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. 2007 Mar 12;151(1):24–34. doi: 10.1038/sj.bjp.0707192

Table 3.

Pharmacokinetic parameters of DA-8159 and DA-8164 after single p.o. administration of DA-8159 at a dose of 30 mg kg−1 without and with simultaneous p.o. administration of terazosin at a dose of 5 mg kg−1 per day for 7 days, and of terazosin after p.o. administration of terazosin at a dose of 5 mg kg−1 per day for 7 days without and with simultaneous single p.o. administration of DA-8159 at a dose of 30 mg kg−1 to rats

Parameter DA-8159
 Parameter Terazosin
  Without terazosin With terazosin   Without DA-8159 With DA-8159
DA-8159     Terazosin    
 AUC (μg min ml−1) 137±12.5 134±20.7  AUC (μg min ml−1) 124±16.7 295±38.7a
 Terminal t1/2 (min) 310±78.1 289±98.0  Terminal t1/2 (min) 305±45.2 254±63.5
 CLR (ml min−1 kg−1) 2.25±2.73 1.57±2.05  CLR (ml min kg−1) 8.63±1.60 3.35±2.19a
 Cmax (μg ml−1) 0.336±0.0913 0.314±0.0753  Cmax (μg ml−1) 0.292±0.0713 0.722±0.193a
 Tmax (min) 45 (15–90) 30 (15–60)  Tmax (min) 120 (60–240) 45 (15–180)b
 Ae0–24 h (% of DA-8159 dose) 1.46±0.735 1.10±1.07  Ae0–24 h (% of terazosin dose) 22.2±5.38 24.7±10.3
 GI24 h (% of DA-8159 dose) 5.06±5.14 3.72±3.52  GI24 h (% of terazosin dose) 3.11±3.27 2.37±2.25
DA-8164          
 AUC (μg min ml−1) 132±26.0 123±20.7      
 Termianal t1/2 (min) 245±115 230±88.2      
 CLR (ml min−1 kg−1) 0.151±0.069 0.131±0.167      
 Cmax (μg ml−1) 0.294±0.101 0.307±0.100      
 Tmax (min) 210 (120–360) 180 (120–240)      
 Ae0–24 h (% of DA-8159 dose) 0.0730±0.0259 0.0754±0.0463      
 GI24 h (% of DA-8159 dose) 0.539±0.221 0.458±0.258      

Abbreviations: Ae0–24 h, percentage of dose excreted in 24 h urine; AUC, total area under the plasma concentration–time curve from time zero to time infinity; CLR, time-averaged renal clearance; Cmax, peak plasma concentration; GI24 h, percentage of dose recovered from the entire gastrointestinal tract (including its contents and feces) at 24 h; t1/2, half-life; Tmax, time to reach a Cmax.

Data are expressed as mean±s.d., (without terazosin, n=10; with terazosin, n=9 for DA-8159, without DA-8159, n=8; with DA-8159, n=9 for terazosin). Significant difference from without DA-8159,

a

P<0.001 and

b

P<0.05.