Design and Optimization of Cyproheptadine Hydrochloride Fastdissolving Tablet Using Design of Experiment

Abstract

Aim: The aim of the current research project was to formulate and optimize a fast-dissolving tablet containing
the antihistamine drug cyproheptadine hydrochloride (HCl), which is frequently used to treat allergies and other
conditions. Materials and Methods: The direct compression method was used to prepare the fast-dissolving
tablets of cyproheptadine HCl. Fourier-transform infrared spectroscopy was employed to evaluate the blend’s
compatibility and ensure the stability of the active ingredient. The effect of two critical formulation variables:
The amount of super-disintegrant (X1) and amount of effervescent agent (X2) – on the dependent variables:
disintegration time (DT) (Y1), percentage drug release at 5 min (Y2), and percentage drug release at 10 min (Y3)
– was examined using a two-factor, two-level Central Composite Design. Results: Design-Expert® software by
Stat-Ease 360 trial version 13.0 was used to study the effect of formulation variables on dependent variables.
Nine formulations were produced and assessed for several physicochemical characteristics as well as in vitro drug
release. The data were analyzed using Response Surface Methodology and Analysis of variance. In comparison
to other formulations, the software suggested an optimized formulation (CP OPT) with 5 mg of super-disintegrant
and 49.572 mg of effervescent agent with shorter DT and a faster drug release, with over 85% of the drug being
released in <10 min. Conclusion: The use of effervescence method with sodium starch glycolate, sodium
bicarbonate, and other excipients resulted in fast dissolution of the drug in the tablet formulation. The effervescent
technique enhanced in masking the bitter taste of the drug and it offered an effective approach for improving
patient compliance and enhancing the therapeutic effects of cyproheptadine HCl through the development of fastdissolving
tablets with desired properties.