Abstract:
The aim of the present investigation was to develop a fast dissolving tablets using beta
cyclodextrin complexation with an objective to enhance solubility and increase
dissolution properties of Loratadine which is Histamine H1 Antagonists.
Complexation of Loratadine was carried out with beta cyclodextrin as a carrier by
kneading and solvent evaporation methods and the prepared complexes were
characterized by FTIR and optimized on the basis of solubility studies. The complex
obtained by kneading method with 1:3 ratio of drug:beta cyclodextrin showed highest
complex efficiency and solubility which was further used in preparation of Fast
Dissolving Tablets (FDTs). Fast dissolving tablets were prepared by direct
compression and sublimation method using superdisintegrants like indion 234 and
Crospovidone at varying amounts. FTIR studies between drug and excipients
suggested the absence of chemical interaction between the drug and excipients.
Various batches were prepared using 32 factorial design. The amounts of indion 234 and crospovidone were taken as formulation variables (factors) and disintegration
time and % drug release were taken as dependent variables (responses). The prepared
batches of FDTs were evaluated for hardness, friability, weight variation, drug
content, disintegration time, wetting time, in vitro dispersion time and drug release.
The formulation S8 prepared by sublimation method containing 18.75 mg indion 234
and 18.75 mg crospovidone was selected as optimized formulation which showed
disintegration time 20.66±0.57 second and drug release 95.31±0.549% after 15
minute. The two extra checkpoint batches were prepared and evaluated and closeness
of predicted and actual values validated the design. The results of stability studies
indicated no significant change in the tablet properties. The optimized batch was
compared with marketed formulation which showed less disintegration and fast drug
release as compared to marketed formulation. Thus, the fast dissolving tablets were
successfully formulated to obtain less disintegration time and fast drug release.
