Method development and validation of repaglinide in human plasma by HPLC and its application in pharmacokinetic studies

Bakar, Ruzilawati Abu; Wahab, Mohd Nadhir Ab; Ahmad, Imran; Ismail, Zabidah; Gan, Siew Hua

doi:10.1016/j.jpba.2006.12.010

Cited by 50 publications

(31 citation statements)

References 12 publications

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“…Several HPLC methods have been reported in the literature for quantitative determination of MET alone [4] or in combination with other drugs in tablets [5][6][7], human serum and other biological fluids [8][9]. Similarly, a few HPLC methods have been reported for the quantitative determination of REPA in tablets alone or in combination with other drugs [10][11][12], and in human serum and other biological fluids [13,14]. Only one UV spectroscopic method has been reported for the simultaneous determination of these compounds, which, however, lacks stabilityindicating nature [15].…”

Section: Introductionmentioning

confidence: 99%

Validated stability-indicating RP-HPLC UV method for simultaneous determination of metformin and repaglinide

Joshi

Nahire

Shastri

et al. 2012

Acta Chromatographica

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Summary.A simple, rapid, precise, and accurate, stability-indicating reversed phase high performance liquid chromatographic method was developed and validated for simultaneous determination of metformin HCl and repaglinide. The chromatographic separation was achieved on YMC Pack AM ODS (5 μm, 250 mm length × 4.6 mm i.d.) column at a detector wavelength of 210 nm, using an isocratic mobile phase consisting of methanol and 10 mM potassium dihydrogen phosphate buffer (pH 2.5) in a ratio of 70:30 v/v at a flow rate of 1 mL min −1 . The retention times for metformin and repaglinide were found to be 2.6 and 11.3 min, respectively. The drugs were exposed to thermal, photolytic, hydrolytic, and oxidative stress conditions, and the stressed samples were analyzed by the proposed method. Validation of the method was carried out as per International Conference on Harmonization (ICH) guidelines. Linearity was established for metformin and repaglinide in the range of 5-200 μg mL −1 and 1-200 μg mL −1 , respectively. The limits of detection were 0.3 μg mL −1 and 0.13 μg mL −1 for metformin and repaglinide, respectively. The method was found to be specific and stability-indicating as no interfering peaks of degradants and excipients were observed. The proposed method is hence suitable for application in quality-control laboratories for quantitative analysis of both the drugs individually and in combination, since it is simple and rapid with good accuracy and precision.

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Section: Introductionmentioning

confidence: 99%

Validated stability-indicating RP-HPLC UV method for simultaneous determination of metformin and repaglinide

Joshi

Nahire

Shastri

et al. 2012

Acta Chromatographica

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“…RPG in plasma was determined by RP-HPLC method reported previously (31), with slight modification. Chromatographic separation was carried out with a Thermo Scientific ODS Hypersil C-18 column (4.8 mm×150 mm; 5 μm) attached with guard column.…”

Section: Bioanalytical Methodsmentioning

confidence: 99%

Ultra Rapidly Dissolving Repaglinide Nanosized Crystals Prepared via Bottom-Up and Top-Down Approach: Influence of Food on Pharmacokinetics Behavior

2014

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Abstract. The present work was undertaken with the objectives of improving the dissolution velocity, related oral bioavailability, and minimizing the fasted/fed state variability of repaglinide, a poorly watersoluble anti-diabetic active by exploring the principles of nanotechnology. Nanocrystal formulations were prepared by both top-down and bottom-up approaches. These approaches were compared in light of their ability to provide the formulation stability in terms of particle size. Soluplus® was used as a stabilizer and Kolliphor™ E-TPGS was used as an oral absorption enhancer. In vitro dissolution profiles were investigated in distilled water, fasted and fed state simulated gastric fluid, and compared with the pure repaglinide. In vivo pharmacokinetics was performed in both the fasted and fed state using Wistar rats. Oral hypoglycemic activity was also assessed in streptozotocin-induced diabetic rats. Nanocrystals TD-A and TD-B showed 19.86 and 25.67-fold increase in saturation solubility, respectively, when compared with pure repaglinide. Almost 10 (TD-A) and 15 (TD-B)-fold enhancement in the oral bioavailability of nanocrystals was observed regardless of the fasted/fed state compared to pure repaglinide. Nanocrystal formulations also demonstrated significant (p<0.001) hypoglycemic activity with faster onset (less than 30 min) and prolonged duration (up to 8 h) compared to pure repaglinide (after 60 min; up to 4 h, respectively).

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“…5 A few HPLC methods have been reported in the literature for the quantitative determination of repaglinide in tablets, human serum and other biological fluids. [6][7][8][9] Repaglinide is produced as a single isomer and (R)-enantiomer could be present as a chiral impurity. An HPLC method was reported in the literature for the enantiomeric separation of repaglinide using chiral AGP (protein based chiral stationary phase) column 10 and Chiralpak AD-H (amylose based stationary phase) column.…”

Section: Repaglinide (Figure 1) Single Enantiomer Is Chemically (S)-(mentioning

confidence: 99%

A validated chiral LC method for the enantiomeric separation of repaglinide on immobilized amylose based stationary phase

Patil¹,

Rane²,

Yeole³

et al. 2012

J. Braz. Chem. Soc.

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Um método de HPLC quiral em fase normal, simples, rápido, isocrático, foi desenvolvido e validado para a separação enantiomérica de repaglinida, ácido (S)-(+)-2-etóxi-4-N [1-(2-piperidinofenil)-3-metil-1-butil] aminocarbonilmetil] benzóico, uma substância antidiabética. Os enantiômeros de repaglinida foram resolvidos em uma coluna Chiralpak IA (fase estacionária a base de amilose imobilisada) usando uma fase móvel consistindo de n-hexano:etanol:ácido trifluoroacético (80:20:20, v/v/v) a uma vazão de 1,0 mL min -1 . A resolução encontrada entre os enantiômeros foi maior do que 2 no método otimizado. O método desenvolvido foi extensivamente validado e mostrou-se robusto, enantiosseletivo, exato, preciso e adequado para determinação quantitativa de (R)-enantiômero na substância a granel e no produto formulado.A simple, rapid, isocratic, normal phase chiral HPLC method was developed and validated for the enantiomeric separation of repaglinide, (S)-(+)-2-ethoxy-4-N [1-(2-piperidinophenyl)-3-methyl-1-butyl] aminocarbonylmethyl] benzoic acid, an antidiabetic drug substance. The enantiomers of repaglinide were resolved on a Chiralpak IA (immobilized amylose based stationary phase) column using a mobile phase consisting of n-hexane:ethanol:trifluoroacetic acid (80:20:0.2, v/v/v) at a flow rate of 1.0 mL min -1 . The resolution between both enantiomers was greater than 2 in the optimized method. The developed method was extensively validated and proved to be robust, enantioselective, accurate, precise, and suitable for quantitative determination of (R)-enantiomer in bulk drug substance and product.

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Method development and validation of repaglinide in human plasma by HPLC and its application in pharmacokinetic studies

Cited by 50 publications

References 12 publications

Validated stability-indicating RP-HPLC UV method for simultaneous determination of metformin and repaglinide

Validated stability-indicating RP-HPLC UV method for simultaneous determination of metformin and repaglinide

Ultra Rapidly Dissolving Repaglinide Nanosized Crystals Prepared via Bottom-Up and Top-Down Approach: Influence of Food on Pharmacokinetics Behavior

A validated chiral LC method for the enantiomeric separation of repaglinide on immobilized amylose based stationary phase

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