Sex differences in the pharmacokinetics of pioglitazone in rats

Fujita, Yukiyoshi; Yamada, Yasuhiko; Kusama, Makiko; Yamauchi, Toshimasa; Kamon, Junji; Kadowaki, Takashi; Iga, Tatsuji

doi:10.1016/s1532-0456(03)00194-7

Cited by 42 publications

(45 citation statements)

References 24 publications

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“…The mean volume of distribution (0.30 L/kg) in sheep after a single IV dosing (10 mg/kg) is close to that in humans (0.25 L/kg) after injection of 5 mg PGT (Eckland and Danhof 2000). In addition, the volume of distribution of the drug after oral administration in our study is higher than that reported for male rats (Fujita et al 2003) (0.38 vs. 0.27 L/kg; Table 2). …”

Section: Discussioncontrasting

confidence: 78%

“…The k el values in two different studies using rats (Fujita et al 2003;Umathe et al 2008) are actually close to the value in sheep (0.26 and 0.22 vs. 0.16 h (1 , respectively; Table 2). …”

Section: Discussionsupporting

confidence: 66%

“…The t 1/2 of PGT after oral administration in male rats (Fujita et al 2003) is less than the value found in sheep (2.5 vs. 4.42 h; Table 2). The clearance of PGT is not reported in the above study.…”

Section: Discussionmentioning

confidence: 65%

“…The mean absorption rate constant (k ab ) after oral administration of PGT in sheep is low and was found to be less than that in male rats (0.16 vs. 0.38 h (1 ; Table 2) (Fujita et al 2003). The values reported for k ab after oral administration of 7.5 mg PGT in humans (Eckland and Danhof 2000) comprise a broader range (0.4Á1.2 h…”

Section: Discussionmentioning

confidence: 98%

“…Therefore, it seems that evaluation of pharmacokinetics parameters and bioavailability of drugs can lead us to determine optimal dosage of drugs in ruminants. Pharmacokinetics of PGT has been investigated in humans (Eckland and Danhof 2000;Budde et al 2003;Kalliokoski et al 2008), rats (Fujita et al 2003;Umathe et al 2008) and horses (Wearn et al 2010), but there is no published data on the pharmacokinetics of PGT in sheep. Thus, the aim of present study was to determine the bioavailability and some other pharmacokinetic parameters of PGT in sheep, as a ruminant model, to define a dosage regimen for the drug administration in sheep as a potential feed additive (growth promoter) due to its useful effects on blood chemistry (e.g., nonesterified fatty acid [NEFA]), lowering the rate of metabolic disorders, improving reproduction and meat marbling.…”

mentioning

confidence: 99%

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Pharmacokinetics of pioglitazone, a thiazolidinedione derivative, in male Naeini (Iranian fat-tailed) sheep

Ghoreishi

Rajaian

Sheykhzade

et al. 2012

Journal of Applied Animal Research

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Pioglitazone (PGT) belongs to thiazolidinedione (TZD) family or insulin sensitizers that are potent ligands for peroxisome proliferator activated receptor gamma and are used in the treatment of type 2 diabetes mellitus. It has been shown that injection of TZD in cattle has some useful effects on blood parameters but there is no published study with respect to the feeding of TZDs in ruminants till now. Therefore, the aim of this study was to determine the bioavailability and several other pharmacokinetic parameters of PGT in sheep. A single intravenous (IV) or oral dose of PGT (10 mg/kg) was administered to five male sheep. Blood samples were collected at various time intervals, and PGT concentration was measured by a validated high-performance liquid chromatography method. The data obtained were best fitted into a two-compartment model for the IV route, and noncompartmental approach for oral route. The bioavailability of PGT was obtained to be approximately 62%. After IV injection of PGT, the elimination half-life (t 1/2b ), the volume of distribution at steady-state (V ss ) and the elimination rate constant (k el ) were obtained to be 4.0490.88 h, 0.3090.06 L/kg and 0.4790.09 h (1 , respectively. After oral administration of PGT, highest drug concentration observed in plasma (C max ), the time (t max ) at which C max occurs, half-life (t 1/2 ), absorption rate constant (k ab ) and elimination rate constant (k el ) were obtained to be 10.291.3 mg/mL, 6.490.3 h, 4.4290.21 h, 0.1690.01 h(1 and 0.1690.01 h (1 , respectively.

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Section: Discussioncontrasting

confidence: 78%

“…The k el values in two different studies using rats (Fujita et al 2003;Umathe et al 2008) are actually close to the value in sheep (0.26 and 0.22 vs. 0.16 h (1 , respectively; Table 2). …”

Section: Discussionsupporting

confidence: 66%

Section: Discussionmentioning

confidence: 65%

Section: Discussionmentioning

confidence: 98%

mentioning

confidence: 99%

See 3 more Smart Citations

Pharmacokinetics of pioglitazone, a thiazolidinedione derivative, in male Naeini (Iranian fat-tailed) sheep

Ghoreishi

Rajaian

Sheykhzade

et al. 2012

Journal of Applied Animal Research

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The Peroxisome Proliferator–Activated Receptor γ Agonist Pioglitazone Preserves Bone Microarchitecture in Experimental Arthritis by Reducing the Interleukin‐17–Dependent Osteoclastogenic Pathway

Koufany

Chappard

Netter

et al. 2013

Arthritis & Rheumatism

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Gender differences in the hepatic elimination and pharmacokinetics of lobeglitazone in rats

Lee

Son

Chae

et al. 2015

Biopharm & Drug Disp

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The pharmacokinetics of lobeglitazone (LB) was studied after intravenous administration at a dose of 1 mg/kg and oral administration at doses of 0.1, 1 and 10 mg/kg in male and female rats. The area under the plasma concentration-time curve from time zero to infinity (AUC ) after intravenous administration was approximately 7.1 times higher in female rats than in male rats. In addition, the AUC in the case of oral administration was at least 4.4 times higher in female rats and appeared to increase in proportion to the dose in both genders. The in vitro half-lives were 18.8 ± 4.45 min and 60.7 ± 11.2 min, as evidenced by incubating liver microsomes obtained from male and female rats, respectively. As a result, the estimated CL for LB for male rat liver microsomes (0.0779 ± 0.0233 ml/min/mg protein) was much higher than that for female rat liver microsomes (0.0233 ± 0.0039 ml/min/mg protein, p < 0.05). These observations suggest that there are gender differences in the pharmacokinetics and hepatic metabolism for LB in rats. Copyright © 2015 John Wiley & Sons, Ltd.

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Sex differences in the pharmacokinetics of pioglitazone in rats

Cited by 42 publications

References 24 publications

Pharmacokinetics of pioglitazone, a thiazolidinedione derivative, in male Naeini (Iranian fat-tailed) sheep

Pharmacokinetics of pioglitazone, a thiazolidinedione derivative, in male Naeini (Iranian fat-tailed) sheep

The Peroxisome Proliferator–Activated Receptor γ Agonist Pioglitazone Preserves Bone Microarchitecture in Experimental Arthritis by Reducing the Interleukin‐17–Dependent Osteoclastogenic Pathway

Gender differences in the hepatic elimination and pharmacokinetics of lobeglitazone in rats

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