DETERMINATION OF NIFEDIPINE IN RAT PLASMA USING HPLC-UV DETECTOR: A SIMPLE METHOD FOR PHARMACOKINETICS AND ORAL BIOAVAILABILITY STUDIES
Keywords:
Nifedipine, HPLC-UV assay, Validation, Stability, Plasma concentrationAbstract
Objective: To develop and validate a high-performance liquid chromatographic method (HPLC) for the determination of nifedipine (NFD) concentration in rat plasma.Methods: 1.5 mol of sodium hydroxide solution was added to each plasma sample, followed by the addition of an extraction solvent based on n-hexane and dichloromethane (70: 30, v/v). The organic layer was transferred and evaporated to dryness under nitrogen flow. The residue was reconstituted with 0.5 mol of acetic acid, followed by the addition of n-hexane. After centrifuging the mixture, the supernatant organic layer of n-hexane was discarded, and the aqueous solution was injected onto the HPLC using A Phenomenex Luna-C18 reversed phase analytical column (250 x 4.6 mm, 5 µm). The mobile phase consisted of 0.01 mol aqueous ammonium formate: methanol: acetonitrile (55: 43: 2, v/v) with pH adjusted to 4.9 using formic acid. The flow rate was 0.8 ml/min; UV detector set at 235 nm and the samples were quantified using the peak area.Results: A well-resolved NFD peak was achieved free of interference from endogenous compounds in rat plasma. Recovery of NFD was more than 93 % over concentrations ranged from 5.00 to 200 ng/ml. The limit of quantification (LOQ) of this assay was 6 ng/ml and, intra-and inter-day coefficient of variation (CV) were 5.75 % and 7.93 %, respectively. NFD was found to be stable in rat plasma after being stored at -30 °C over 90 d.Conclusion: The stability, sensitivity, specificity and reproducibility of this method make it suitable for the determination of NFD plasma concentration in pharmacokinetics and oral bioavailability studies.Downloads
References
Stone PH, Antman EM, Muller JE, Braunwald E. Calcium channel blocking agents in the treatment of cardiovascular disorders. Part II: hemodynamic effects and clinical applications. Ann Intern Med 1980;93:886-904.
Sorkin EM, Clissold SP, Brogden RN. Nifedipine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy, in ischaemic heart disease, hypertension and related cardiovascular disorders. Drugs 1985;30:182–274.
Cao QR, Cui JH, Park JB, Han HK, Lee J, Oh KT, Park I, Lee BJ. Effect of food components and dosing times on the oral pharmacokinetics of nifedipine in rats. Int J Pharm 2010;396:39-44.
Abrahamsson B, Alpsten M, Bake B, Jonsson UE, Eriksson-Lepkowska M, Larsson A. Drug absorption from nifedipine hydrophilic matrix extended release (ER) tablet-comparison with an osmotic pump tablet and effect of food. J Controlled Release 1998;52:301-10.
Filgueira GC, Filgueira OA, Carvalho DM, Marques MP, Moisés EC, Duarte G, et al. Analysis of nifedipine in human plasma and amniotic fluid by liquid chromatography-tandem mass spectrometry and its application to clinical pharmacokinetics in hypertensive pregnant women. J Chromatogr B: Anal Technol Biomed Life Sci 2015;993-994:20-5.
Raemsch KD, Sommer J. Pharmacokinetics and metabolism of nifedipine. Hypertension 1983;5:18–24.
Eichelbaum M, Echizen H. Clinical pharmacology of calcium antagonists: a critical review. J Cardiovasc Pharmacol 1984;6:S963-7.
Ozaltin N, Yardimci C, Suslu I. Determination of nifedipine in human plasma by square wave adsorptive stripping voltammetry. J Pharm Biomed Anal 2002;30:573-82.
Guengerich FB, Martin MV, Beaune PH, Kremers P, Wolff T, Waxman DJ. Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. J Biol Chem 1986;261:5051–60.
Challenor VF, Waller DG, Renwick AG, Gruchy BS, George CF. The trans-hepatic extraction of nifedipine. Br J Clin Pharmacol 1987;24:473-7.
Rosseel MT, Bogaert MG. Determination of nifedipine in human plasma by capillary gas chromatography with nitrogen detection. J Chromatogr 1983;279:675-80.
Abou-Auda HS, Najjar TA, Al-Hadiya KI, Ghilzai NM, Al-Fawzan NF. Liquid chromatographic assay of nifedipine in human plasma and its application to pharmacokinetic studies. J Pharm Biomed Anal 2000;22:241-9.
Goldnik A, Gajewska M, Marszałek D, Przyzyçki M. Determination of nifedipine in serum by HPLC. Acta Pol Pharm 1996;53:7-8.
Jankowski A, Lamparczyk H. Evaluation of chromatographic methods for the determination of nifedipine in human serum. J Chromatogr A 1994;668:469-73.
Grundy JS, Kherani R, Foster RT. Sensitive high-performance liquid chromatographic assay for nifedipine in human plasma utilizing ultraviolet detection. J Chromatogr B: Biomed Appl 1994;654:146-51.
Schmid BJ, Perry HE, Idle JR. Determination of nifedipine and its three principal metabolites in plasma and urine by automated electron-capture capillary gas chromatography. J Chromatogr 1988;425:107-19.
Patrick KS, Jarvi EJ, Straughn AB, Meyer MC. Gas chromatographic mass spectrometric analysis of plasma nifedipine. J Chromatogr 1989;495:123-30.
Le Guellec C, Bun H, Giocanti M, Durand A. Determination of nifedipine in plasma by a rapid capillary gas chromatographic method. Biomed Chromatogr 1992;6:20-3.
