Pharmacokinetics of a New Tetramethylpyrazine Analogue CXC195 in Rats.

Pharmacokinetics of a New Tetramethylpyrazine Analogue CXC195 in Rats.

Drug Res (Stuttg). 2013 Mar 28;
Wei C, Kong L, Wei X, Chen L, Liu X, Zhang X, Liu X, Liu H

To investigate the pharmacokinetical characteristics of a new neuroprotective drug CXC195 after intraperitoneal injection in rats.A single 10 mg · kg-1 of CXC195 was intraperitoneally injected to 8 rats after fasting overnight, respectively. 500 microliters of blood samples were collected at scheduled time before and after administration. CXC195 in rats’ plasma was separated on a Diamonsil C18 column (150 mm×4.6 mm, 5 ?m), eluted using methanol – 0.05 mM NaH2PO4 solution (86:14, v/v) as mobile phase, and detected by UV detector at wavelength of 278 nm. The plasma concentration of CXC195 was determined by established HPLC method after disposition and its pharmacokinetic parameters were analyzed and evaluated by Drug and Statistic (version 2.0).The Cmax, Tmax, t1/2, AUC0-8, AUC0-?, MRT0-8, MRT0-?, CL/F and V/F of CXC195 after-single dose intraperitoneal injection of 10 mg · kg-1 CXC195 were 12.37±5.35 ?g · mL-1, 0.5±0.21 h,4.24±2.43 h, 24.89±8.32 ?g · mL-1 · h, 28.57±9.66 ?g · mL-1 · h, 2.00±0.53 h, 2.93±0.75 h, 1.4±0.73 L · h-1 and 1.16±0.68 L.The established HPLC method was sensitive, rapid, and suitable for CXC195 pharmacokinetic study. The procedure of CXC195 in rat was fit to double-compartmental model with lag time of 0.13 h. HubMed – drug


Bioequivalence Study of 2 Formulations of Film-coated Tablets containing a Fixed Dose Combination of Bisoprolol Fumarate 5 mg and Hydrochlorothiazide 6.25 mg in Healthy Subjects.

Drug Res (Stuttg). 2013 Mar 28;
Tjandrawinata RR, Setiawati E, Yunaidi DA, Santoso ID, Setiawati A, Susanto LW

The present study was conducted to compare the bioavailability of 2 formulations of fixed-dose combination of bisoprolol fumarate 5 mg and hydrochlorotiazide (HCT) 6.25 mg film-coated tablet (test and reference formulations).This study was a randomized, single-blind, 2-period, 2-sequence cross-over study which included 18 healthy adult male and female subjects under fasting condition. The pharmacokinetic parameters, AUCt, AUCinf, Cmax, tmax, and t½ were determined based on the concentrations of bisoprolol (CAS 66722-44-9) and HCT (CAS 58-93-5), using ultra-performance liquid chromatography with tandem mass spectrometer detector (UPLC-MS/MS). In each of the 2 study periods (with a washout of 1 week) a single dose of test or reference product was administered.The geometric mean ratios (90% CI) of the test drug/reference drug for bisoprolol were 97.22% (93.75-100.83%) for AUCt(0-48), 97.20% (93.97-100.54%) for AUCinf, and 100.36% (93.83-107.34%) for Cmax; while those for HCT were 93.22% (84.72-102.57%), 93.39% (85.43-102.10%) and 99.39% (85.45-115.61%), for AUCt(0-24), AUCinf, and Cmax, respectively. The differences between the test and reference drug products for tmax values of bisoprolol as well as t½ values of both bisoprolol and hydrochlorothiazide were not statistically significant; yet, the difference was statistically significant for the tmax values of hydrochlorothiazide. There was no adverse event encountered during this bioequivalence test.It was concluded that the 2 formulations of fixed dose combination of bisoprolol fumarate 5 mg and hydrochlorotiazide (HCT) 6.25 mg film-coated tablet (the test and reference products) were bioequivalent. HubMed – drug


Effects of Andrographolide on the Pharmacokinetics of Aminophylline and Doxofylline in Rats.

Drug Res (Stuttg). 2013 Mar 28;
Li XP, Zhang CL, Gao P, Gao J, Liu D

Andrographolide, which is one of the main pharmaceutical ingredients in traditional Chinese medicine Andrographis paniculata, can clear heat, detoxify human body, cool blood and reduce swelling, etc. Respiratory tract infectious diseases have been treated with the combination of andrographolide and theophyllines clinically. As andrographolide inhibits the CYP1A2 activity in vitro, it potentially interacts with theophyllines that are mainly metabolized by CYP1A2. Therefore, we herein studied the effects of andrographolide on the pharmacokinetics of aminophylline and doxofylline in rats. The blood drug concentrations of aminophylline, doxofylline and its metabolite theophylline were determined by HPLC. The theophylline AUC(0-t) was significantly elevated confronting the combination of andrographolide and aminophylline compared to that of the control group (P<0.05). Meanwhile, when only aminophylline was used, the theophylline clearance rate was significantly higher than those in the case of combination (P<0.05). The pharmacokinetics parameters of doxofylline and its metabolite theophylline in the individual administration group showed no significantly different from that combined with andrographolide. The results suggest that andrographolide and aminophylline should not be simultaneously administered because the former may raise the risks of side effects by inhibiting the clearance of the latter. In contrast, it is more secure to combine doxofylline with andrographolide owing to the almost intact pharmacokinetics. HubMed – drug


Gastric bezoars – diagnostic and therapeutic challenges.

J Gastrointestin Liver Dis. 2013 Sep; 22(1): 111
Mihai C, Mihai B, Drug V, Cijevschi Prelipcean C

HubMed – drug