Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry® yellow 20A82938 on an industrial scale.

PURPOSE: The aim of this study was to formulate stable film-coated montelukast sodium (MS) tablets using Opadry(®) yellow 20A82938 (Montikast(®) tablets) and to evaluate their in vitro and in vivo release profile. METHODS: MS core tablets were manufactured using a direct compression method. Opadry yellow 20A82938 aqueous coating dispersion was used as the film-coating material. Dissolution of the film-coated tablets was tested in 900 mL of 0.5% sodium lauryl sulfate solution and the bioequivalence of the tablets was tested by comparing them with a reference formulation - Singulair(®) tablets. In vitro-in vivo correlation was evaluated. The stability of the obtained film-coated tablets was evaluated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines. RESULTS: The efficiency of the film coating was determined by subjecting the coated tablets to gastric pH and drug release was analyzed using high-performance liquid chromatography. The coated tablets had no obvious defects. MS release met the study criterion of not less than 80% dissolved after 30 minutes in 0.5% sodium lauryl sulfate solution. Statistical comparison of the main pharmacokinetic parameters clearly indicated no significant difference between test and reference in any of the calculated pharmacokinetic parameters. Level A correlation between in vitro drug release and in vivo absorption was found to be satisfactory. CONCLUSION: These findings suggest that aqueous film coating with Opadry yellow 20A82938 is an easy, reproducible, and economical approach for preparing stable MS film-coated tablets without affecting the drug-release characteristics.

Formulation and stability evaluation of extemporaneously prepared atenolol capsules from crushed atenolol tablets.

The purpose of this study was to formulate a 25-mg atenolol capsule starting from a commercial 100-mg atenolol tablet, given the fact that this strength is not available in Palestine and also because 50-mg atenolol tablets failed the splitting uniformity test of the European Pharmacopoeia, and to evaluate the chemical stability and dissolution behavior of the obtained capsules so as to ensure a high-quality product. A high-performance liquid chromatographic system was used for the analysis and quantification of atenolol in the samples studied. Samples of atenoIol for analysis were prepared as reported by the United States Pharmacopeia monograph. Disintegration and dissolution tests were performed according to the United States Pharmacopeia. The high-performance liquid chromatography assay indicated that the 25-mg atenolol capsules were stable for four months when stored at ambient temperature conditions. The disintegration time for all atenolol capsules was within the United States Pharmacopeia limits of 15 minutes. Atenolol release profile showed that approximately 90% of atenolol dissolved after 10 minutes. This study is important for patients who need to take one half of a 50-mg tablet, but for whom the splitting process doesn't give equal halves, and also for modifying the dose for patients with renal or hepatic problems. Therefore, it is possible for the community pharmacist to crush atenolol 100-mg tablets and refill them in new capsules with each containing a precise amount of atenolol, calculated according to body surface area and kidney and liver functions without affecting the chemical stability of the active ingredient nor its dissolution profile and also have a cost effective dosage form.