Formulation of stomach-specific floating microparticles of nizatidine and their radiographic evaluation

Nizatidine is an anti-secretogogue and a gastroprotective drug with a half-life of 1-2 h and is well absorbed in the stomach. This study aimed to optimize the process and develop floating microparticles of nizatidine that are based on low methoxyl pectin. Oil-in-oil dispersion method and Taguchi orthogonal array design were employed, and the prolonged residence time of the microparticles in the stomach was demonstrated. The constraints for independent variables, viz. A-polymer, B-internal solvent volume, C-surfactant, D-stirring rate and E-stirring time were set to generate the experimental runs. Particle size, percentage yield, micromeritic properties, entrapment efficiency, in vitro buoyancy and in vitro release were characterized. Surface morphology, zeta potential, in vitro release kinetics and in vivo floating performance of the optimized formulation was examined. The microparticles were free-flowing, irregular in shape and had a mean particle size distribution of 73-187 µ. Low methoxyl pectin played a predominant role in achieving buoyancy and optimum gastric retention for the modified release of the drug, suggesting Korsmeyer-Peppas model as the possible release mechanism. In vivo radiographic study in rabbits revealed that the drug was retained in the stomach for a period of 6 h. These results indicate that nizatidine floating microparticulate system provides modified drug release for the effective treatment of gastric ulcer

A case of nizatidine-induced immediate hypersensitivity

Nizatidine is a histamine H₂ receptor antagonist that inhibits stomach acid production and is commonly used in the treatment of peptic ulcer and gastroesophageal reflux. H₂ receptor antagonists are typically well tolerated, and hypersensitivity reactions are rare. A 19-year-old woman developed urticaria 30 minutes after taking a drug containing nizatidine. Allergic reactions to nizatidine were confirmed via skin prick test, which also revealed cross-reactions to ranitidine. We believe that this is the first case report on immediate hypersensitivity to nizatidine in Korea.

A case of nizatidine induced cholestatic hepatitis / 대한내과학회지

Histamine H2-receptor antagonists are commonly used in many clinical conditions, and their hepatotoxicity has been reported occasionally.However, cholestatic hepatitis induced by nizatidine is very rare. Here, we report a young female patient with severe cholestatic hepatitis associated with nizatidine use. She had taken nizatidine to manage asymptomatic reflux laryngitis by an otonasolaryngology doctorfor about 20 days. After about 15 days of nizatidine administration, jaundice developed and continued for more than2 months withmaximal serum total bilirubin reaching 17.5 mg/dL, in spite of the discontinuation of medication. Liver specimen obtained by needle biopsy revealed severe centrilobular cholestatic hepatitis. Her liver function improved slowly and serum total bilirubin decreased down to 1.7 mg/dL after months later from the development of jaundice. As far as our knowledge, this is the second case of nizatidine- induced cholestatic hepatitis reported in the literature.