Brazilian Journal of Pharmaceutical Sciences
versión On-line ISSN 2175-9790
JAGDALE, Swati Changdeo; GAWALI, Vaibhav Uttam; KUCHEKAR, Bhanudas Shankar y CHABUKSWAR, Aniruddha Rajaram. Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride. Braz. J. Pharm. Sci. [online]. 2011, vol.47, n.4, pp.907-916. ISSN 2175-9790. http://dx.doi.org/10.1590/S1984-82502011000400028.
Diltiazem hydrochloride is a calcium channel blocker generally indicated for the treatment of angina and hypertension, and it is extensively metabolized due to the hepatic metabolism. Formulation of diltiazem hydrochloride into an oro-dispersible dosage form can provide fast relief with higher bioavailability. The bitter taste of the drug should be masked to formulate it in a palatable form. In the present work, an attempt was made to mask the taste by complexation technique, with a formulation into an oro-dispersible dosage form, using superdisintegrants Doshion P544, crospovidone (CP) and sodium starch glycolate (SSG). The complexes of diltiazem hydrochloride with β-CD (1:1 molar ratio) were prepared by kneading, co-evaporation, co-grounding, freeze-drying and melting methods. Phase solubility showed stability constant 819.13M-1. Prepared inclusion complexes were evaluated for taste masking and characterized by I.R, XRD, DSC. Using the drug β-CD complex, oro-dispersible tablets were prepared and evaluated for hardness, friability, weight variation, thickness, disintegrating time (DT), dissolution rate and taste. Formulations with 4 % Doshion, 8 % CP and 4 % SSG showed DT of 0.54, 0.35 and 1.23 minutes, respectively.
Palabras clave : Diltiazem hydrochloride; Cyclodextrin; Drugs [taste-masking]; Freeze-drying.