Soluplus ® based solid dispersion as fast disintegrating tablets: a combined experimental approach for enhancing the dissolution and antiulcer efficacy of famotidine.

Autor: Basha M; Department of Pharmaceutical Technology, National Research Centre, Cairo, Egypt., Salama A; Department of Pharmacology, National Research Centre, Cairo, Egypt., Noshi SH; Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Cairo, Egypt.
Jazyk: angličtina
Zdroj: Drug development and industrial pharmacy [Drug Dev Ind Pharm] 2020 Feb; Vol. 46 (2), pp. 253-263. Date of Electronic Publication: 2020 Jan 23.
DOI: 10.1080/03639045.2020.1716376
Abstrakt: Famotidine (FM) is considered among the first-line therapy for treatment of gastric ulcers; however, its poor aqueous solubility resulted in low bioavailability and limited therapeutic efficacy. Therefore, fast disintegrating tablet (FDT) incorporating FM solid dispersion was developed in a combined formulation approach for efficient treatment of ulcers. Within the investigated polymers, solid dispersions were prepared using the novel copolymer, Soluplus ® (SP) by kneading and freeze-drying techniques at various FM:SP ratios. FM solid dispersion prepared at 1:10 ratio using freeze drying (FM-SP10) manifested the highest saturation solubility, having smooth porous surface with the complete conversion of FM to the amorphous form. FDTs of FM-SP10 was produced by direct compression using three ready-to-use excipients; F-melt, Pearlitol Flash, and Fujicalin. All tablets showed adequate thickness, diameter, weight variation, drug content, and friability (<1%). Fujicalin-FDTs (FM-FDT-FU) exhibited the shortest disintegration time with almost complete dissolution of the drug (>95%) within 30 min. It also revealed remarkable antiulcerogenic effect on ethanol induced gastric ulcers in terms of ulcer and protection indices compared to the market product. Pretreated rats with FM-FDT-FU demonstrated normal gastric area with the absence of edema and leucocytes infiltration, supported by the histological examination. FM-FDT-FU administration protected the stomach from oxidative damage and severe inflammatory response via the significant increase of glutathione level and the decreased levels of nitric oxide, interleukin and cyclooxygenase. Thus, the present study provides a promising dosage form of FM characterized by superior antiulcerogenic potential with desired tableting properties.
Databáze: MEDLINE
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