Formulation, optimization, and evaluation of raft-forming formulations containing Nizatidine

Abstract

Objective: The main objective of this research is to formulate, optimize, and evaluate raft-forming chewable tablets of Nizatidine. Various raft-forming agents were used in preliminary screening. Sodium alginate showed maximum raft strength, so tablets were prepared using sodium alginate as the raft forming agent, along with calcium carbonate (CaCO₃) as antacid and raft strengthening agent, and sodium bicarbonate (NaHCO₃) as a gas generating agent.

Research design and methods: Raft forming chewable tablets containing Nizatidine were prepared by direct compression and wet granulation methods, and evaluated for drug content, acid neutralization capacity, raft strength, and in-vitro drug release in 0.1 N HCl. Box–Behnken design was used for optimization.

Results: Two optimized formulations were predicted from the design space. The first optimized recommended concentrations of the independent variables were predicted to be X₁ = 275.92 mg, X₂ = 28.60 mg, and X₃ = 202.14 mg for direct compression technique and the second optimized recommended concentrations were predicted to be X₁ = 253.62 mg, X₂ = 24.60 mg, and X₃ = 201.77 mg for wet granulation technique. Optimized formulations were stable at accelerated environmental testing for six months at 35 °C and 45 °C with 75% relative humidity. X-Ray showed that the raft floated immediately after ingestion and remained intact for ∼3 h.

Conclusion: Raft was successfully formed and optimized. Upon chewing tablets, a raft is formed on stomach content. That results in rapid relief of acid burning symptoms and delivering the drug into systemic circulation with enhanced bioavailability.

Keywords:

• Raft forming agents
• chewable tablets
• optimization
• texture analyzer
• raft strength
• acid neutralization capacity
• x-ray
• bioavailability of Nizatidine

Acknowledgements

I would like to give a privilege to all members of the faculty of pharmacy, Al-Azhar University for providing excellent facilities and deep support for carrying out the research work. I would also present a token of thanks to my colleague as this work would not have been possible without their keen interest and support. The author would also thankful to parents and dear friends.

Disclosure statement

No potential conflict of interest was reported by the authors.