Formulation Study for Lansoprazole Fast-disintegrating Tablet. I.Effect of Compression on Dissolution Behavior

Formulation Study for Lansoprazole Fast-disintegrating Tablet. II. Effect of Triethyl Citrate on the Quality of the Products

“…Effect of Triethyl Citrate on the Quality of EntericCoated Microgranules In our previous study, 1) four different formulations of enteric-coated microgranules containing increased concentrations of triethyl citrate were prepared to investigate the effects of the triethyl citrate concentration on the damage to the enteric layer during the compression process. When we evaluated the unpleasant bitter taste of these enteric-coated microgranules in a sensory evaluation, it was found that the unpleasant bitter taste tended to increase with the increase in the triethyl citrate concentration.…”

“…Triethyl citrate plays an important role in the formulation of enteric-coated microgranules to reduce the brittle character of methacrylic acid copolymer dispersion, 1) but it has an unpleasant bitter taste and is especially incompatible with lansoprazole. It was found that triethyl citrate adversely affects the taste and the stability of lansoprazole.…”

“…The first issue is damage to the enteric layer during the compression process, because the enteric-coated microgranules are compressed with a tablet press. In our previous study, 1) it was clarified that sufficient flexibility of the enteric layer was achieved by the optimized combined ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion and adding the optimized concentration of triethyl citrate to reduce the damage during the compression process. The second issue is the taste of LFDT.…”

Formulation Study for Lansoprazole Fast-disintegrating Tablet. III. Design of Rapidly Disintegrating Tablets

“…Previously we reported the design of the enteric-coated microgranules. 21,22) We had to resolve the three issues of damage to the enteric layer during the compression process, the unpleasant bitter taste of triethyl citrate, and the poor stability of lansoprazole in the enteric-coated microgranules. Finally we developed enteric-coated microgranules comprising seven layers: 1) core, 2) active compound layer, 3) intermediate layer (stabilization of lansoprazole), 4) first enteric layer (stabilization of lansoprazole), 5) second enteric layer (reduction of damage to the enteric layer during the compression process), 6) third enteric layer (masking the unpleasant bitter taste), and 7) overcoating layer (preventing agglomerates of enteric-coated microgranules during the drying process) with improved oral acceptance, sufficient flexibility of the enteric layers against compression, and improved stability of lansoprazole.…”

“…LFDT consist of enteric-coated microgranules and inactive granules. In our previous studies, 21,22) we reported the design of multifunctional enteric-coated microgranules with improved oral acceptance, sufficient flexibility of the enteric layers against compression, and improved stability of lansoprazole. In the design of the inactive granules, it was necessary to find a suitable binder with excellent compactibility and a suitable rapid disintegrant in saliva.…”