This thesis describes evaluation of a novel self-sealing chewable sustained
release tablet that can maintain controlled release of drug regardless of compaction,
crushing, or chewing. The new formulation contains polyethylene oxide which
produces a sealant effect for cracks produced in the polymer coating during
compaction. Dissolution studies were conducted and showed that the controlled
release properties of the multiple-layered coated beads were present but decreased
upon compaction and crushing.
Itraconazole solid formulations were formulated using solid dispersion and
solvent/co-cosolvent techniques. Solid dispersion of itraconazole in polyethylene glycol 20000 (PEG 20000) with trisodium citrate gave higher rate of dissolution
than dispersion in PEG 20000 alone but didn't have as much effect as desired on
rate of drug dissolution. Neutralized acetic acid itraconazole loaded beads exhibited
the same in vitro and in vivo release patterns as Sporanox®.
Itraconazole liquid formulations were developed and evaluated.
Polyethylene glycol 400 (PEG 400) and acetic acid mixtures were found to be a
good cosolvent system to solubilize itraconazole and showed good physical
stability. Acetic acid, citric acid, and tartaric acid were studied to minimize the
amount of PEG 400 needed to produce 1% (w/v) itraconazole solution. Citric acid
alone or combined with other agents produced a good physically stable solution;
however, these solutions didn't have as much extent as desired on drug dissolution.
Bioavailability and bioequivalence of itraconazole capsule was determined
is 13 fasted human volunteers and compared to Sporanox®. The 90% confidence
intervals for individual percent ratios of the Cmax, AUC₀₋₇₂ and AUC0-inf were above
the range of 80 to 125%, suggesting that these formulations are not bioequivalent.
However, this new formulation significantly increased amount of itraconazole
absorbed and Cmax of itraconazole in plasma.
A novel controlled release tablet which releases a drug independently of pH
and paddle speed, following a lag time and with zero-order kinetics identically to
an osmotic pump but using a matrix tablet coated with a diffusional barrier
membrane was produced and evaluated. This new matrix tablet generates a diffusional barrier support platform on horizontal surfaces in situ and can be used
as an alternative to other zero-order release systems.
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