Horváth V, Hrabéczy-Páll A, Niegreisz Z, Kocsi E, Horvai G, Gödörházy L, et al. Sensitive high-performance liquid chromatographic determination of nifedipine in dog plasma using an automated sample preparation system with laboratory robot. J Chromatogr B: Biomed Appl 1996;686:211-9.
Streel B, Zimmer C, Sibenaler R, Ceccato A. Simultaneous determination of nifedipine and dehydronifedipine in human plasma by liquid chromatography-tandem mass spectrometry. J Chromatogr B; Biomed Sci Appl 1998;720:119-28.
Kostewlcz E, Sansom L, Flshlock R, Morella A, Kuchel T. Examination of two sustained release nifedipine preparations in humans and in pigs. Eur J Pharm Sci 1996;4:351-7.
Yritia M, Parra P, Iglesias E, Barbanoj JM. Quantitation of nifedipine in human plasma by on-line solid-phase extraction and high-performance liquid chromatography. J Chromatogr A 2000;870:115-9.
Zhiping L, Mingkang Z, Xiaojin S, Zhongdong L. A solid phase extracted-HPLC method for determining nifedipine in human plasma. J Clin Pharm 2005;14:115-7.
Niopas I, Daftsios AC. Determination of nifedipine in human plasma by solid phase extraction and high-performance liquid chromatography: validation and application to pharmacokinetic studies. J Pharm Biomed Anal 2003;32:1213-8.
Vertzoni MV, Reppas C, Archontaki HA. Sensitive and simple liquid chromatographic method with ultraviolet detection for the determination of nifedipine in canine plasma. Anal Chim Acta 2006;573-574:298-304.
Zendelovska D, Simeska S, Sabinovska O, Kostova E, Milosevska K, Jakovski K, et al. Development of an HPLC method for the determination of nifedipine in human plasma by solid-phase extraction. J Chromatogr B: Anal Technol Biomed Life Sci 2006;839:85-8.
Guo Y, Dai J, Qian G, Guo N, Ma Z, Guo X. Determination of nifedipine in human plasma and its use in bioequivalence study. Int J Pharm 2007;341:91-6.
Wang XD, Li JL, Lu Y, Chen X, Huang M, Chowbay B, et al. Rapid and simultaneous determination of nifedipine and dehydronifedipine in human plasma by liquid chromatography-tandem mass spectrometry: Application to a clinical herb-drug interaction study. J Chromatogr B: Anal Technol Biomed Life Sci 2007;852:534-44.
Dankers J, van den Elshout J, Ahr G, Brendel E, van der Heiden C. Analytical determination of nifedipine in human plasma by flow-injection tandem mass spectrometry. J Chromatogr B: Biomed Sci Appl 1998;710:115-20.
Baranda AB, Mueller CA, Alonso RM, Jimenez RM, Weinmann W. Quantitative determination of the calcium channel antagonists amlodipine, lercanidipine, nitrendipine, felodipine, and lacidipine in human plasma using liquid chromatography-tandem mass spectrometry. Ther Drug Monit 2005;27:44-52.
Golocorbin-Kon S, Mikov M, Arafat M, Lepojevic Z, Mikov I, Sahman-Zaimovic M. Cefotaxime pharmacokinetics after oral application in the form of 3alpha,7alphadihydroxy-12-keto-5beta-cholanate microvesicles in rat. Eur J Drug Metab Pharmacokinet 2009;34:31-6.
Arafat M, Golocorbin Kon S, Mikov M. The measurement of cefotaxime sodium in rat plasma after oral administration: a sensitive HPLC-UV method. Int J Pharm Pharm Sci 2015;7:343-6.
Arafat M. Simple HPLC validated method for determination of diltiazem hydrochloride in human. Int J Pharm Pharm Sci 2014;6:213-6.
Plumley C, Gorman EM, El-Gendy N, Bybee CR, Munson EJ, Berkland C. Nifedipine nanoparticle agglomeration as a dry powder aerosol formulation strategy. Int J Pharm 2009;369:136-43.
Zaater M, Hasan E, Najib N. Trace-level determination of nifedipine in human serum by reversed phase high performance liquid chromatography. Pol J Pharmacol 2000;52:307-12.
Jankowski A, Lamparczyk H. Evaluation of chromatographic methods for the determination of nifedipine in human serum. J Chromatogr A 1994;668:469-73.
Grundy JS, Kherani R, Foster RT. Sensitive high-performance liquid chromatographic assay for nifedipine in human plasma utilizing ultraviolet detection. J Chromatogr B: Biomed Appl 1994;654:146-51.
Thongnopnua P, Viwatwongsa K. Quantitative analysis of nifedipine in plasma by high-performance liquid chromatography. J Pharm Biomed Anal 1994;12:119-25.
Soons PA, Schellens JH, Roosemalen MC, Breimer DD. Analysis of nifedipine and its pyridine metabolite dehydronifedipine in blood and plasma: review and improved high-performance liquid chromatographic methodology. J Pharm Biomed Anal 1991;9:475-84.
Gurley BJ, Buice RG, Sidhu P. Reversed-phase high performance liquid chromatographic determination of nifedipine in human plasma. Ther Drug Monit 1985;7:321-3.
Rashid TJ, Martin U, Clarke H, Waller DG, Renwick AG, George CF. Factors affecting the absolute bioavailability of nifedipine. Br J Clin Pharmacol 1995;40:51-8.
Arafat M. Approaches to achieve an oral controlled release drug delivery system using polymers: a recent review. Int J Pharm Pharm Sci 2015;7:16-21.