Hyperlipidemia Alters the Pharmacokinetics of Posaconazole and Vincristine Upon Co-Administration in Rats

Khalil, Hadeel A.; Elkhatib, Mohammed A.W.; Belal, Tarek S.; El-Yazbi, Ahmed F.; Hamdy, Dalia A.

doi:10.1007/s40268-017-0178-8

Cited by 10 publications

(6 citation statements)

References 36 publications

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“…The t 1/2 of Gb in NL rats was calculated as 19.51 h while the t 1/2 in HL rats was noted as 7.59 h, although the difference was not significant. The results of present study are in agreement with the previous findings that reported lesser t 1/2 of investigated drug in HL rats ( Katnapally et al, 2009 , Khalil et al, 2017 , Khalil et al, 2016 ). The CL of Gb in NL rats was recorded as 2.53 ml/h while the CL in HL rats was noted as 1.39 ml/h.…”

Section: Resultssupporting

confidence: 94%

“…HL was induced by single intraperitoneal injection of 1 g/kg of Poloxamer-407. Control and the HL groups were dosed with the drug; HL group were treated after 36 h from the P407 injection ( Chaudhary and Brocks, 2013 , Khalil et al, 2017 , Khalil et al, 2016 ).…”

Section: Methodsmentioning

confidence: 99%

“…HL has also been associated with a decreased level of expression and some activity of cytochrome P450 (CYP) isoforms that are primarily engaged in drug metabolism ( Patel and Brocks, 2009 ). Antecedently, HL has been shown to modify the pharmacokinetic profile of several candidate in rats ( Khalil et al, 2017 , Khalil et al, 2016 , Lee et al, 2012 , Lee et al, 2019 Bin Jardan and Brocks, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

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Assessment of glibenclamide pharmacokinetics in poloxamer 407-induced hyperlipidemic rats

Jardan

Ahad

Raish

et al. 2021

Saudi Pharmaceutical Journal

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The aim of the present research was to describe the consequences of hyperlipidemia (HL) on the pharmacokinetics of glibenclamide (Gb) in poloxamer 407-induced hyperlipidemic rats. Rats were given intraperitoneal dose of poloxamer 407 to cause hyperlipidemia. A single oral dose of Gb (10 mg/Kg) was given to normal and HL rats. The C max and t max after oral dose of Gb in normal rats were 340.10 µg/ml and 3.67 h, respectively. Whereas, the C max and t max after oral dose of Gb in HL rats were noted as 773.39 µg/ml and 2.50 h respectively. The AUC value of Gb was found considerably higher in the HL rats. While the plasma clearance (CL) after oral dose of Gb was 2.53 ml/h and 1.39 ml/h in normal and HL rats respectively. The improved plasma concentration of Gb following oral dosing in rats with HL seems to be due to a direct influence on hepatic clearance or metabolizing enzymes. In conclusion, the Gb pharmacokinetics was considerably affected by the HL in rats. Such findings play an important role for predicting the alterations in the pharmacokinetics of drugs including GB, in cases having hyperlipidemia.

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Section: Resultssupporting

confidence: 94%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Assessment of glibenclamide pharmacokinetics in poloxamer 407-induced hyperlipidemic rats

Jardan

Ahad

Raish

et al. 2021

Saudi Pharmaceutical Journal

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“…Restricted transmembrane transport caused by protein binding results in a reduction in metabolism and excretion and an elevation of plasma concentrations, which fits with the findings of M10 31 . However, this study did not find a relationship between albumin and PK parameters, indicating that the CL/F of posaconazole may be influenced by other plasma-binding proteins such as lipoprotein 59,60 and C-reactive protein (CRP) 54 . M2 24 found that posaconazole exposure decreased with the baseline bilirubin [?]…”

