Effect of polymers and excipients on the release kinetics, bioadhesion, and floatability of metronidazole tablet

Abstract

S tomach-specific floating tablet of metronidazole based on the buoyancy and bioadhesion concept was prepared with a purpose to retain the drug in stomach for longer duration and helps in releasing the drug in the antrum region of gastric mucosa, a safe heaven for Helicobacter pylori. This research work systematically studied the effects of various polymeric blends of bioadhesive polymers namely chitosan and carbopol 971P with low density polymer-methocel K100LV on the desired in vitro drug release profile in the stomach, buoyancy, swelling index, and mucoadhesion of tablet formulation. Chitosan and carbopol 971P concentration significantly influence the in vitro drug release and bioadhesion strength. An increase in buoyancy was observed with increase in Methocel K100LV concentration in the polymeric blend. The increase in buoyancy and drug release was obtained in the presence of microcrystalline cellulose, sodium bicarbonate, and sodium citrate. The optimum formulation provides desired high drug concentration (~35%) during 1 hour and sustained release up to 12 hours, following the Higuchi model. The mechanism of release of metronidazole from the floating bioadhesive tablets was anomalous diffusion transport. The studies indicated successful formulation of gastroretentive compressed tablet with excellent controlled release, mucoadhesion, and hydrodynamic balance.

Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of H. pylori: Preparation and In Vitro Characterization

“…The obtained results were in the range of 95.21–99.03% for metronidazole. Our results are in agreement with previous reported findings [ 7 , 19 ].…”

“…The final blend of mixture was again passed through a sieve number 40 followed by thorough mixing for 10 min, and compressed into tablets by employing a single punch tablet machine (Erweka-Apparatebau compression machine type T B-24). Tablet hardness was kept constant at 6.5 ± 0.33 kg/cm 2 [ 7 ].…”

“…It undergoes absorption in the stomach and possesses pH-independent effects [ 5 , 6 ]. Conventionally, metronidazole exhibits a rapid and almost complete absorption when given orally [ 7 ].…”

Formulation and Optimization of Immediate Release Cajanus Cajan Starch-Based Tablets Containing Metronidazole

“…Also, few researchers had declared that Cajanus cajan contains high carbohydrate sources, making it a prospective origin for starch. 5 Metronidazole is a nitroimidazole compound, 10 used widely as an antibiotic against anaerobes, 11 and for treatment of infection caused by protozoa. 12 The MNA powder possesses poor compression characteristics.…”

“…12 After the oral administration, the MNA absorbed wholly and rapidly. 10,12 Various binders and disintegrants sourced from natural origins such as starch, gum, and mucilage from cashew, Colocassia esculenta, Albelmoschus esculentus, Cochorus olitorious, Aloe barbadensis, Spondias purpurea, Brachystegia eurycoma, Irvingia gabonensis, Cyperus esculentus L., Triticum aestivum, cassava, and Zingiber officinale in addition to sodium starch glycolate, gelatin, microcrystalline starch methylcellulose and maize starch BP have been evaluated and used in metronidazole tablet formulation. [12][13][15][16][17][18][19][20][21][22][23][24][25] Most scientific experiments measure the effect of one or more factors (independent variables) on the experiment's outcome (response or dependent variable).…”