The study was carried out to develop useful formulation for omeprazole(OMP) through OMP-ethylendiamine complex(OMPED), and the pharmaceutical properties of formula were tested to find out the difference in vivo behaviors of formulations between
the
free
and complexed OMP. Oral and suppository dosage forms were also formulated and the dissolution profiles and pharmacokinetic parameters were measured to observe the difference in bioavailability between the free and complex form, and the
correlation
between dissolution rate and bioavailability was evaluated. The results are summarized as follows. In the case of formulation for oral administration, the release of OMP from enteric OMPED pellets was found satisfactory to the requirement
standard
and
no decomposition of OMP in the pellets was found in acidic solution. Therefore the enteric OMPED pellets are anticipated to be a stable formulation. The releaseof OMP from OMPED tablet with chitosan as excipient and coated with cellulose acetate
phthalate was found to be significantly retarded. The results of bioavailability test for OMP and OMPED tablets with lactose-excipient showed that the AUC value of OMP tablet was 116.89㎍. min/ml, that of OMPED tablet was 161.10㎍. min/ml,
respectively.
The reason why was though that OMP decomposes more readily in body than OMPED, and the AUC of the tablet with chitosan-excipient and coated with cellulose acetate phthalate was most enhanced. In the case of bioavailability for suppositories with
OMP,
OMP-β -cyclodextrin complex and OMPED, the AUC of OMPED suppository was most increased. From the above results, it is thought that the more stable and bioavailable oral or rectal dosage forms could be developed by using the OMPED as a potential
OMP
complex.
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