0.50, 1:0.75, 1:1) were prepared with view to increase its
solubility. Solid dispersion were evaluated by solubility study and drug content and
characterized by FTIR. Buclizine HCl with β Cyclodextrin (1:1) ratio showed maximum
amount of drug release hence it selected for mouth dissolving tablets formulation. Mouth
dissolving tablets of Buclizine HCl were prepared by direct compression, wet granulation
method and sublimation method by addition of superdisintigrants like sodium starch
glycolate, crospovidone, croscarmelose sodium in different concentration (2.5 %, 5 %,
7.5 %). Mannitol used to enhance mouth feel effect. Mouth dissolving tablets were
evaluated for pre compression parameters like angle of repose, bulk density, tapped
density and carr’s index and post compression parameters like hardness, thickness,
weight variation, friability, drug content and disintegration time. In vitro dissolution
study was performed using USP dissolution apparatus type II. Disintegration test was performed using disintegration apparatus as per IP specifications. % CDR measured in
Sorenson Phosphate buffer pH 6.8 measured at 230 nm. Among all formulation F8
containing 5 % Crospovidone was found suitable disintigraton time 15 secounds in
phosphate buffer pH 6.8 and drug release 99.90 % in 20 minute. F8 was selected for
stability study at room temperature condition (25±2ºC and 65±5 % RH) and accelerated
condition (40±2ºC and 75±5 % RH) for period of one month. IR results showed that drug
and excipients were compatible to each other. The results of stability studies showed that
the F8 formulation was stable in room temperature condition (25±2˚C and 65±5 % RH)
and accelerated condition (40±2˚C and 75±5 % RH). Mouth dissolving tablets of
Buclizine HCl prepared by direct compression method showed acceptable pre
compression properties and satisfactory disintegration time and in vitro dissolution
studies with improved patient compliance.
