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Development of novel spray coated soft elastic gelatin capsule sustained release formulations of nifedipine, bioavailability and bioequivalence of verapamil HCL controlled release formulations, pharmacokinetics of terbinafine after single oral doses in raptorsFahmy, Sahar Abd El-Sattar 08 July 2004 (has links)
This dissertation describes the development of a new sustained release
formulation of nifedipine. The new formulation was developed by coating
commercially available immediate release soft elastic gelatin capsules using a spray
coating technique with two different polymeric combinations. Dissolution studies
were conducted and showed that controlled release of nifedipine was obtained by
increasing the ratio of the water insoluble polymer in the coat and increasing the
percent weight gain of the coating. Simulated plasma concentration versus time
profiles after administration of 30 mg dose of selected formulations showed a
prolonged nifedipine release with concentrations above the minimum effective
concentration for up to 12 hours.
Bioavailability and bioequivalence of tableted test formulation of verapamil
HCL was determined in 8 volunteers and compared to Covera HS® under fed and
fasting conditions. The 90% confidence intervals for individual percent ratios of the
Cmax, AUC₀₋₅₈ and AUC₀ were not within the range of 80 - 125% in both fed fasted states, suggesting that these formulations are not bioequivalent. the bioavailability of verapamil from the new formulation was higher state but this effect was not statistically significant.
Pharmacokinetics of terbinafine administered orally at single doses of 15,
30, 60 and 120 mg were determined in raptors to recommend an appropriate dosing
scheduled for terbinafine in the treatment of Aspergillosis. Calculation of steady
state trough terbinafine plasma concentration after administration of daily doses of
15 or 30 mg/day showed that 30 mg daily dose of terbinafine administered orally
in raptors produces a steady state trough terbinafine plasma concentration above the
minimum inhibitory concentration (MIC) of(0.8 1.6) µg/ml against aspregillus
fumigatus. From the data, 30 mg per day oral dose of terbinafine should be the
recommended dose for treatment of aspergillosis in raptors. Approximate
pharmacokinetic linearity of terbinafine was demonstrated for AUC[subscript 0-t] in the dose
range of 15 120 mg while non-linearity for Cmax in the same dose range was
demonstrated using the power model. / Graduation date: 2005
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