Development and Validation of RP‐HPLC Method for the Determination of Adefovir Dipivoxil in Bulk and in Pharmaceutical Formulation

Zaheer, Ahmed; Gopinath, B.; Shetty, A. Sathish Kumar; Sridhar, B. K.

doi:10.1155/2009/157868

Cited by 10 publications

(8 citation statements)

References 6 publications

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“…The concentration of testosterone in the microsomal samples was determined according to a method reported previously with slight modifications (Ahmed, Gopinath, Shetty, & Sridhar, ). A 100‐μL microsomal sample was deproteinized using 300‐μL acetonitrile containing IS.…”

Section: Methodsmentioning

confidence: 99%

“…The concentration of testosterone in the microsomal samples was determined according to a method reported previously with slight modifications (Ahmed, Gopinath, Shetty, & Sridhar, 2009 expression between the two rat groups. In contrast, intestinal CYP3A1 expression was 458% higher (p = .044) in 1,25(OH) 2 D 3 -treated rats than in control rats (Figure 1b).…”

Section: Hplc Analysismentioning

confidence: 99%

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Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D₃: Effects on in vivo oral absorption and disposition of buspirone in rats

Maeng

Doan

Yoon

2018

Drug Development Research

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1α,25‐Dihydroxyvitamin D3 (also called 1,25(OH)2D3 or calcitriol) is the biologically active form of vitamin D, which functions as a ligand to the vitamin D receptor (VDR). It was previously reported that intestinal cytochrome P450 3A (CYP3A) expression was altered by 1,25(OH)2D3‐mediated VDR activation. However, to clarify whether the change in CYP3A subfamily expression by VDR activation can affect metabolic function, further evidence is needed to prove the effect of 1,25(OH)2D3 treatment on CYP3A‐mediated drug metabolism and pharmacokinetics. Here, we report the effects of 1,25(OH)2D3 on CYP3A activity and in vivo pharmacokinetics of buspirone in Sprague–Dawley rats. CYP3A mRNA expression and CYP3A‐mediated testosterone metabolism were enhanced in the intestine but were unaffected in the livers of rats treated with 1,25(OH)2D3. Notably, the oral pharmacokinetic profile of buspirone (CYP3A substrate drug) and 6′‐hydroxybuspirone (major active metabolite of buspirone formed via CYP3A‐mediated metabolism) was significantly altered, while its intravenous pharmacokinetic profile was not affected by 1,25(OH)2D3 treatment. To the best of our knowledge, this study provides the first reported data regarding the effects of 1,25(OH)2D3 treatment on the in vivo pharmacokinetics of intravenous and oral buspirone in rats, by the differential modulation of hepatic and intestinal CYP3A activity. Our present results could lead to further studies in clinically significant CYP3A‐mediated drug–nutrient interactions with 1,25(OH)2D3, including 1,25(OH)2D3–buspirone interaction. Preclinical Research & Development

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Section: Methodsmentioning

confidence: 99%

“…The concentration of testosterone in the microsomal samples was determined according to a method reported previously with slight modifications (Ahmed, Gopinath, Shetty, & Sridhar, 2009 expression between the two rat groups. In contrast, intestinal CYP3A1 expression was 458% higher (p = .044) in 1,25(OH) 2 D 3 -treated rats than in control rats (Figure 1b).…”

Section: Hplc Analysismentioning

confidence: 99%

Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D₃: Effects on in vivo oral absorption and disposition of buspirone in rats

Maeng

Doan

Yoon

2018

Drug Development Research

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“…26) A 100-µL aliquot of the samples was deproteinized with a 200-µL aliquot of acetonitrile. After vortex-mixing and centrifugation at 16000×g for 10 min, a 50-µL aliquot of the supernatant was directly injected into a reversed phase (C18) HPLC column.…”

Section: Methodsmentioning

confidence: 99%

Effects of 1α,25-Dihydroxyvitamin D<sub>3</sub> on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats

