Solid Dispersions of Famotidine: Physicochemical Properties and In Vivo Comparative Study on the Inhibition of Hyperacidity
- At August 09, 2020
- By Yori Yuliandra
- In Scientific Paper
44
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.
Read More»Cocrystal of Ibuprofen–Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation
- At July 11, 2018
- By Yori Yuliandra
- In Scientific Paper
- 45
Yori Yuliandra, Erizal Zaini, Syofyan Syofyan, Wenny Pratiwi, Lidiya Novita Putri, Yuti Sahra Pratiwi, Helmi Arifin
ABSTRACT: Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phase of ibuprofen-nicotinamide, determine the solubility, and evaluate its in vivo analgesic activity. The cocrystal of ibuprofen-nicotinamide was prepared by a slow evaporation method. The solid-state characterization was conducted by powder X-ray diffraction (PXRD) analysis, differential thermal analysis (DTA), and scanning electron microscopy (SEM). To investigate the in vivo analgesic activity, 28 male Swiss-Webster mice were injected with acetic acid 0.5% following oral administration of intact ibuprofen, physical mixture, and its cocrystalline phase with nicotinamide (equivalent to 26 mg/kg ibuprofen). The number of writhes was counted, and pain inhibition was calculated. All data were analyzed with one-way ANOVA followed by Duncan’s Multiple Range Test (95% confidence interval). The results revealed that a new cocrystalline phase was successfully formed. The solubility testing showed that the cocrystal formation enhanced the solubility significantly as compared with the physical mixture and intact ibuprofen. A significant increase in the analgesic activity of cocrystal ibuprofen-nicotinamide was also confirmed.
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