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

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.

Isomeric Coformer Responsive Conformational Adjustment to Recuperate Stability, Solubility, and In Vitro Permeation Behavior of Drug Molecular Salts

“…The chemical stability, aqueous solubility, and oral bioavailability enhancement of the drug have been studied by complex formation with carboxymethyl-β-cyclodextrin . Optional methods such as solid dispersion were employed to improve the FAM solubility, dissolution rate, and in vivo effectiveness against gastric fluid hyperacidity . Salt-forming agents such as salicylic acid can improve the drug solubility when compared to the parent drug, as demonstrated by Brittain .…”

“…25 Optional methods such as solid dispersion were employed to improve the FAM solubility, dissolution rate, and in vivo effectiveness against gastric fluid hyperacidity. 26 Salt-forming agents such as salicylic acid can improve the drug solubility when compared to the parent drug, as demonstrated by Brittain. 27 Following up, FAM-maleate salt and cocrystal of FAM with malonic acid were further studied and found to be stable and better soluble than the pure drug.…”

Facile Synthesis of Hollow Starch Nanoparticles for the Delivery of Piroxicam, a Poorly Water‐Soluble Drug

“…A variety of oral delivery systems have been used to solve this ongoing solubility challenge, such as inclusion complexes, [1] nanoparticles, [2] self‐emulsifying drug delivery systems (SEDDS), [3] and solid dispersions [4] . Among these systems, solid dispersions have emerged as a common and effective strategy for enhancing the delivery of poorly water‐soluble drugs [4,5] . Solid dispersions involve dispersing a poorly water‐soluble active ingredient in a hydrophilic carrier in the solid state [6] .…”

“…[4] Among these systems, solid dispersions have emerged as a common and effective strategy for enhancing the delivery of poorly water-soluble drugs. [4,5] Solid dispersions involve dispersing a poorly water-soluble active ingredient in a hydrophilic carrier in the solid state. [6] The proper selection of carriers is crucial for the properties of the resulting solid dispersion.…”