Melatonin Orally Disintegrating Tablets Developed Ba Luosha Star Tablets Healthy Human Pharmacokinetic Study

[Objective] : To prepare orally disintegrating tablets (ODTs) of melatonin and to provide a more convenient and effective medicine.[Method]: The hygroscopicity of disintegrants was measured by a self-made apparatus for measurement of water uptake.The prescription was optimized by means of orthogonal design and the melatonin ODTs were prepared by press the powder directly. The angle of repose and compressibility were used to investigate the flowability of powder. The disintegration time both in vivo and in vitro, hardness and uniformity of content of melatonin ODTs were examined. The dissolution rate of drug was compared with that of the conventional tablets. The stability of tablet was determined by a homoiothermic acceleration test. The plasma concentration of melatonin of 6 Beagle dogs was determined by HPLC and the pharmacokinetic parameters were caculated with drug and statistic (DAS) softerware after administered random crossover with single dose of 6mg conventional tablets or orally disintegrating tablets.[ Result ] : The evaluation of microcrystalline cellulose(MCC), crospolyvinylpyrrolidone (PVPP ) and effervescent indicated that it can achieve good hydrophilism when the content of MCC was between 5%-8%, PVPP between 5%-8%, effervescent between 5%-10%. The optimized formulation was MCC in 6%, crospolyvinylpyrrolidone in 8%, effervescent in 18%.The powder's angle of repose of optimal prescription was 32.15±2.42° and compressibility was 28.45±3.17%. The disintegration time both in vivo and in vitro was within 30 seconds. Either hardness or uniformity of content of melatonin ODTs was coincided with the requirement of Chinese Pharmacopoeia 2005. The dissolution of ODTs was more quickly than that of commom tablets. There are no difference of appearance, content, disintegration time and dissolution of melatonin ODTs after three month by a homoiothermic acceleration test. The C_max of the ODTs and common tablets of melatonin was...