Yoon

Son

Kim

et al. 2015

Biological & Pharmaceutical Bulletin

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The aim of this study was to investigate the effect of 1α,25-dihydroxyvitamin D 3 (1,25(OH) 2 D 3 ), an active form of vitamin D, on the oral absorption and disposition of adefovir dipivoxil (P-glycoprotein (P-gp) substrate) and its major active metabolite, adefovir (multidrug resistance-associated protein 4 (Mrp4) substrate), in rats. The pharmacokinetics of intravenous adefovir and oral adefovir dipivoxil was evaluated in control and 1,25(OH) 2 D 3 -treated rats. The intestinal absorption of adefovir dipivoxil was investigated through an in situ closed loop study, and the tissue distribution of adefovir after oral administration of adefovir dipivoxil was evaluated in the two groups. There was no significant difference in pharmacokinetic parameters of intravenous adefovir between the two groups. Importantly, the total area under the plasma concentration-time curve from time zero to time infinity (AUC), peak plasma concentration (C max ) and extent of absolute oral bioavailability (F) of adefovir after oral administration of adefovir dipivoxil were significantly higher in 1,25(OH) 2 D 3 -treated rats than in control rats. In the in situ closed loop study, there was no significant difference in the remaining fraction of adefovir dipivoxil in the duodenum, jejunum and ileum loops between the two groups. In the tissue distribution study after oral administration of adefovir dipivoxil, the tissue-toplasma partition coefficients of adefovir in the liver, brain, kidney, and intestine were significantly lower in 4) During the past decades, significant physiological roles of VDR in calcium and bone homeostasis have been well established. 5)However, it is increasingly recognized that VDR is also crucial in the regulation of drug transporters, and 1,25(OH) 2 D 3 can lead to VDR-mediated changes in target genes of drug transporters. [6][7][8][9][10] Since VDR is abundantly expressed in the intestine, 11) the effects of 1,25(OH) 2 D 3 (i.e., VDR activation) on the expression of intestinal drug transporters are frequently investigated. 1,25(OH) 2 D 3 increases the mRNA expression and function of multidrug resistance protein 1 (MDR1) in the human colorectal adenocarcinoma cell lines, LS174T and Caco-2 cells in vitro. 8,12) It also increases the protein expressions of multidrug resistance-associated protein 2 and 4 (MRP2 and MRP4) in Caco-2 cells. 8,13) In rats, 1,25(OH) 2 D 3 treatment in vivo increases the protein expressions of Mrp2, Mrp3, Mrp4, and the oligopeptide transporter 1 (PepT1) without altering the mRNA and protein expressions of Mdr1a (P-glycoprotein; P-gp). 14)Moreover, our previous studies using rat everted intestinal sac technique confirmed that the in vitro functions of rat intestinal Mrp2, Mrp4 and PepT1, but not P-gp are induced by 1,25(OH) 2 D 3 treatment via VDR activation. 15) However, changes in the expression and/or in vitro functions of drug transporters do not always correlate with the fates of therapeutic agents in the whole body system. Therefore, further studies are needed on the effects of 1,25(O...

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“…Only one method made use of ultraviolet (UV) for detection of TEN at 259 nm [15]. Other HPLC methods are applied for assay of TEN in bulk powder and in pharmaceutical preparations [20][21][22].…”

Section: Fig 1 Structures Of Tenofovir Disproxyl Fumarate (Ten) Andmentioning

confidence: 99%

Selective RP-HPLC DAD method for determination of tenofovir fumarate and emtricitabine in bulk powder and in tablets

Abdelhay¹,

Gazy²,

Shaalan³

et al. 2015

Acta Chromatographica

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Summary.A simple and selective liquid chromatographic method was developed for the simultaneous determination of tenofovir disoproxil fumarate (TEN) and emtricitabine (EMT) in combined tablets. The method is based on separation of TEN and EMT on a Zorbax SB-C8 column, 5 μm, 4.6 × 250 mm, with a mobile phase consisting of 50 mM disodium hydrogen phosphate-acetonitrile (50:50, v/v). The mobile phase contains 0.1% triethylamine (TEA) and was adjusted to pH 6.0. Quantification of the analytes is achieved with diode array -ultraviolet detector (DAD-UV) at 260 and 280 nm for TEN and EMT, respectively, based on peak area. Different variables affecting the method were carefully investigated and optimized. Reliability and analytical performance of the proposed method, including linearity, range, precision, accuracy, and detection and quantitation limits, were statistically validated. The high-performance liquid chromatography (HPLC) method was successfully applied for determination of each drug in their binary tablets.

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Development and Validation of RP‐HPLC Method for the Determination of Adefovir Dipivoxil in Bulk and in Pharmaceutical Formulation

Cited by 10 publications

References 6 publications

Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D₃: Effects on in vivo oral absorption and disposition of buspirone in rats

Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D₃: Effects on in vivo oral absorption and disposition of buspirone in rats

Effects of 1α,25-Dihydroxyvitamin D<sub>3</sub> on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats

Selective RP-HPLC DAD method for determination of tenofovir fumarate and emtricitabine in bulk powder and in tablets

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Development and Validation of RP‐HPLC Method for the Determination of Adefovir Dipivoxil in Bulk and in Pharmaceutical Formulation

Cited by 10 publications

References 6 publications

Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D3: Effects on in vivo oral absorption and disposition of buspirone in rats

Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D3: Effects on in vivo oral absorption and disposition of buspirone in rats

Effects of 1α,25-Dihydroxyvitamin D<sub>3</sub> on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats

Selective RP-HPLC DAD method for determination of tenofovir fumarate and emtricitabine in bulk powder and in tablets

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Resources

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Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D₃: Effects on in vivo oral absorption and disposition of buspirone in rats

Differential regulation of intestinal and hepatic CYP3A by 1α,25‐dihydroxyvitamin D₃: Effects on in vivo oral absorption and disposition of buspirone in rats