A rapid and highly sensitive method for the determination of glimepiride in human plasma by liquid chromatography–electrospray ionization tandem mass spectrometry: application to a pre‐clinical pharmacokinetic study

Lagishetty, Chakradhar V.; Kallem, Rajareddy; Karthik, A.; Sundari, Bala Tripura; Ramesh, S.; Mullangi, Ramesh; Srinivas, Nuggehally R.

doi:10.1002/bmc.896

Cited by 30 publications

(15 citation statements)

References 15 publications

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“…8 There are two polymorphs of this molecule reported in the literature, form I and form II, of which form II has about 3.5-fold higher solubility than that of form I. 9 There is a growing number of studies describing the determination of glimepiride concentration in biological fluids [10][11][12][13][14][15][16][17][18] and pharmaceutical formulations [19][20][21][22][23][24][25][26][27][28][29][30] using a variety of methods. However, there is no dissolution method for glimepiride tablets in the literature.…”

Section: Introductionmentioning

confidence: 99%

A Discriminating Dissolution Method for Glimepiride Polymorphs

Bonfílio

Pires

Ferreira

et al. 2012

Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 99%

A Discriminating Dissolution Method for Glimepiride Polymorphs

Bonfílio

Pires

Ferreira

et al. 2012

Journal of Pharmaceutical Sciences

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“…A rapid and reliable LC-MS/MS bioanalytical method was developed for simultaneous quantification of GMP and TA in rat plasma. [15][16][17][18] This method was applied successfully to study the plasma pharmacokinetics of GMP and TA in rats. We also conducted mechanistic studies to elucidate the pharmacokinetic interaction between GMP and PDT that has been demonstrated in this study.…”

Section: )mentioning

confidence: 99%

Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats

Kim

Choi

et al. 2015

Biological & Pharmaceutical Bulletin

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The objective of the present work was to investigate the potential for pharmacokinetic drug-drug interactions between glimepiride (GMP) and piperazine dithioctate (PDT) in rats to support the development of an orally combined product of the two drugs. An LC-MS/MS bioanalytical method was developed for simultaneous quantification of GMP and thioctic acid (TA) in rat plasma. The accuracy, precision, linearity, selectivity, and recovery were all within an acceptable range. The oral plasma exposure of the GMP solution was more than 14-times greater than that of the GMP suspension at a dose of 0.5 mg/kg, suggesting a dissolutionlimited absorption of the GMP suspension. Oral co-administration of PDT (72 mg/kg) with GMP suspension (0.5 mg/kg) reduced the plasma GMP exposure by approximately 80% without a significant change in t 1/2 and t max . Oral co-administration of PDT with GMP solution had no significant effect on the plasma pharmacokinetics of GMP. PDT lowered the pH (from ca. 7 to 5.6) and the dissolved GMP concentration in the GMP suspension. It was also shown that GMP was more soluble at pH 7 than at 5.7 in an aqueous solution, and the oral plasma exposure of a GMP suspension at pH 7.0 was substantially higher than that of a suspension at pH 5.7. These results suggest that the pH-dependent solubility of GMP was likely responsible for PDT's effect on the oral absorption of GMP. In conclusion, the current work suggests a possibility of drug-drug interaction between GMP and PDT upon oral co-administration.Key words glimepiride; piperazine dithioctate; pharmacokinetics; thioctic acid; drug-drug interaction Glimepiride (GMP) (Fig. 1) is a medium-to long-acting oral sulfonylurea widely prescribed to treat type 2 diabetes. 1)GMP lowers blood glucose by stimulating the release of insulin and by enhancing the activity of intracellular insulin receptors.2,3) GMP is rapidly and completely absorbed following oral administration, with a bioavailability close to 100% and a t max of 2-3 h in humans. 4) GMP is eliminated mainly by metabolism by CYP2C9, and the mean plasma elimination half-life (t 1/2 ) is 5-8 h in humans. 5)Thioctic acid (TA) (Fig. 1) is an antioxidant present in prokaryotic and eukaryotic cells. It has been administered for the treatment of various oxidative stress-related diseases, including alcoholic liver disease, diabetes, glaucoma, and neurodegenerative disorders.6,7) TA can also decrease neuropathy symptoms, therefore, it has been approved as a prescription drug for the treatment of diabetic polyneuropathy, and has been frequently co-prescribed with GMP. [8][9][10][11] TA also is widely available as a nutritional supplement in the United States. TA was shown to be absorbed rapidly with a t max of 0.8 h following a single oral dose of 200 mg in humans, and its mean oral bioavailability is 29.1%, with a mean t 1/2 of 0.5 h. 12)Piperadine dithioctate (PDT) (Fig. 1) is a piperazine salt of TA with physicochemical properties more suitable for formulations than TA itself. The melting points of PDT and TA are...

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“…M1 has one-third the pharmacological activity of the parent drug, whereas M2 has no effect (Rosenkranz et al, 1996). A method using liquid chromatography/mass spectrometry (LC/MS) to determine glimepiride in human plasma was reported by a couple of groups (Salem et al, 2004;Pistos et al, 2005;Chakradhar et al, 2008), and a method for determination in equine plasma was reported by Ho et al (2004). However, the simultaneous measurement of M1, M2, and glimepiride in human serum has been introduced only by Lehr and Damm (1990).…”

Section: Introductionmentioning

confidence: 95%

Simultaneous determination of glimepiride and its metabolites in human plasma by liquid chromatography coupled to a tandem mass spectrometry

et al. 2011

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Glimepiride, a second-generation sulfonylurea, is a glucose-lowering agent widely used to treat diabetes mellitus. It is converted into metabolite M1 by CYP2C9, and M1 is then transformed into the carboxyl derivative M2 by cytosolic enzymes. In this study, we introduce a sensitive liquid chromatography/tandem mass spectrometry (LC/MS/MS) method for determining glimepiride, M1, and M2 in human plasma. After simple protein precipitation with acetonitrile, the analytes were chromatographed on a reversed-phase CN column with a mobile phase of 10 mM ammonium acetate aqueous solution and acetonitrile (1:1, v/v). The accuracy and precision of the assay were in accordance with FDA regulations for the validation of bioanalytical methods. This method was used to measure the concentrations of glimepiride, M1, and M2 in plasma after a single oral 2-mg dose of glimepiride in volunteers.

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A rapid and highly sensitive method for the determination of glimepiride in human plasma by liquid chromatography–electrospray ionization tandem mass spectrometry: application to a pre‐clinical pharmacokinetic study

Cited by 30 publications

References 15 publications

A Discriminating Dissolution Method for Glimepiride Polymorphs

A Discriminating Dissolution Method for Glimepiride Polymorphs

Effect of Piperazine Dithioctate on the Oral Pharmacokinetics of Glimepiride in Rats

Simultaneous determination of glimepiride and its metabolites in human plasma by liquid chromatography coupled to a tandem mass spectrometry

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