[Preparation of the 5-Fu floating sustained release tablet for gastric retention].
OBJECTIVE
To develop a pH independent floating sustained release tablet for gastric retention using 5-Fluorouracil (5-Fu) as a model drug.


METHODS
According to the theory of the Hydro-dynamically Balanced System, the granules for the floating and drug loading layer were prepared separately and pressed together to make two-layer floating tablets for gastric retention. The floating kinetics indexes were measured and the data about drug release studied with media of different pH values.


RESULTS
An excellent floating ability was observed in the media of different acidity for the gastric retentive tablet prepared according to the optimum formulation. The in vitro drug release can be modified by the regulation of the formulation ingredients. At the rotating speed of 100 r/min and in 0.1 mol/L HCl, the drug release was found to conform to first-class dynamics rule.


CONCLUSIONS
The two-layer floating tablet made in this experiment,whose floating ability is independent of the gastric acidity variation, is of the possibility to be used for the auxiliary treatment of gastric carcinoma because of its prolonged gastric retention.
Wei
Zhen-ping
ZP
Department of nutrition, Peking University College of Public Health, Beijing 100083, China.
Huang
Lei
L
Han
Jing
J
Li
Yong
Y
D000964:Antimetabolites, Antineoplastic / Q000737:chemistry* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods*; D015195:Drug Design; D005472:Fluorouracil / Q000737:chemistry* / Q000493:pharmacokinetics; D005750:Gastric Juice / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D013274:Stomach Neoplasms / Q000188:drug therapy; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods
D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D013607:Tablets; D005472:Fluorouracil