Abstract

Tmax (hours) after IV, IM, PO were 5.4(1.1), 5.1(0.7) and 5.8(1.2); Cmax (ng/ml) were 7.56(0.79), 7.21(0.66) and 7.26(0.03) and mean(SD) AUC0−∞ (ng·hr/ml) 147.6 (36.4), 126.6 (31.0) and 138.0 (36.1) were not significantly different (p = 0.518, p = 0.920, p = 0.368) respectively. However, the mean(SD) elimination halflife, for all were 28.6(10.4), 25.1(7.8) and 26.7(9.4) hrs and the mean(SD) percentage absolute bioavailability of 9-OHR for IM and PO of 90.10(30.70) vs 97.30(28.00) were not significant differently (p = 0.779, p = 0.388) respectively. All routes of risperidone administration were well tolerated. No clinical relevant changes in vital signs observed. Minor spontaneous reports were similar among 3 groups including sedation (p> 0.05). Discussion: Pharmacokinetic parameters predictive onset (Tmax&Cmax) for clinical effect reflects for IM and PO is slower than IV. Unless, otherwise overall pharmacokinetics parameters were not statistically different among all routes of administration. However, in our studies, LORS appear better Tmax and absolute bioavailabilty than earlier studies by Huang (1993) [3]. Conclusion: The pharmacokinetics investigation supports that intravenous administration and non-intravenous administration provided comparable bioavailability. SARI and LORS are well tolerated and worth consideration for clinical applications.

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