Formulation and Evaluation of Controlled-Release Diltiazem Hydrochloride Buccoadhesive Tablets

[摘要] Diltiazem HCl (DTZ) is a calcium channel blocker used in the treatment of hypertension and angina (variant & classical angina). Diltiazem HCl was selected as a model drug for investigation because of its suitable properties like half-life of 4.5 hrs, optimum partition coefficient (158) and molecular weight (450.98), was formulated onto buccoadhesive tablets to overcome the limitations in the currently available dosage and routes of administration which in sequence will increase patient’s compliance. Mucoadhesive buccal tablets of Diltiazem hydrochloride were prepared using carbopol-934, Sodium carboxy methyl cellulose (SCMC), Hydroxy propyl methyl cellulose (HPMC) and sodium alginate as mucoadhesive polymers. Ten formulations were developed with varying concentrations of polymers. Each formulated batch was subjected to various evaluation parameters. The physical appearance of buccal patch was examined by scanning electron microscopy. The release behavior was non-Fickian controlled by a combination of diffusion and chain relaxation mechanisms and best fitted zero-order kinetics. All tablets were acceptable with regard to thickness, weight variation, hardness, and drug content. The maximum bioadhesive strength was observed in tablets formulated with a NaCMC followed by CP and CP-NaCMC. Formulation F10 showed maximum release of 79% in 8hours. Formulation F8 showed maximum swelling index of 3.7 after 8hours. Formulation F10 follows zero order drug release. FTIR studies show no evidence on interaction between drug and polymers. The results indicate that suitable mucoadhesive buccal tablets with desired properties could be prepared. Key Words: Mucoadhesive, Buccal patch

[学科分类] 药理学