Analysis of nifedipine and its pyridine metabolite dehydronifedipine in blood and plasma: Review and improved high-performance liquid chromatographic m

Soons, P. A.; Schellens, J.H.M.; Roosemalen, M.C.M.; Breimer, D.D.

doi:10.1016/0731-7085(91)80249-9

Cited by 30 publications

(18 citation statements)

References 51 publications

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“…Assay of NFP The NFP concentrations in rat plasma were determined by means of the HPLC-UV method reported by Waller et al 13) and Soons et al 14) with a slight modification as follows. Plasma samples of 100 ml were placed in shaded glass tubes (10 ml) to prevent photo-degradation, and 5 mg/ml of nicardipine-toluene solution (internal standard; 100 ml) and 100 ml of 0.1 M sodium hydroxide were added.…”

Section: Methodsmentioning

confidence: 99%

Studies on Interactions between Functional Foods or Dietary Supplements and Medicines. III. Effects of Ginkgo biloba Leaf Extract on the Pharmacokinetics of Nifedipine in Rats

Yoshioka

Ohnishi

Sone

et al. 2004

Biological & Pharmaceutical Bulletin

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Standardized Ginkgo biloba leaf extract (GBE) is a widely used dietary supplement for the treatment or prevention of Alzheimer's disease, failing memory, age-related dementias, etc. in Japan as well as the United State, and now a phytomedicine in many countries in Europe.1) GBE consists of many flavonoid glycosides and various unique diterpenes such as ginkgolides, which are potent inhibitors of platelet activating factor.1) It is highly likely that GBE is used in combination with various medicines by many patients.Previously, we reported that the simultaneous addition of GBE to the rat small intestine and liver microsomes inhibited the formation of N-demethyl diltiazem (MA), an active metabolite of diltiazem (DTZ) produced by a well-known drug metabolizing enzyme P450 (CYP) 3A, in a concentration-dependent manner.2) This inhibition appeared to be caused, at least in part, by a mechanism-based inhibition. Both the rate of formation of MA and total amount of CYP in intestinal or hepatic microsomes after a single oral pretreatment with GBE (20 mg/kg) decreased transiently. Furthermore, it was found the concomitant use of GBE in rats significantly increased the bioavailability after oral administration of DTZ, a typical substrate of CYP3A, as well as a highly extracted drug, while the elimination after intravenous administration of DTZ was slightly delayed by simultaneous oral treatment with GBE.2) These findings suggest that there is a possibility of potential pharmacokinetic interactions between GBE and other drugs that are both substrates for CYP3A and extensively extracted drugs.3,4) However, there are still many unclear points regarding the inhibitory mechanism of action because DTZ is a substrate of not only CYP3A, but also esterase in rats and humans, 5) and of the multidrug transporter P-glycoprotein (P-gp) which is expressed in normal tissues with excretory function, playing an important role in drug pharmacokinetics. [6][7][8] Therefore, in this study, we examined the effects of simultaneous oral treatment with GBE on the pharmacokinetics of nifedipine (NFP), which is a representative substrate of CYP3A, but not P-gp, [6][7][8] and is at first metabolized only to dehydronifedipine (NFPO) in the intestine and liver in both rats and humans, 9-13) after intravenous and oral administration of NFP to rats. MATERIALS AND METHODSChemicals GBE (Ginkgolon-24; Lot No. 830301034) powders were kindly provided by Tokiwa Phytochemical Co., Ltd. (Chiba, Japan). GBE was produced using a standard method by extraction from milled leaves with ethanol. The final quality of this extract was assured by maintaining the prescribed range of index components (over 24% flavonoid glycosides and 6% terpene lactones and less than 1 ppm ginkgolic acids). NFP, nicardipine (an internal standard for HPLC analysis) and polyethylene glycol (PEG) 400 were purchased from Wako Pure Chemical Ind., Ltd. (Osaka, Japan). All other chemicals were reagent-or HPLC-grade commercial products.Animals Nine-week-old male Wistar rats (Japan SLC, Inc., Hama...

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Section: Methodsmentioning

confidence: 99%

Studies on Interactions between Functional Foods or Dietary Supplements and Medicines. III. Effects of Ginkgo biloba Leaf Extract on the Pharmacokinetics of Nifedipine in Rats

Yoshioka

Ohnishi

Sone

et al. 2004

Biological & Pharmaceutical Bulletin

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“…Assays of NFP and NFPO Plasma NFP and NFPO (a major metabolite of NFP) concentrations were simultaneously determined by means of the HPLC-UV method reported by Soons et al 17) with slight modifications as follows. Plasma samples of 1 ml were placed in shaded glass tubes (10 ml) to prevent photo-degradation, and 500 ng/ml of nicardipine-toluene solution (internal standard; 0.1 ml) and 1 ml of 0.1 M sodium hydroxide were added.…”

