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The present study was carried out in three parts. Firstly, to
determine the solubility of cisapride powder in various pH value
of media at three different temperatures. The effects of various
surfactants on the solubility of the powder were also studied. A
reliable HPLC method for the determination of cisapride
concentration in solution was established.The evaluation on the
commercial products, cisapride tablets, was the second part. Two
generic tablets which were bioequivalent to the innovator's
product were studied for the general tablet properties, such as
disintegration time, hardness, friability, thickness, diameter,
uniformity of dosage units ( weight variation and content
uniformity ) and dissolution profile, then compared to those of
the innovator's product. The storage effects on these properties
were also determined.In the third part, the effects of various
disintegrants, disintegrant concentration and diluents on the
physical properties （disintegration time, hardness, friability,
thickness and diameter） and the release of cisapride tablet
were determined. A 23 full factorial design of experiments was
employed to evaluate the effects of the three factors on the
percentage release of cisapride；the subsequent data was
compared using analysis of variance ( ANOVA ). Furthermore, the
physical properties and dissolution pIt was found that cisapride
powder dissolved freely in 0.1N HCl and pH4.5 acetate buffer,
respectively but not in pH6.8 phosphate buffer. The solubility
of cisapride powder was increased by adding a surfactant to the
latter medium. Sodium lauryl sulfate was found to be the most
effective one. Temperature would have a greater influence on the
solubility of the cisapride powder for the lower pH medium.The
SUPAC-IR method showed that no similarity was found between the
innovator's product and the two respective generic products as
the ?2 values were smaller than 50.After storage for three
months at three different temperatures, the content of the
subsequent cisapride powder was decreased. The most serious
reduction was obtained at the highest temperature, 60℃. A
higher storage temperature also showed a more significant effect
on the properties of the commercial cisapride tablets.Both the
dissolution rate and amount release were poor for cisapride
tablets using either lactose or Emcompress per se as the
diluent. However, incorporation of a disintegrant in the tablet
formulation would markly increase the dissolution rate as well
as the percentage release of cisapride.The experimental design
study illustrated that the kinds of disintegrants, the
concentration of disintegrant and the kinds of diluents had
significant effects on the release percentage of cisapride
determined in two minutes, but had no significant interaction
between them.A cross-over comparison between the dissolution
profiles of the formulated cisapride tablets and the three
commercial products using the SUPAC-IR method produced some
informative results.
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