Development of fast disintegrating compressed tablets using amino acid as disintegration accelerator: evaluation of wetting and disintegration of tablet on the basis of surface free energy.
A fast disintegrating compressed tablet was formulated using amino acids, such as L-lysine HCl, L-alanine, glycine and L-tyrosine as disintegration accelerator. The tablets having the hardness of about 4 kgf were prepared and the effect of amino acids on the wetting time and disintegration time in the oral cavity of tablets was examined on the basis of surface free energy of amino acids. The wetting time of the tablets increased in the order of L-lysine HCl, L-alanine, glycine and L-tyrosine, whereas the disintegration time in the oral cavity of the tablets increased in the order of L-alanine, glycine, L-lysine HCl and L-tyrosine. These behaviors were well analyzed by the introduction of surface free energy. When the polar component of amino acid was large value or the dispersion component was small value, faster wetting of tablet was observed. When the dispersion component of amino acid was large value or the dispersion component was small value, faster disintegration of tablet was observed, expect of L-tyrosine tablet. The fast disintegration of tablets was explained by the theory presented by Matsumaru.
Fukami
Jinichi
J
Kyoto Pharmaceutical Industries, Ltd., Nishinokyo, Japan.
Ozawa
Asuka
A
Yoshihashi
Yasuo
Y
Yonemochi
Etsuo
E
Terada
Katsuhide
K
D000328:Adult; D000596:Amino Acids / Q000737:chemistry*; D002482:Cellulose / Q000031:analogs & derivatives; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005079:Excipients; D005998:Glycine / Q000737:chemistry; D006244:Hardness; D006801:Humans; D009055:Mouth; D010316:Particle Size; D011208:Powders; D012995:Solubility; D012997:Solvents; D013229:Stearic Acids; D013499:Surface Properties; D013607:Tablets
D000596:Amino Acids; D005079:Excipients; D011208:Powders; D012997:Solvents; D013229:Stearic Acids; D013607:Tablets; C031183:stearic acid; D002482:Cellulose; C008079:hydroxypropylcellulose; D005998:Glycine