Section: Methodsmentioning

confidence: 99%

Studies on Interactions between Functional Foods or Dietary Supplements and Medicines. IV. Effects of Ginkgo biloba Leaf Extract on the Pharmacokinetics and Pharmacodynamics of Nifedipine in Healthy Volunteers

Yoshioka

Ohnishi

Koishi

et al. 2004

Biological & Pharmaceutical Bulletin

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“…Roosmemalen et al [22] Streel et al [25] Wang et al [26] Wang et al [27] Patel et al [28] Plasma volume (ml) …”

Section: Referencementioning

confidence: 99%

“…Although Roosmemalen et al reported a method on estimation of polar metabolites of nifedipine, arresting ex vivo inter-conversion among metabolites and analyte [22] remained unaddressed. Reported LC-MS/MS methods showed marked limitations as these methods are not tuned to labile metabolite separation and arresting ex vivo degradation of nifedipine [25][26][27][28]. Role of dwell time in MS, special analytical precautions, use of appropriate anticoagulant along with detailed stability in diverse type of matrices remained unmet (Table 1).…”

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confidence: 99%

“…These methods include HPLC [8][9][10][11][12][13][14] coupled with UV detectors or electrochemical detector, but tedious sample processing technique, lengthy analysis time and lack of sensitivity were major limitations in these methods. Diverse detection techniques like electron-capture detection [15][16][17][18][19][20], nitrogen phosphorus detection [21] and mass spectrometric (MS) detection [22,23] were reported. However, scope of thermal decomposition of nifedipine under gas chromatography conditions was a co ncern and MS methods are usually preferred.…”

mentioning

confidence: 99%

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Method Development Challenges and Regulatory Expectation in Nifedipine

Goswami

Gurule

Singh

et al. 2016

Int. J. Pharmacokinet.

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Aim: A novel and accurate high-throughput tandem mass spectroscopic method has been developed and validated for determination of nifedipine, a calcium-channel blocker. Materials & methods: Nifedipine was detected on a triple quadruple tandem mass spectrometer by multiple reactions monitoring mode via ESI source. Results: The selective and sensitive method was linear in the concentration range of 0.501 to 360.100 ng/ml and reported no matrix effect. The percent accuracy of the method was found to be between 99.7 and 102.80%, while percentage of RSD was in range of 1.77 to 4.73%. Conclusion: Validated method was used for bioavailability studies under fasting and fed conditions. Clinical pharmacokinetics of noncommunicable disease such as hypertension has interested the academicians and practitioners alike due to intricacies and limited knowledge of labile metabolites. Calciumchannel blocker drug slows down the progression of coronary artery calcification. Nifedipine (1,4-dihydro-2, 6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine dicarboxylic acid dimethyl ester), belonging to the group of 1,4-dihydropyridines is one of the highly prescribed calcium-channel blockers that selectively dilates peripheral arteries [1]. It is widely used in the treatment of cardiovascular diseases such as hypertension, angina pectoris and Raynaud's phenomenon [2][3][4]. It inhibits the influx of extracellular calcium through myocardial and vascular membrane pores as well as restricts contractile processes of smooth muscle cells thereby decreasing total peripheral resistance and systemic blood pressure [5,6]. However, developing a robust method for analysis of Nifedipine in plasma is highly challenging due to multiple reasons. Nifedipine is a photo-labile compound, undergoing oxidative biotransformation in human body into pharmacologically inactive metabolites, dehydronifedipine and hydroxydehydro nifedipine carboxylate [7].In recent past, several analytical methods were reported for the determination of nifedipine in biological matrix. These methods include HPLC [8][9][10][11][12][13][14] coupled with UV detectors or electrochemical detector, but tedious sample processing technique, lengthy analysis time and lack of sensitivity were major limitations in these methods. Diverse detection techniques like electron-capture detection [15][16][17][18][19][20], nitrogen phosphorus detection [21] and mass spectrometric (MS) detection [22,23] were reported. However, scope of thermal decomposition of nifedipine under gas chromatography conditions was a co ncern and MS methods are usually preferred.Nifedipine is metabolized by cytochrome P-450 IIIA4 enzymatic activity, in vivo. Nifedipine metabolism involves oxidative dehydrogenation to dehydronifedipine, followed

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Analysis of nifedipine and its pyridine metabolite dehydronifedipine in blood and plasma: Review and improved high-performance liquid chromatographic m

Cited by 30 publications

References 51 publications

Studies on Interactions between Functional Foods or Dietary Supplements and Medicines. III. Effects of Ginkgo biloba Leaf Extract on the Pharmacokinetics of Nifedipine in Rats

Studies on Interactions between Functional Foods or Dietary Supplements and Medicines. III. Effects of Ginkgo biloba Leaf Extract on the Pharmacokinetics of Nifedipine in Rats

Studies on Interactions between Functional Foods or Dietary Supplements and Medicines. IV. Effects of Ginkgo biloba Leaf Extract on the Pharmacokinetics and Pharmacodynamics of Nifedipine in Healthy Volunteers

Method Development Challenges and Regulatory Expectation in Nifedipine

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