Journal of Bioequivalence & Bioavailability

Bioavailability enhancement of sulpiride from a gastro retentive drug delivery system in rabbits

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Kaleem Ullah, Yusrida Darwis, Peh Kok Yang, Mallikarjun Chitneni and Jiyauddin Khan

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

The present study was aimed to develop, validate a simple reversed-phase high performance liquid chromatographic method
for determination of sulpiride in plasma and also to evaluate in vivo performance of the optimized gastroretentive formulation
in comparison with a non-gastroretentive reference product (Dogmatil®) using rabbits as an animal model. The HPLC system was
operated at an excitation and emission wavelengths of 300 nm and 365 nm, respectively with the gain was set at 4 and sensitivity
at medium. The mobile phase was consisted of 0.01 M phosphoric acid, acetonitrile and methanol (84:12:4, v/v) with addition of
Triethylamine (0.15%v/v). The mobile phase pH was adjusted to 6 by using glacial acetic acid. The mobile phase was isocratically
pumped at a flow rate of 1 mL/min. The analytical column Luna C18 (5 μm, 250 x 4.6 mm ID, Phenomenex, USA) fitted with a
refillable guard column (Upchurch Scientific, Oak Harbour, WA, USA) packed with Perisorb RP-18 (30-40 μm, pellicular) was used
for chromatographic separation. The mobile phase was filtered under vacuum through 0.45 μm nylon membrane filter (Whatman
International, England) and degassed before used. The calibration curve was linear in the range of 15 to 4000 ng/ml with
correlation coefficient (r) of 0.9999 (±0.0001). The intra-day accuracy ranged from -4.59% to 12.91% with a precision from 1.42% to
6.79%. The inter-day accuracy ranged from -1.86% to 6.29% with a precision from 4.21% to 13.91%. The extraction recovery values
were found to be 95.99 ± 9.44%, 96.12 ± 11.94% and 93.49 ± 5.13%, with precision of 9.84%, 12.42% and 5.49% respectively. The mean
recovery for internal standard (metoclopramide) was 90.28 ± 3.95%. The values of accuracy, precision and recovery obtained were
within the acceptable limits as proposed by USFDA Bioanalytical Guidelines. For in vivo pharmacokinetics study a balanced twoway
crossover design was used using 6 rabbits. The optimized formulation had higher Tmax, andAUC0-∞ values but lower Cmax value
than non-gastroretentive reference product (Dogmatil® capsule). The bioavailability of sulpiride in the optimized gastroretentive
dosage form was 2.20 times higher than the non-gastroretentive reference product (Dogmatil® capsule). In addition, the amount of
drug released in vitro was correlated with the amount of drug absorbed in vivo.