Solid Dispersions of Famotidine: Physicochemical Properties and In Vivo Comparative Study on the Inhibition of Hyperacidity

Yori Yuliandra, Lili Fitriani, Robby Kurniawan, Fuji Yasardi, Erizal Zaini

Abstract

Famotidine is a potent histamine 2 antagonist used in the treatment of gastric acid overproduction. Famotidine belongs to Class IV in Biopharmaceutics Classification System (BCS) which has low solubility and membrane permeability. The purpose of this study was to compare the solubility and dissolution profile of solid dispersions (SDs) of famotidine with mannitol (SD‐MAN) and with hydroxypropyl methylcellulose (SD‐HPMC), and to comparatively study their in vivo effectiveness against hyperacidity. Famotidine SDs were prepared by cogrinding technique with the respective carriers in various ratios and grinding time. SDs with the best solubility underwent dissolution rate studies, solid‐state characterization, and in vivo efficacy evaluation. The in vivo evaluation was conducted in Sprague Dawley rats receiving famotidine formulations in the dose equivalent to 12 mg/kg of famotidine. The study found that the famotidine SDs could greatly improve the solubility of famotidine by 100.61 and 120.91% for SD‐MAN and SD‐HPMC, respectively. The solid‐state characterization revealed the decrease in crystallinity degree of famotidine solid dispersion systems. The comparative study on the in vivo efficacy of famotidine SDs showed that SD‐HPMC was significantly better than SD‐MAN. This study concludes that SDs can improve the solubility and in vivo effectiveness of famotidine in overproduction of gastric acid.

Keywords: Absorption; Famotidine; In vivo; Polymers; Solid dispersion