Characterization and Improvement Dissolution Profile of the Hydrochlorothiazide-β-Cyclodextrin Inclusion Complex using Kneading Method

Abstract

Hydrochlorothiazide is a drug antihypertensives are classified into Biopharmaceutics Classification System (BCS) class IV, so required technique formulation to improve solubility, one of them with complex inclusion. The inclusion complex was prepared with a kneading method with a comparison amount of hydrochlorothiazide - β- cyclodextrin 1:1 (F1) mol, 2:1 (F2) mol, and a physical mixture prepared in a ratio of 1:1 mol. This research aims to see the effect of complex formation inclusion on dissolution rate and characteristics of physicochemical properties of hydrochlorothiazide. Complex inclusions formed are characterized by scanning electron microscopy (SEM), and infrared spectrophotometer (FT-IR). X-ray diffraction, differential scanning calorimetry (DSC), and dissolution profiles. Characterization of physicochemical results analysis diffraction X-rays show that powder complex inclusion hydrochlorothiazide with β-cyclodextrin experiences decline peak intensity approaches a more amorphous nature. Characterization results FT-IR analysis shows No interaction chemistry exists between hydrochlorothiazide β-cyclodextrin. SEM analysis shows morphology substance active Already coated with β- cyclodextrin. DSC analysis shows a decline in enthalpy of the complex inclusions that indicate physical interactions form a simple eutectic mixture. Research results show that complex inclusion hydrochlorothiazide - β-cyclodextrin can repair characteristic physicochemical and can increase hydrochlorothiazide dissolution profile in a way significant (p<0.05) compared with powder The physical mixture with the highest dissolution results was shown by the F1 inclusion complex (82.843 %).