Section: Discussioncontrasting

confidence: 71%

A review of population pharmacokinetic models of posaconazole

Ding

Huang

Sun

et al. 2022

Preprint

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Aims: Posaconazole is often used for the prophylaxis and treatment of invasive fungal infections (IFI). However, intra- and inter-individual differences and drug interactions affect the efficacy and safety of posaconazole. Precision dosing of posaconazole based on the population pharmacokinetic (PopPK) model may assist in making significant clinical decisions. This review aimed to comprehensively summarize the published PopPK models of posaconazole and analyze covariates that significantly influence posaconazole exposure. Methods: Articles published until May 2022 for PopPK analysis of posaconazole were searched in PubMed and EMBASE databases. Demographic characteristics, model characteristics, and results of PopPK analysis were extracted from the selected articles. In addition, the steady-state pharmacokinetic profiles of posaconazole were simulated at different covariate levels and dosing regimens. Results： Out of the 13 studies included in our review, nine studies included adults, three included children, and one included both adults and children. All oral administration models were one-compartment models, and all intravenous administration models were two-compartment models. Body weight, proton pump inhibitors, and incidence of diarrhea were found to be important covariates. In addition, age, sex, total protein, rifampin, phenytoin, intake of nutritional supplements, levels of bilirubin and gamma-glutamyl transferase, and administration of chemotherapy also appeared as covariates in several PopPK models. Conclusion: Posaconazole exposure was found to be influenced by various factors such as the type of formulation, the incidence of diarrhea, body weight, and use of concomitant medications. It was concluded that routine therapeutic drug monitoring was required for dose adjustment and in promoting individualized dosing.

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“…The transport of pharmaceutical components is varied due to the interaction between the components [12]. Thus, it is necessary to further study and quantitatively express the interaction and change process of chemical composition in vivo [13,14]. The plasma concentration method can provide scientific and objective pharmacokinetic parameters reveal the rationality of compatibility, which provides scientific basis for the optimization of prescription compatibility and clinical application [15,16].…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic Study on Protocatechuic Aldehyde and Hydroxysafflor Yellow A of Danhong Injection in Rats with Hyperlipidemia

Zhou¹,

Li²,

Jin³

et al. 2018

Pharmacology

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Background: Protocatechuic aldehyde (PAL) and hydroxysafflor yellow A (HSYA) are 2 effective ingredients of Danhong Injection, which is extensively used for the clinical treatment of cardio-cerebrovascular diseases. This study aims to investigate the pharmacokinetic differences between single and combined medication of PAL and HSYA and analyze the interaction of the above effective components in hyperlipidemia rats. Methods: Thirty male SD rats were randomly divided into the control group (n = 6) and the model group (n = 24). The hyperlipidemia model was established by feeding with superfatted forage. The successful model rats were then randomly divided into the PAL group (16 mg/kg), the HSYA group (10 mg/kg), and the combination group (16 mg/kg + 10 mg/kg). Administration through tail-vein, and orbital blood was sampled at different time points. The mass concentration of PAL and HSYA was determined by high performance liquid chromatography (HPLC-DAD). Analysis of pharmacokinetic parameters was conducted by using DAS 3.2.6 software and SPSS 19.0 statistical analysis software. Results: According to the parameters of statistical moment of non-compartmental model, there was a significant difference in plasma clearance (CL) between the PAL group and the drug combination group (p < 0.01), as well as in the area under the first moment of the plasma concentration-time curve and the elimination half-life (t_1/2) between the HSYA group and the drug combination group (p < 0.01) but no obvious differences about the blood concentration time curve area, the average dwell time (MRT), and the peak concentration (C_max; p > 0.05). Conclusion: The combined medication of PAL and HSYA could increase the plasma CL significantly and have a great influence on the absorption of HSYA in rats with hyperlipidemia.

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Hyperlipidemia Alters the Pharmacokinetics of Posaconazole and Vincristine Upon Co-Administration in Rats

Cited by 10 publications

References 36 publications

Assessment of glibenclamide pharmacokinetics in poloxamer 407-induced hyperlipidemic rats

Assessment of glibenclamide pharmacokinetics in poloxamer 407-induced hyperlipidemic rats

A review of population pharmacokinetic models of posaconazole

Pharmacokinetic Study on Protocatechuic Aldehyde and Hydroxysafflor Yellow A of Danhong Injection in Rats with Hyperlipidemia

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