RESUMO
Aim To evaluate the pharmacokinetics and bioequivalence of two osmotic pump tablets of hydrochloride venlafaxine in Chinese healthy volunteers.Methods The fed test each enrolled twenty-six Chinese healthy volunteers in a randomized-sequence, open-label, two-period crossover single-dose oral test and reference preparations of hydrochloride venlafaxine extended-release tablets.The plasma concentrations of venlafaxine and its active metabolites O-desmethylvenlafaxine were determined by a validated liquid chromatography-tandem mass spectrometry(LC-MS/MS)method, and the pharmacokinetic parameters and bioequivalence of the two tablets were analyzed using PhoenixTM WinNonlin 6.4 software.Results The pharmacokinetic parameters of venlafaxine after single dose for the test and reference tablets were as follows: Cmax(58.50±19.47)vs(60.14±22.18)μg•L-1, AUC0-t(1 074.1±526.7)vs(1 057.9±539.7)μg•h•L-1, AUC0-∞(1 084.7±536.8)vs(1 067.8±554.0)μ g•h•L-1.The pharmacokinetic parameters of O-desmethylvenlafaxine were as follows: Cmax(101.63±29.64)vs(101.45±31.62)μg•L-1, AUC0-t(2 694.0±834.5)vs(2 702.9±946.4)μg• h•L-1, AUC0-∞(2 753.9±885.5)vs(2 753.2±988.4)μg•h•L-1.The 90% confidence intervals of the geometric mean ratios of Cmax, AUC0-t, AUC0-∞ for the test preparation and the reference preparationwere all within the equivalent interval of 80.00%-125.00%.Conclusion The test and reference preparations of hydrochloride venlafaxine extended-release tablets are bioequivalent in Chinese healthy volunteers under fed conditions.
RESUMO
Objective:To observe the effect of Taohong Siwu granule on dysmenorrhea rats. Method:Forty-eight healthy SD female rats were randomly divided into six groups: control group, model group, Taohong Siwu granule groups (18, 9, 4.5 g·kg-1) and Fuke Qianjin tablet group (0.08 g·kg-1). The rats were given Bugaorer (0.35 mg·kg-1) every day and ice-water bath for 8 minutes for 10 consecutive days. Oxytocin was injected intraperitoneally on the 11th day. The writhing reaction of rats was observed, and the effect of Taohong Siwu granules on hemorheology was measured. The levels of 6-ketoprostacyclin F1α(6-keto-PGF1α), thromboxane B2(TXB2), prostaglandinF2α（PGF2α）, PGE2 of rats were detected by enzyme-linked immunosorbent assay (ELISA). Ca2+ in uterine tissues was scanned by laser confocal microscopy. Result:Each dose of Taohong Siwu granule group reduced the number of writhing, the time of writhing and the incidence of writhing in dysmenorrhea rats, which were significantly lower than those in model group (P<0.05，P<0.01). Compared with the model group, high, medium and low-dose Taohong Siwu granules groups could reduce blood viscosity and plasma viscosity, and Taohong Siwu granules can significantly reduce the content of TXB2, Ca2+，PGF2α, and significantly increase the content of 6-keto-PGF1α，PGE2 (P<0.05，P<0.01). Conclusion:Taohong Siwu granule can significantly alleviate dysmenorrhea symptoms in rats. The mechanism may be correlated with the contents of 6-keto-PGF1α, TXB2 and PGF2α, PGE2 and Ca2+.
